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Information on EC 2.7.10.2 - non-specific protein-tyrosine kinase and Organism(s) Homo sapiens and UniProt Accession P00519

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EC Tree
IUBMB Comments
Unlike EC 2.7.10.1, receptor protein-tyrosine kinase, this protein-tyrosine kinase does not have a transmembrane domain. In the human genome, 32 non-specific protein-tyrosine kinases have been identified and these can be divided into ten families .
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This record set is specific for:
Homo sapiens
UNIPROT: P00519
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
bcr-abl, focal adhesion kinase, c-abl, zap-70, src kinase, janus kinase, v-src, ephb4, p56lck, bruton's tyrosine kinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Abl kinase
-
Abl protein tyrosine kinase
-
Abl tyrosine kinase
-
ABL1 tyrosine kinase
-
Bcr-Abl kinase
-
c-Abl tyrosine kinase
-
c-Src tyrosine kinase
-
non-receptor tyrosine kinase ABL
-
proto-oncogene tyrosine-protein kinase ABL1
-
70 kDa zeta-associated protein
-
-
-
-
A-Raf proto-oncogene serine/threonine-protein kinase
-
Abelson murine leukemia viral homolog (1) protein
-
-
Abelson tyrosine kinase
-
-
Abl kinase
-
-
Abl nonreceptor tyrosine kinase
-
-
Abl protein tyrosine kinase
-
-
Abl tyrosine kinase
-
-
ABL1
-
-
ABL2
-
-
ABL2/ARG tyrosine kinase
-
-
activated Cdc42-associated tyrosine kinase 1
-
activin receptor type I
-
activin receptor type II
-
ACTR-IIB
-
-
-
-
ACTRIIA
-
-
-
-
Agammaglobulinaemia tyrosine kinase
-
-
-
-
Amylovoran biosynthesis membrane-associated protein amsA
-
-
-
-
anti-mullerian hormone type II receptor
-
ATK
-
-
-
-
B cell progenitor kinase
-
-
-
-
B lymphocyte kinase
-
-
-
-
B-cell/myeloid kinase
-
-
-
-
B-Raf proto-oncogene serine/threonine-protein kinase
-
BCR-Abl
-
-
BCR-ABL tyrosine kinase
BCR/ABL kinase
-
-
Blk kinase
-
BMK
-
-
-
-
BMP type II receptor
-
-
-
-
BMP-2/BMP-4 receptor
-
-
-
-
Bmx tyrosine kinase
-
Bone marrow kinase BMX
-
-
-
-
bone morphogenetic protein receptor type IA
-
bone morphogenetic protein receptor type IB
-
BPK
-
-
-
-
Breast tumor kinase
breast tumour kinase
-
Bruton tyrosine kinase
-
Bruton's tyrosine kinase
Bruton's tyrosine kinase PH domain
-
Brutons tyrosine kinase
Bruton’s tyrosine kinase
-
-
Btk tyrosine kinase
-
-
c-ABL
c-Abl tyrosine kinase
c-FER
-
-
-
-
C-FES
-
-
-
-
c-Fes protein-tyrosine kinase
-
-
c-Fes tyrosine kinase
-
-
C-SRC
C-SRC kinase
c-Src nonreceptor tyrosine kinase
-
-
c-Src protein tyrosine kinase
-
-
c-Src tyrosine kinase
C-terminal Src kinase
-
-
C-YES
CADTK
-
-
-
-
CAK beta
-
-
-
-
Calcium-dependent tyrosine kinase
-
-
-
-
CARD-containing interleukin-1 beta converting enzyme associated kinase
-
Cell adhesion kinase beta
-
-
-
-
Chk tyrosine kinase
-
-
Chk1
-
-
Csk homologous kinase
-
-
Csk protein-tyrosine kinase
-
-
CSK-homologous kinase
-
-
cytoplasmic protein tyrosine kinase
-
-
cytoplasmic tyrosine-protein kinase BMX
-
D-ash
-
-
-
-
DFer
-
-
-
-
Dsrc28C
-
-
-
-
ectoprotein kinase
-
-
-
-
Epithelial and endothelial tyrosine kinase
-
-
-
-
EPS I polysaccharide export protein epsB
-
-
-
-
FADK1
-
-
FADK2
-
-
FAK2
-
-
FER tyrosine kinase
-
Fes tyrosine kinase
-
-
Fgr kinase
-
focal adhesion kinase 1
-
-
-
-
focal adhesion protein tyrosine
-
-
Frk kinase
-
Fyn kinase
-
-
Fyn tyrosine kinase
-
-
fyn-related kinase
-
gene lck protein kinase
-
-
-
-
gene lck tyrosine kinase
-
-
-
-
Hck kinase
-
Hematopoietic consensus tyrosine-lacking kinase
Hemopoietic cell kinase
-
-
-
-
IL-1R-associated kinase
-
IL-2-inducible T-cell kinase
-
-
-
-
integrin-linked protein kinase 1
-
integrin-linked protein kinase 76
-
interleukin-1 receptor-associated kinase 1
-
interleukin-1 receptor-associated kinase-81
-
JAK protein tyrosine kinase
-
-
-
-
Jak tyrosine kinase
-
-
Jak2 protein
-
JAK2 tyrosine kinase
-
-
Janus family kinase JAK3
-
Janus kinase
Janus kinase 1
-
-
Janus kinase 2
just another kinase
-
-
Kinase EMB
-
-
-
-
Kinase EMT
-
-
-
-
Kinase TLK
-
-
-
-
kinase, protein (phosphorylating tyrosine)
-
-
-
-
kinase, protein p56lck (phosphorylating)
-
-
-
-
L-JAK
-
-
-
-
Lck kinase
-
Lck Tyrosine kinase
-
-
-
-
Leukocyte janus kinase
LIM domain kinase 2
-
LSK
-
-
-
-
lymphocyte-specific protein tyrosine kinase
-
-
Lyn tyrosine kinase
-
megakaryocyte-associated tyrosine-protein kinase
-
MIS type II receptor
-
non-receptor protein tyrosine kinase
-
-
non-receptor protein-tyrosine kinase
-
-
non-receptor PTK
-
-
non-receptor tyrosine kinase
-
-
non-receptor tyrosine kinase brk
-
non-receptor tyrosine-protein kinase TYK2
-
nonreceptor protein tyrosine kinase
-
-
-
-
nonreceptor tyrosine kinase
nonreceptor tyrosine kinase c-Abl
-
nonreceptor tyrosine kinase Fes
-
nonreceptor tyrosine kinase SYK
-
nonreceptor tyrosine kinase Tec
-
NRTK
-
-
NTK38
-
-
-
-
Nuclear tyrosine protein kinase RAK
-
-
-
-
ORF6
-
-
-
-
p135tyk2 tyrosine kinase
-
p150
-
-
-
-
p55-BLK
-
-
-
-
P55-FGR
-
-
-
-
p56-HCK
-
-
-
-
p56-HCK/p59-HCK
-
-
-
-
P56-LCK
-
-
-
-
p56lck kinase
-
-
-
-
p56lck protein kinase
-
-
-
-
p56lck protein tyrosine kinase
-
-
-
-
p56lck tyrosine kinase
-
-
-
-
P57-STK
-
-
-
-
P59-FYN
-
-
-
-
p59-HCK/p60-HCK
-
-
-
-
P60-SRC
-
-
-
-
p60-YRK
-
-
-
-
P61-YES
-
-
-
-
p94-FER
-
-
-
-
phosphotyrosyl-protein kinase
-
-
-
-
PP125FAK
proline-rich tyrosin ekinase 2
-
-
proline-rich tyrosine kinase 2
proline-rich tyrosine kinase-2
-
-
Protein kinase (tyrosine-phosphorylating)
-
-
-
-
protein kinase A
-
-
-
-
Protein kinase BATK
-
-
-
-
Protein kinase HYL
-
-
-
-
Protein kinase Lck
-
-
-
-
Protein kinase NTK
-
-
-
-
Protein kinase p56-LCK
-
-
-
-
Protein kinase p56lck
-
-
-
-
Protein p56c-lck kinase
-
-
-
-
Protein p56lck tyrosine kinase
-
-
-
-
Protein tyrosine kinase
protein tyrosine kinase 2
-
-
protein tyrosine kinase 2beta
-
-
-
-
protein tyrosine kinase 6
-
protein tyrosine kinase 70
-
protein tyrosine kinase focal adhesion kinase
-
-
Protein tyrosine kinase lck
-
-
-
-
Protein tyrosine kinase p56lck
-
-
-
-
Protein tyrosine kinase pp56lck
-
-
-
-
protein-tyrosine kinase
-
-
protein-tyrosine kinase Brk
-
Protein-tyrosine kinase C-TKL
-
-
-
-
Protein-tyrosine kinase CYL
-
-
-
-
Protein-tyrosine kinase Syk
-
-
proto-oncogene serine/threonine-protein kinase mos
-
proto-oncogene tyrosine-protein kinase FER
-
proto-oncogene tyrosine-protein kinase FES/FPS
-
proto-oncogene tyrosine-protein kinase FYN
-
proto-oncogene tyrosine-protein kinase LCK
-
proto-oncogene tyrosine-protein kinase SRC
-
proto-oncogene tyrosine-protein kinase YES
-
PTK-RL-18
-
-
-
-
PTK6/Sik
-
-
PTK70
Pyk-2
-
-
Quek1
-
-
-
-
RAF proto-oncogene serine/threonine-protein kinase
-
Raf-1 protein kinase
-
Rak tyrosine kinase
-
receptor interacting protein 3
-
receptor-associated kinase JAK2
-
receptor-interacting serine/threonine protein kinase 2
Related adhesion focal tyrosine kinase
-
-
-
-
Resting lymphocyte kinase
-
-
-
-
Rlk/Txk
-
-
-
-
S-domain receptor-like protein kinase
-
-
-
-
serine/threonine-protein kinase receptor R2
-
serine/threonine-protein kinase receptor R3
-
SLK
-
-
-
-
Spleen tyrosine kinase
Src family kinase
-
-
Src kinase
Src protein tyrosine kinase
-
-
src protein tyrosine kinase p56Lck
-
-
Src protein-tyrosine kinase
-
-
Src tyrosine kinase
Src-family protein tyrosine kinase
-
-
src-kinase
-
-
-
-
SRC-related intestinal kinase
-
-
-
-
Syk kinase
-
-
Syk-related tyrosine kinase
-
-
-
-
SYN
-
-
-
-
T cell-specific protein-tyrosine kinase
-
-
-
-
T-cell-specific kinase
-
-
-
-
Tec family tyrosine kinase
-
-
Tec kinase
-
-
testis-specific protein kinase 1
-
testis-specific protein kinase 2
-
TGF-beta receptor type I
-
TGF-beta receptor type II
-
TGF-beta RII
-
transforming growth factor beta type II receptor
-
transforming growth factor-beta type I receptor 7
-
Tyrosine kinase
-
-
-
-
tyrosine kinase 2
-
tyrosine kinase Abl
-
-
Tyrosine kinase ARG
-
-
-
-
tyrosine kinase c-Src
-
-
tyrosine kinase cyl
-
tyrosine kinase Fyn
-
Tyrosine kinase lck
-
-
-
-
Tyrosine kinase p56lck
-
-
-
-
tyrosine kinase p60c-src
-
-
tyrosine kinase PTK6
-
tyrosine kinase Src
-
-
tyrosine kinases src
-
tyrosine kinases yes
-
Tyrosine phosphokinase
-
-
-
-
Tyrosine protein kinase
-
-
-
-
Tyrosine protein kinase p56lck
-
-
-
-
tyrosine-protein kinase 6
-
tyrosine-protein kinase ABL2
-
tyrosine-protein kinase BLK
-
Tyrosine-protein kinase brk
-
-
-
-
tyrosine-protein kinase BTK
-
tyrosine-protein kinase CSK
-
Tyrosine-protein kinase CTK
-
-
-
-
tyrosine-protein kinase FRK
-
tyrosine-protein kinase HCK
-
tyrosine-protein kinase ITK/TSK
-
tyrosine-protein kinase JAK1
-
tyrosine-protein kinase JAK2
-
tyrosine-protein kinase JAK3
-
Tyrosine-protein kinase Lyk
-
-
-
-
tyrosine-protein kinase LYN
-
tyrosine-protein kinase SYK
-
tyrosine-protein kinase Tec
-
tyrosine-protein kinase TXK
-
Tyrosine-protein kinase TYRO 10
-
-
-
-
tyrosine-protein kinase ZAP-70
-
Tyrosine-specific protein kinase
-
-
-
-
Tyrosylprotein kinase
-
-
-
-
v-fps Protein-tyrosine kinase
-
-
-
-
WEE1hu
YES related kinase
-
-
-
-
ZAP-70
-
-
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
phospho group transfer
SYSTEMATIC NAME
IUBMB Comments
ATP:[protein]-L-tyrosine O-phosphotransferase (non-specific)
Unlike EC 2.7.10.1, receptor protein-tyrosine kinase, this protein-tyrosine kinase does not have a transmembrane domain. In the human genome, 32 non-specific protein-tyrosine kinases have been identified and these can be divided into ten families [1].
CAS REGISTRY NUMBER
COMMENTARY hide
114051-78-4
p56lck protein kinase
80449-02-1
protein-tyrosine kinase
9026-43-1
this CAS Reg. No. encompasses a great variety of protein kinases including the serine/threonine specific kinases
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a [Tyr-2 peptide]-L-tyrosine
ADP + a [Tyr-2 peptide]-L-tyrosine phosphate
show the reaction diagram
-
-
-
?
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
show the reaction diagram
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion, estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen receptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + a [homeodomain-interacting protein kinase 2]-L-tyrosine
ADP + a [homeodomain-interacting protein kinase 2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [peptide]-L-tyrosine
ADP + a [peptide]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + A-kinase anchor protein 8
?
show the reaction diagram
-
-
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
ATP + arsenate resistance protein ARS2
?
show the reaction diagram
-
-
-
-
?
ATP + ataxin 2 related protein
?
show the reaction diagram
-
-
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + Bcl-2-associated transcription factor 1
?
show the reaction diagram
-
-
-
-
?
ATP + beta 1-integrin cytoplasmic domain peptide
ADP + ?
show the reaction diagram
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + biotin-GGEAIYAAPFKK-amide
ADP + phosphorylated biotin-GGEAIYAAPFKK-amide
show the reaction diagram
-
a peptide with the preferred c-Abl substrate sequence carrying an Nterminal biotin
-
-
?
ATP + c-Src
?
show the reaction diagram
-
-
-
-
?
ATP + calponin 3
?
show the reaction diagram
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
show the reaction diagram
-
-
-
-
?
ATP + cdc2(6-20) peptide
?
show the reaction diagram
-
i.e. KVEKIGEGTYGVVYK, substrate of Src family kinases
-
-
?
ATP + chromosome 20 open reading frame 77
?
show the reaction diagram
-
-
-
-
?
ATP + cleavage and polyadenylation specific factor 5
?
show the reaction diagram
-
-
-
-
?
ATP + cofilin
ADP + phosphorylated cofilin
show the reaction diagram
phosphorylation specifically at Ser-3
-
-
?
ATP + cortactin
?
show the reaction diagram
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
show the reaction diagram
ATP + EEEEY
ADP + EEEE(phospho)Y
show the reaction diagram
-
-
-
-
?
ATP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
ADP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G phosphate
show the reaction diagram
-
Y7 Sox-based substrate, kinetic assay
-
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
show the reaction diagram
ATP + EQEDEPEGDYFEWLE
ADP + EQEDEPEGDpYFEWLE
show the reaction diagram
-
-
-
-
?
ATP + eukaryotic translation initiation factor 3, subunit 4
?
show the reaction diagram
-
-
-
-
?
ATP + ewing sarcoma breakpoint region 1
?
show the reaction diagram
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
show the reaction diagram
-
-
-
-
?
ATP + F peptide
ADP + phospho-L-tyrosinyl-F peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIFGEI-NH2
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
show the reaction diagram
-
-
-
-
?
ATP + FUS interacting protein (serine/arginine rich) 1
?
show the reaction diagram
-
-
-
-
?
ATP + FUS/TLS oncogene
?
show the reaction diagram
-
-
-
-
?
ATP + FUSE binding protein
?
show the reaction diagram
-
-
-
-
?
ATP + FUSE binding protein 2
?
show the reaction diagram
-
-
-
-
?
ATP + GAPEVIYATPGAKKK
ADP + GAPEVI-phosphotyrosinyl-ATPGAKKK
show the reaction diagram
-
consensus substrate
-
-
?
ATP + GGEAIYAAPFKK
ADP + GGEAIYAAPFKK phosphate
show the reaction diagram
-
kinase assay using biotinylated model substrate peptide
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein A3
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein AB
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein D-like
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein K
?
show the reaction diagram
-
-
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
serine/threonine-specific kinase activity
-
-
?
ATP + homeobox prox 1
?
show the reaction diagram
-
-
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
show the reaction diagram
ATP + KVEKIGEGTYGVVYK
ADP + ?
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + lysozyme-L-tyrosine
ADP + lysozyme-L-tyrosine phosphate
show the reaction diagram
-
substrate of Src, low activity with Csk or Chk
-
-
?
ATP + myelin basic protein
ADP + ?
show the reaction diagram
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
show the reaction diagram
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + NEFA-interacting nuclear protein
?
show the reaction diagram
-
-
-
-
?
ATP + NICE-4
?
show the reaction diagram
-
-
-
-
?
ATP + P1 peptide
ADP + phospho-L-tyrosinyl-P1 peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIpYGEI-NH2
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
show the reaction diagram
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
show the reaction diagram
-
-
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
show the reaction diagram
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
show the reaction diagram
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
show the reaction diagram
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu,Tyr)
? + ADP
show the reaction diagram
substrate used in the tyrosine kinase asssay
-
-
?
ATP + poly(Glu-Tyr)
? + ADP
show the reaction diagram
-
substrate used in the activity assay
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
show the reaction diagram
ATP + proteasome activator subunit 3
?
show the reaction diagram
-
-
-
-
?
ATP + protein
?
show the reaction diagram
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
show the reaction diagram
-
Csk inactivates the enzyme substrate
-
-
?
ATP + RasGAP SH3-domain binding protein
?
show the reaction diagram
-
-
-
-
?
ATP + recombinant GST/beta3 integrin cytoplasmic tail peptide
ADP + ?
show the reaction diagram
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
show the reaction diagram
-
-
-
-
?
ATP + RNA binding motif protein 10
?
show the reaction diagram
-
-
-
-
?
ATP + RNA binding motif protein 4B
?
show the reaction diagram
-
-
-
-
?
ATP + S1 peptide
ADP + phospho-L-tyrosinyl-S1 peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIYGEI-NH2
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
show the reaction diagram
-
-
-
-
?
ATP + signal transducer and activator of transcription
ADP + phospho-L-tyrosinyl-signal transducer and activator of transcription
show the reaction diagram
-
-
-
-
?
ATP + similar to zinc finger CCCH-type domain-containing protein 6
?
show the reaction diagram
-
-
-
-
?
ATP + splicing factor proline/glutamine-rich
?
show the reaction diagram
-
-
-
-
?
ATP + splicing factor, arginine/serine-rich9
?
show the reaction diagram
-
-
-
-
?
ATP + Src
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
wild-type Src and catalytically inactive mutant Src K295M, terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site, Glu510 of Src interacts with Arg283 of Csk in Csk-Src recognition, activity with Src fragments, overview
-
-
?
ATP + Src family kinase
?
show the reaction diagram
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
show the reaction diagram
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-L-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
show the reaction diagram
ATP + thyroid hormone receptor associated protein 3
?
show the reaction diagram
-
-
-
-
?
ATP + TRK-fused gene
?
show the reaction diagram
-
-
-
-
?
ATP + Tyr267 of Vav1
ADP + phosphorylated Tyr267 of Vav1
show the reaction diagram
-
-
isoform c-Abl kinase probably regulates the activity of Rho guanine exchange factor Vav1 by direct phosphorylation at Tyr267 in the Dbl homology domain. The C-terminal SH3-SH2-SH3 domain and proline-rich region of Vav1 are required for its interaction with c-Abl kinase
-
?
ATP + zinc finger, CCHC domain containing protein 8
?
show the reaction diagram
-
-
-
-
?
ATP + [Abi1]-L-tyrosine
ADP + [Abi1]-L-tyrosine phosphate
show the reaction diagram
-
c-Abl phosphorylates Y213 of Abi1
-
-
?
ATP + [actin-stabilizing adapter protein HS1]-L-tyrosine
ADP + [actin-stabilizing adapter protein HS1]-L-tyrosine phosphate
show the reaction diagram
-
c-Abl binds to phospho-HS1 via its SH2 domains and is required for full tyrosine phosphorylation of HS1 during T-cell activation
-
-
?
ATP + [androgen receptor]-L-tyrosine
ADP + [androgen receptor]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
show the reaction diagram
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
show the reaction diagram
ATP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine
ADP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CAEEEIYGEFEA derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGKYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTFGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTpYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYFVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVEYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVFK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGKGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
show the reaction diagram
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
show the reaction diagram
ATP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine
ADP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine phosphate
show the reaction diagram
substrate HCN4, tyrosine 531 is phosphorylated
-
-
?
ATP + [kdSrc kinase]-L-tyrosine
ADP + [kdSrc kinase]-L-tyrosine phosphate
show the reaction diagram
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine
ADP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p21Cip1]-L-tyrosine
ADP + [p21Cip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p27Kip1]-L-tyrosine
ADP + [p27Kip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p57Kip2]-L-tyrosine
ADP + [p57Kip2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
show the reaction diagram
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + [Runx1]-L-tyrosine
ADP + [Runx1]-L-tyrosine phosphate
show the reaction diagram
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
show the reaction diagram
ATP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine
ADP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
?
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
show the reaction diagram
-
substrate of ZAP-70
-
-
?
ATP + [tubulin]-L-tyrosine
ADP + [tubulin]-L-tyrosine phosphate
show the reaction diagram
-
highly active with c-Fes, which also catalyzes tubulin polymerization in vitro
-
-
?
ATP + [vimentin]-L-tyrosine
ADP + [vimentin]-L-tyrosine phosphate
show the reaction diagram
-
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
show the reaction diagram
ATP + [[Lys19]Cdc2-(6-20) peptide]-L-tyrosine
?
show the reaction diagram
-
i.e. KVEKIGEGTYGVVKK
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
show the reaction diagram
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
show the reaction diagram
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
show the reaction diagram
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
show the reaction diagram
-
i.e. WASP, phosphorylation by Fak
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
show the reaction diagram
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + a [homeodomain-interacting protein kinase 2]-L-tyrosine
ADP + a [homeodomain-interacting protein kinase 2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is an important substrate for Src signalling in normal cells
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
show the reaction diagram
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
show the reaction diagram
Wee1 negatively regulates cyclin-dependent kinases by phosphorylation on Y15
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
show the reaction diagram
-
the activated Abl tyrosine kinase negaively regulates endocytosis of the epidermal growth factor, e.g. in NR6 cells, overview, Abl allows the ligand-activated EGFR to escape Cbl-dependent down-regulation by inhibiting the accumulation of Cbl at the plasma membrane in response to epidermal growth factor stimulation and disrupting the formation of the EGFR-Cbl complex without affecting Cbl protein stability
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
show the reaction diagram
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
show the reaction diagram
-
p56lck regulates cell motility and nuclear factor kappaB-mediated secretion of urokinase type plasminogen activator through tyrosine phosphorylation of IkappaBalpha following hypoxia/reoxygenation, molecular mechanism, physiological role
-
-
?
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
show the reaction diagram
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
show the reaction diagram
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
show the reaction diagram
-
-
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
show the reaction diagram
Wee1 kinase inhibits mitosis by directly phosphorylating p34cdc2 on Y15
-
?
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
show the reaction diagram
-
Jak2 is involved in the regulation of serine-threonine kinase PAK1, maximal cell motility is required for tyrosyl phosphorylation of PAK1
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
show the reaction diagram
-
i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation by fyn is essential for PIKE-A complex formation and apoptotic cleavage, overview
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
ATP + protein
?
show the reaction diagram
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R
-
-
?
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
show the reaction diagram
-
Csk inactivates the enzyme substrate
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
show the reaction diagram
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
show the reaction diagram
-
-
-
-
?
ATP + Src family kinase
?
show the reaction diagram
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
show the reaction diagram
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
show the reaction diagram
-
physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, TCGAP is involved in Fyn-mediated regulation of axon and dendrite outgrowth
-
-
?
ATP + [androgen receptor]-L-tyrosine
ADP + [androgen receptor]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
show the reaction diagram
-
Src tyrosine kinases are involved in a signaling transduction pathway activating aryl hydrocarbon receptor AhR-mediated signalling by omeprazole or 2,3,7,8-tetrachlorodibenzo-4-dioxin TCDD ligand-binding, AhR phosphorylation at Tyr320, the omeprazole-dependent mechanism probably involves S318 and K316
-
-
?
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
show the reaction diagram
-
proto-oncogenic PTK protein substrate
-
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine
ADP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p21Cip1]-L-tyrosine
ADP + [p21Cip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p27Kip1]-L-tyrosine
ADP + [p27Kip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p57Kip2]-L-tyrosine
ADP + [p57Kip2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
show the reaction diagram
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + [Runx1]-L-tyrosine
ADP + [Runx1]-L-tyrosine phosphate
show the reaction diagram
the enzyme phosphorylates transcription factor Runx1 and regulates Runx1-mediated megakaryocyte maturation
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
show the reaction diagram
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
show the reaction diagram
-
substrate of ZAP-70
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
show the reaction diagram
-
substrate of Lck, Fyn, and c-Abl, leads to ZAP-70 activation, mechanism
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
show the reaction diagram
-
phosphorylation by PYK2 increases the binding of gelsolin to phosphoatidylinositol lipids and actin polymerization at the fibroblastic cell periphery
-
-
?
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
show the reaction diagram
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
show the reaction diagram
-
phosphorylation at Tyr31 and Tyr118 by Fak plays a role in tumor cell motility inhibition
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
show the reaction diagram
-
i.e. WASP, phosphorylation by Fak
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Fe3+
-
when Lyn or Hck kinases, which have been stabilised in the inactive state by phosphorylation of the C-terminal regulatory tyrosine, are incubated with Fe3+ ions, a significant enhancement of kinase activity is observed
additional information
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
inhibitor binds to residues Arg386/Glu282 that isoform ABL1 uses to switch between inactive and active conformations. It potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant chronic myeloid leukemia resistance mutants, including T315I. The compound inhibits isoform BCR-ABL1T315I-expressing cell lines, prolongs survival in mouse models of T315I-mutant chronic myeloid leukemia and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing mutation T315I in vitro and in vivo
bosutinib
dasatinib
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
imatinib
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
nilotinib
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
-
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
-
(2E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide
-
WP1066
(2E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
-
LS104
(2E,4E)-N-benzyl-2-cyano-5-(3,4-dihydroxyphenyl)penta-2,4-dienamide
-
AG490, potent JAK2 inhibitor
1-(4-((5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) amino)piperidin-1-yl)ethan-1-one
100 nM, 70.5% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)ethan-1-one
100 nM, 66.2% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)pentane-1,4-dione
100 nM, 56.4% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)propan-1-one
100 nM, 73.4% inhibition. 28°C, pH not specified in the publication
1-(4-acetylphenyl)-3-(1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)azetidin-3-yl)urea
100 nM, 21.9% inhibition. 28°C, pH not specified in the publication
1-(4-acetylphenyl)-3-(1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)pyrrolidin-3-yl)urea
100 nM, 57.4% inhibition. 28°C, pH not specified in the publication
1-(4-[5-(4-ethoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]piperazin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 24.04%
1-(4-[5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]piperazin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 48.54%
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
-
1-(4-[[5-(4-ethoxybenzoyl)-6-(ethylamino)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 6.81%
1-(4-[[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is %
1-(4-[[6-(dimethylamino)-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 9.8%
1-(4-[[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is %
1-(4-[[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 10.61%
1-(4-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 78.13%
1-azaanthraquinones
-
-
-
1-methyl-emodin
-
inhibition of p56lck and c-Src
1-[(3R)-3-([5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 14.56%
1-[(3R)-3-[[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 10.27%
1-[(3R)-3-[[5-(4-phenoxybenzoyl)-6-(piperidin-1-yl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 15.67%
1-[(3R)-3-[[6-(dimethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 11.42%
1-[(3R)-3-[[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 18.24%
1-[(3R)-3-[[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 6.66%
1-[(3R)-3-[[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 52.88%
1-[(3R)-3-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 100%
1-[4-([5-(4-ethoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 8.69%
1-[4-([5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 1.2%
1-[4-[5-(4-ethoxybenzoyl)-6-(ethylamino)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 6.43%
1-[4-[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 11-87%
1-[4-[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 17.53%
1-[4-[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 8.14%
1-[4-[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 87.67 %
1-[4-[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 93.21%
2,5-dihydroxy-3-(3,4-dihydroxyphenyl)-6-phenyl-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,5-dihydroxy-3-phenyl-6-(3,4,5-trihydroxyphenyl)-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,7,8-trihydroxy-3-phenyl-1,4-dibenzofurandione
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one
-
i.e. JAK inhibitor-I
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
-
2-(4-acetylphenyl)-1-(4-(2-((4-morpholinophenyl)amino)thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)ethan-1-one
100 nM, 44% inhibition. 28°C, pH not specified in the publication
2-chloro-omega-hydroxy-emodin
-
inhibition of p56lck and c-Src
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-one
-
potent pan-JAK inhibitor
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
-
3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
-
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
-
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
-
CP-690,550 JAK3-specific inhibitor
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
-
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
-
4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
-
inhibitor of Src and Abl
4-(2-(4-(2-((4-morpholinophenyl)amino)thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)-2-oxoethyl)benzonitrile
100 nM, 17.6% inhibition. 28°C, pH not specified in the publication
4-(4-(cyclopropylsulfonyl)piperazin-1-yl)-5-methyl-N-(4-morpholinophenyl)pyrimidin-2-amine
100 nM, 76.2% inhibition. 28°C, pH not specified in the publication
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
PP2, AG-1897
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp1, inhibits Src family members like Lyn, no inhibition of Syk
4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide
-
-
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
5-methyl-4-(4-(methylsulfonyl)piperazin-1-yl)-N-(4-morpholinophenyl)pyrimidin-2-amine
100 nM, 1.0% inhibition. 28°C, pH not specified in the publication
8-(1-acetylpiperidin-4-yl)-2-((4-morpholinophenyl)amino)pteridin-7(8H)-one
100 nM, 3.5% inhibition. 28°C, pH not specified in the publication
8-methyl-emodin
-
inhibition of p56lck and c-Src
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
-
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
A-419259
-
-
acacetin
-
inhibition of p56lck
AcpYEEI
ATP-phosphopeptide conjugate
ADP
-
competitive versus ATP, noncompetitive versus S1 peptide
AG-490
-
inhibits JAK2 tyrosine kinase
AG1024
-
-
AG490
alsterpaullone
-
at 0.01 mM: 66% inhibition of CHK, 81% inhibition of LCK, and 10% inhibition of CSK
AMN107
-
a specific BCR-ABL tyrosine kinase inhibitor, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
AP23464
apigenin
-
inhibition of p56lck
AST-487
-
-
ATP-1,13-Trioxa-SA-phospho-Tyr-g-p-azido-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-1,13-Trioxa-Suc-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-1,8-Diam-Suc-1,8-Diam-Suc-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-11-Aund-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-6-Ahex-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-8-Aoct-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-beta-Ala-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-gamma-S
-
AZ960
potent and selective ATP competitive inhibitor of JAK2 enzyme activity
AZD-1480
-
Jak2 inhibitor
AZM 475271
-
-
BAY61-3606
-
-
Bcr protein
-
negative regulator
-
bengamide A
-
c-Src from bengamide A-treated cells retains its N-terminal methionine and suffers a decrease in N-terminal myristoylation, which is accompanied by a shift of its subcellular distribution from the plasma membrane to the cytosol, and decreased tyrosine kinase activities of c-Src both in vitro and in vivo and eventually delayed cell-cycle progression through G2/M, overview, bengamide A reduced tyrosine phosphorylation on a few proteins, and is not a general tyrosine kinase inhibitor
BGB324
i.e. Bemcentinib
-
bisindolylmaleimide I
-
blocks alboaggregin-A activation of Fyn
bosutinib
C-terminal Src kinase
-
i.e. CSK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
catenarin
-
i.e. 4-hydroxy-emodin, inhibition of p56lck and c-Src
caveolin
-
a non-catalytic inhibitor of SFKs, transient inhibition
-
CGP 76030
-
-
CGP 77675
-
-
CGP76030
-
growth-inhibitory in vivo
Chk
-
i.e. Csk-homologous kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, Chk is also a 'non-catalytic inhibitor' binding directly to the SFK forming stable complexes and inhibiting it, mechanism, overview
-
chrysin
-
inhibition of p56lck
CMP6
-
i.e. 2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-1, specific for JAK2, kinase domain binding structure and mechanism
CP-690 550
-
Jak3 and Jak2 inhibitor
CP-690,550
CP690,550
-
targeting Jak3
Csk
-
i.e. C-terminal Src kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, mechanism, overview
-
CSK-homologous kinase
-
i.e. CHK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, a second non-catalytic inhibitory mechanism involves tight binding of CHK to the enzyme's SFKs. The binding alone is sufficient to inhibit SFKs inhibition, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
curcumin
cyclopropyl(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazin-1-yl)methanone
100 nM, 77.0% inhibition. 28°C, pH not specified in the publication
damnacanthal
-
an anthraquinone, strong and selective inhibition of p56lck
dasatinib
datiscetin
-
inhibition of p56lck
emodic acid
-
inhibition of p56lck and c-Src
emodin
emodin derivatives
-
synthetic analogues, inhibition of p56lck and Src, overview
-
endocrocin
-
inhibition of p56lck and c-Src
epihematoxylol
-
F-actin
-
negative regulator
-
Fe3+
-
Lyn or Hck kinases in the unphosphorylated active state are significantly inhibited by Fe3+ ion
fisetin
-
inhibition of p56lck
flavone derivatives
-
inhibition of p56lck, overview
-
Fus1 protein
-
negative regulator
-
galangin
-
inhibition of p56lck
genistein
genkwanin
-
inhibition of p56lck
Gleevec
also known as STI-571 or imatinib
haematoxylene
-
haematoxylone
-
hematoxylin
-
Hg2+
-
at PO2 of about 20 mM
ibrutinib
-
iclusig
-
potent inhibitor of Abl
imatinib
imatinib mesylate
INCB018424
INCB16562
-
selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3
INCB18424
INCB20
-
potently inhibits all members of the JAK family with a 100-1000fold selectivity for JAKs over more than 70 other kinases, potent and specific Pan-JAK inhibitor
-
indirubin-3'-monoxime
-
at 0.01 mM: 62% inhibition of CHK, 89% inhibition of LCK, but no inhibition of CSK
INNO-406
-
previously NS-187, inhibits ABL1
interdomain B
-
connects the enzyme's catalytic kinase domain with its SH2 domain, is responsible for regulatory autoinhibition of ZAP-70 involving Tyr315 and Tyr319, deletion of the interdomain B preserves enzyme function, the regulation mechanism is similar to receptor protein tyrosine kinase EphB2, EC 2.7.10.1, overview
-
ITF2357
-
Jak2 inhibitor
JAK-inhibitor I
40% JAK2 residual activity in the presence of 0.002 mM JAK-inhibitor I and 0.02 mM ATP
-
kaempferide
-
inhibition of p56lck
kaempferol
-
inhibition of p56lck
kaempferol-3-O-arabinoside
-
slight inhibition of p56lck
kaempferol-3-O-rhamnoside
-
slight inhibition of p56lck
kenpaullone
-
at 0.01 mM: 35% inhibition of CHK, 85% inhibition of LCK, and 14% inhibition of CSK
lestaurtinib
LFM-A13
-
significantly impairs CXCL12-induced human B lymphoma cell line, and blocks Akt activation, homing of transferred B cells to peripheral lymph nodes is impaired, LFM-A13 significantly reduces the CXCL12-induced increases in Ca2+, overview
LS104
luteolin
-
inhibition of p56lck
M 475271
-
-
methyl 2,5-dihydroxycinnamate
-
i.e. DHC, inhibition of Syk and Lyn
MK-0457
-
Jak2 inhibitor
Mn2+
-
inhibitory above 1 mM
morin
-
inhibition of p56lck
myricetin
-
inhibition of p56lck
N,N-dimethyl-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 63.4% inhibition. 28°C, pH not specified in the publication
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-methylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-phenoxyphenyl)-4-(thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-[2-[4-(2-acetamidoethoxy)anilino]quinazolin-6-yl]-4-methylphenyl)-3-(trifluoromethyl)benzamide
-
-
N-(4-acetylphenyl)-1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperidine-4-carboxamide
100 nM, 74.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-3-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)azetidine-1-carboxamide
100 nM, 8.1% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-3-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)pyrrolidine-1-carboxamide
100 nM, 69.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)piperidine-1-carboxamide
100 nM, 80.5% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-5-(trifluoromethyl)pyr-imidin-4-yl)piperazine-1-carboxamide
100 nM, 74.6% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-5-nitropyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 68.4% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-7-oxopteridin-8(7H)-yl)piperidine-1-carboxamide
100 nM, 2.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)quinazolin-4-yl)piperazine-1-carboxamide
100 nM, 3.2% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-amino-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 22.8% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-chloro-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 99.4% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-fluoro-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 93.5% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperazine-1-sulfonamide
100 nM, 82.4 % inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
2.9 nM, 81.8% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(6-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 15.6% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-[2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl]piperazine-1-carboxamide
27 nM, 86.7% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperidine-4-carboxamide
100 nM, 72.8% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(2-((4-morpholinophenyl)amino)quinazolin-4-yl)piperazine-1-carboxamide
100 nM, 9.7% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 88.5% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(6-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 8.9% inhibition. 28°C, pH not specified in the publication
N-(4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]phenyl)-3-(trifluoromethyl)benzamide
-
-
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
-
N-tert-butyl-3-([5-methyl-2-[(4-piperazin-1-ylphenyl)amino]pyrimidin-4-yl]amino)benzenesulfonamide
-
TG101209
N-tert-butyl-3-[(5-methyl-2-[[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino]pyrimidin-4-yl)amino]benzenesulfonamide
-
TG101348, JAK2-specific inhibitor
N-[3-([3-[4-(4-methoxyanilino)-1,3,5-triazin-2-yl]pyridin-2-yl]amino)-4-methylphenyl]-3-(trifluoromethyl)benzamide
-
-
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-methyl-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-[2-(cyclopropylamino)quinazolin-6-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide
-
-
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
-
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(5-methyl-1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
-
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
-
N-[4-methyl-3-([3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide
-
-
N-[4-methyl-3-([3-[6-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide
-
-
N-[4-[4-amino-1-(propan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea
-
-
nevadensin
-
inhibition of p56lck
nilotinib
NS-187
-
a specific dual ABL-LYN inhibitor
ON012380
-
inhibits wild-type and mutant Abls, substrate-competitive, ATP-incompetitive
paeciloquinone A
-
inhibition of p56lck and c-Src
Paeciloquinone B
-
inhibition of p56lck and c-Src
paeciloquinone C
-
inhibition of p56lck and c-Src
paeciloquinone D
-
inhibition of p56lck and c-Src
PAG protein
-
negative regulator
-
PD166326
PD173955
-
-
PD180970
-
-
peroxiredoxin 1
-
inhibits ABL1 intracellularly
-
phosphoinositide
-
negative regulator
piceatannol
PIP2
-
inhibits ABL1 intracellularly
PNU156804
-
Jak3 inhibitor
protein tyrosine phosphatases
-
e.g. T-cell protein tyrosine phosphatase, catalytic inhibitor of SFKs dephosphorylating the autoactivation tyrosine residue of SFK which leads to inhibition of SFK
-
purpurin
-
inhibition of p56lck and c-Src
purvalanol
-
at 0.01 mM: 22% inhibition of CHK, 80% inhibition of LCK and CSK
Pyk2-specific siRNA
-
-
-
quercetin
-
inhibition of p56lck
R112
-
-
R406
-
-
RACK1
-
a non-catalytic inhibitor of SFKs, transient inhibition
-
rebastinib
-
potent inhibitor of Abl
resokaempferol
-
inhibition of p56lck
resveratrol
-
inhibition of p56lck
RNAi
knockdown of Btk results in decreased tumor necrosis factor-alpha
-
saracatinib
-
inhibitor of Src and Abl
SB1518
-
Jak2 inhibitor
siRNA
-
SKI-1
-
-
SKI-606
staurosporine
stilbene derivatives
-
inhibition of p56lck, overview
-
SU-6656
-
-
SU6656
syringetin
-
inhibition of p56lck
T47
-
57% inhibition of Syk at 0.1 mM
TG101209
TG101348
tyrophostin A25
-
-
tyrphostin 25
-
p38 MAP kinase inhibitor SB203580 and protein tyrosine kinase inhibitor tyrphostin 25 combined can be used for inhibition of matrix metalloproteinase-9 expression, overview
tyrphostin A23
-
broad-spectrum PTK inhibitor, slight inhibition of Src
tyrphostin A25
-
broad-spectrum PTK inhibitor, slight inhibition of Src
tyrphostin A9
-
-
tyrphostin AG490
-
Jak3 inhibitor
WASP
-
a non-catalytic inhibitor of SFKs, e.g. c-Src, mechanism, transient inhibition
-
WHI-P131
-
Jak3 inhibitor
WHI-P154
-
Jak3 inhibitor
Wortmannin
-
-
WP1066
-
-
XL019
YM193306
-
-
[2-(2-[[3-methoxy-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
[2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
alboaggregin-A
-
Trimeresurus albolabris venom, activates Fyn activity and translocation
-
AMpYSSV
-
CBP-based phosphopeptide, activates
angiotensin subtype 1 receptor
-
AT-1 receptor
-
Ca2+
G-protein coupled receptor PAC1 regulates the tyrosine phosphorylation of isoform PYK2 in NCI-H838 nonsmall cell lung cancer cells. PYK2 phosphorylation is dependent upon Ca2+. The ability of PAC1 to regulate PYK2 is dependent on phospholipase and Src, and partially dependent on proteinkinase C
CD45
-
transmembrane receptor-like protein tyrosine phosphatase activating the SFK by dephosphorylation of the regulatory tyrosine residue
-
CXCL12
-
-
-
cytokine receptors
-
-
-
Epidermal growth factor
epidermal growth factor receptor
-
the Abl nonreceptor tyrosine kinase is activated by ligand-stimulated EGFR
-
epithelial growth factor receptor
-
-
-
EPQYEEIPIYL
-
a src kinase activating peptide, binds to the SH2 domain of the src-kinase and activates it, activation of endogenous src-PTKs does not inhibit Kv1.3 channels in T lymphocytes, overview
insulin-like growth factor 1 receptor
-
-
-
interleukin 5
-
activates Janus kinases JAK1 and JAK2
-
lipopolysaccharide
Lyn kinase
as part of the activation process Lyn phosphorylates Btk in Tyr551, which is subsequently autophosphorylated in Tyr223
-
lysophosphatidic acid
-
activates fyn
macrophage antigen-1
-
i.e. Mac1, a beta2-integrin activates Src PTKs Hck and Lyn, interaction of both requires Mn2+
-
NGF
rapidly stimulates both Ser and Thr phosphorylation in vivo and autophosphorylation activity in vitro of the B-Raf protein
-
pervanadate
activation of isoform Fer by reactive oxygen species causes increased phosphorylation of RhoGDIalpha, regulator of the small GTPase Rac, and pervanadate treatment further augmented this
platelet-derived growth factor
-
PDGF
-
platelet-derived growth factor receptor
-
-
-
prolactin
-
activates Jak2
-
pseudolaric acid B
-
pseudolaric acid B, PAB, activates PTK to induce apoptosis
reactive oxygen species
activation of isoform Fer by reactive oxygen species causes increased phosphorylation of RhoGDIalpha, regulator of the small GTPase Rac, and pervanadate treatment further augmented this
-
sphingosylphosphorylcholine
-
activates fyn
Src
-
activated Src kinase in aggressive breast cancer cell lines can activate c-Abl kinase
-
transforming growth factor beta receptor
-
TGF-beta receptor
-
tyrosine growth factor
-
the enzyme is activated by the tyrosine growth factor and seven transmembrane-spanning receptors
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.014 - 17.64
ATP
0.057
EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
-
-
0.018 - 0.659
poly(Glu4-Tyr)
0.037
S1 peptide
-
BTK
0.0057 - 0.24
[kdSrc kinase]-L-tyrosine
-
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.16 - 55
ATP
0.072 - 2.27
EEEEY
396
EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
-
-
0.01 - 2.07
poly(Glu4-Tyr)
0.11 - 1.88
[kdSrc kinase]-L-tyrosine
-
additional information
additional information
-
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000169 - 0.00076
2-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000272 - 0.000718
2-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000406 - 0.0009
2-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000272 - 0.00126
2-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000083 - 0.000219
2-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000073 - 0.000195
4-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000064 - 0.000217
4-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000104 - 0.0002
4-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000189 - 0.000199
4-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000092 - 0.000165
4-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000167 - 0.000569
4-fluoro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000044 - 0.000354
4-fluoro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000195 - 0.000263
4-fluoro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.00017 - 0.00021
4-fluoro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
0.000013 - 0.0031
imatinib
0.00092 - 0.001137
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
0.00007 - 0.000464
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
0.000247 - 0.000369
N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
0.000225 - 0.000522
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
0.000047 - 0.000217
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
0.000089 - 0.000221
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
0.00001
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
-
0.000004
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
-
0.000032
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
-
0.00021
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
0.000009
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
0.000022
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
-
0.00005
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
-
0.000026
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
-
0.000044
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
-
0.0000005 - 0.000023
4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide
0.001817
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.1414
AcpYEEI
30°C, Src
0.0026 - 0.03
ATP-1,13-Trioxa-SA-phospho-Tyr-g-p-azido-Glu-Glu-Ile-OH
0.0017 - 0.0253
ATP-1,13-Trioxa-Suc-phospho-Tyr-Glu-Glu-Ile-OH
0.0161 - 0.0426
ATP-1,8-Diam-Suc-1,8-Diam-Suc-phospho-Tyr-Glu-Glu-Ile-OH
0.0158 - 0.0472
ATP-11-Aund-phospho-Tyr-Glu-Glu-Ile-OH
0.0115 - 0.0455
ATP-6-Ahex-phospho-Tyr-Glu-Glu-Ile-OH
0.0141 - 0.0355
ATP-8-Aoct-phospho-Tyr-Glu-Glu-Ile-OH
0.0101 - 0.1078
ATP-beta-Ala-phospho-Tyr-Glu-Glu-Ile-OH
0.0571
ATP-gamma-S
30°C, Src
0.00000013 - 0.000001
iclusig
0.00000081 - 0.0033
imatinib
0.000014
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000008
N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000056
N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000023
N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000082
N-(3-methylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.00063
N-(3-phenoxyphenyl)-4-(thiazol-2-yl)pyrimidin-2-amine
-
-
0.00000011 - 0.00000018
N-(3-[2-[4-(2-acetamidoethoxy)anilino]quinazolin-6-yl]-4-methylphenyl)-3-(trifluoromethyl)benzamide
0.00000028 - 0.0000089
N-(4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]phenyl)-3-(trifluoromethyl)benzamide
0.00000076 - 0.0000016
N-[3-([3-[4-(4-methoxyanilino)-1,3,5-triazin-2-yl]pyridin-2-yl]amino)-4-methylphenyl]-3-(trifluoromethyl)benzamide
0.000028
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000023
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.00011
N-[3-methyl-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.00000012 - 0.00000068
N-[3-[2-(cyclopropylamino)quinazolin-6-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide
0.00000039 - 0.000019
N-[4-methyl-3-([3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide
0.0000028 - 0.00053
N-[4-methyl-3-([3-[6-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide
0.00000022 - 0.00000082
N-[4-[4-amino-1-(propan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea
0.00000042 - 0.0000051
rebastinib
0.000033
[2-(2-[[3-methoxy-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
0.00001
[2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
additional information
additional information
-
substrate inhibition kinetics and analysis
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000008 - 0.000004
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
0.0029 - 0.0218
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
0.00107
1-(4-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0018
1-[(3R)-3-[[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00132
1-[4-[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00088
1-[4-[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00000129 - 0.0000323
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.00000046
3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
Homo sapiens
-
0.0000097 - 0.00014
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000055 - 0.00007
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00000055 - 0.000016
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00000098 - 0.000024
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
0.00000092 - 0.000007
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000091 - 0.00083
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000063 - 0.00031
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000015 - 0.000015
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000012 - 0.00039
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000033 - 0.00018
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000012 - 0.000067
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000021 - 0.000017
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00000046 - 0.00000732
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
0.00000089 - 0.0000158
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
0.00000046
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
Homo sapiens
-
0.00000046 - 0.00000163
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
0.00000046 - 0.00000157
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
0.00000023 - 0.0000068
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
0.00000046 - 0.0000005
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
0.00000046 - 0.0000018
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
0.00000023 - 0.00000302
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
0.00000143 - 0.0000195
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
0.00000358 - 0.00000831
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.00000178 - 0.00000593
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
0.000004 - 0.0000173
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
0.00000374 - 0.0000176
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
0.00000277 - 0.00000556
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.0000694 - 0.000126
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.00000658 - 0.0000543
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
0.0102 - 0.0154
AG490
0.000001
AP23464
Homo sapiens
-
0.0000008 - 0.000025
baricitinib
-
0.000037
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.000005 - 0.000297
dasatinib
0.00036
epihematoxylol
Homo sapiens
-
0.0016
haematoxylene
Homo sapiens
-
0.0018
haematoxylone
Homo sapiens
-
0.00044
hematoxylin
Homo sapiens
-
0.00000065
ibrutinib
Homo sapiens
pH and temperature not specified in the publication
0.00000025 - 0.0000101
INCB16562
0.0000003 - 0.0000009
INCB20
-
0.00093 - 0.00252
LS104
0.00016 - 0.0056
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
0.00000236 - 0.000017
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
0.0000167 - 0.000198
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
0.00000046
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(5-methyl-1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000318 - 0.0000733
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
0.000376 - 0.000626
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
0.000025
nilotinib
Homo sapiens
-
ABL1
0.00001
ON012380
Homo sapiens
-
below, inhibition of BCR-ABL
0.000001
SKI-606
Homo sapiens
-
inhibition of BCR-ABL
0.008
staurosporine
Homo sapiens
-
i.e. ST, inhibition of Syk and Lyn, IC50 for Syk is 0.008 mM
additional information
additional information
Homo sapiens
-
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.0173
-
purified recombinant Strep-tagged GST-fusion Chk
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7
-
assay at
7.1
-
assay at
7.6
-
assay at
7.7
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
21
-
assay at room temperature
22
-
assay at room temperature
23
-
immune complex kinase assay
37
tyrosine kinase assay
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
cell line K562
Manually annotated by BRENDA team
-
specific expression of ALK-MYH9
Manually annotated by BRENDA team
-
Frk, Src, Fyn, Yes
Manually annotated by BRENDA team
hematopoietic cancer cells
Manually annotated by BRENDA team
-
Brk, Frk, Src, Fyn, Yes
Manually annotated by BRENDA team
testicular, specifically expressed in
Manually annotated by BRENDA team
metastatic fibrosarcoma cell line
Manually annotated by BRENDA team
metastatic human melanoma cell line
Manually annotated by BRENDA team
-
Srm, Src, Fyn, Yes
Manually annotated by BRENDA team
IM-9 lymphoblast
Manually annotated by BRENDA team
-
Frk, Src, Fyn, Yes
Manually annotated by BRENDA team
altered expression in human lymphocyte tumor cell lines may contribute to their transformed phenotype
Manually annotated by BRENDA team
-
breast epithelial cell line
Manually annotated by BRENDA team
-
breast cancer cell line
Manually annotated by BRENDA team
-
human HCC cell line
Manually annotated by BRENDA team
skeletal muscle
Manually annotated by BRENDA team
-
atrial
Manually annotated by BRENDA team
-
isoform c-Src and Notch-1 co-localize in tissues of pancreatic cancer patients
Manually annotated by BRENDA team
-
Brk, Src, Fyn, Yes
Manually annotated by BRENDA team
activity is significantly lower in prostate cancer tissue after androgen withdrawal and is also low in prostate cancer cell lines
Manually annotated by BRENDA team
predominant expression in
Manually annotated by BRENDA team
weak activity
Manually annotated by BRENDA team
-
Brk, Src, Fyn, Yes
Manually annotated by BRENDA team
T cells and C cells
Manually annotated by BRENDA team
expressed in primary human vascular cells, as well as other non-lymphoid and non-myeloid cell types
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
Fyn is localized at both ends of F-actin bundles
Manually annotated by BRENDA team
additional information
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
the BCR-ABL oncogene is a product of chromosome translocation between chromosome 9 and chromosome 22, that causes leukemia
physiological function
the N-terminal domain of the non-receptor tyrosine kinase ABL confers protein instability and suppresses tumorigenesis
drug target
malfunction
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
ABL1_HUMAN
1130
0
122873
Swiss-Prot
other Location (Reliability: 2)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
117000
-
determined by SDS-PAGE and Western Blot analysis
120000
-
x * 120000, SDS-PAGE
130000
32643
x * 32641.6 calculated, x * 32643, mass spectrometry
50000
56000
determined by SDS-PAGE and Western Blot analysis
60000
determined by SDS-PAGE and Western Blot analysis
60801
x * 60801, calculation from nucleotide sequence
70000
77000
-
x * 77000, recombinant GST-fusion Chk, SDS-PAGE, x * 50000, proteolytic fragment of recombinant GST-fusion Chk, SDS-PAGE
93000
x * 93000, calculation from nucleotide sequence
93390
x * 93390, calculation from nucleotide sequence
95000
additional information
determination of secondary structure of the SH2 domain for Hck
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
homodimer
the Btk PH domain forms a homodimer
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
acetylation
-
normal activation of the ABL1 proteins requires acetylation
acylation
-
normal activation of the ABL1 proteins requires myristoylation
phosphoprotein
side-chain modification
additional information
-
isoform 1b has a myristoylation site
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
crystal structure of the Abl regulatory region containing the SH3 and SH2 domains
crystal structure of the Abl-SH3 domain in complex with the high-affinity peptide ligand p41 at 1.6 A resolution
in complex with inhibitor 4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
inhibitor bosutinib bound to the kinase domain of isoform Abl, to 2.4 A resolution. Two distinct chemical compounds are currently being sold under the name bosutinib, spectroscopic and structural characterizations of both Structure reveals that similar inhibitors that lack a nitrile moiety could be effective against the common T315I mutant
1.94 A resolution crystal structure of the Bruton's tyrosine kinase Y551E mutant kinase domain bound to Dasatinib and a 1.6 A resolution crystal structure of the unphosphorylated human wild-type kinase domain bound to 4-amino-5-(4-phenoxyphenyl)-7H-pyrrolospyrimidin-7-yl-cyclopentane
crystal structure determined at 2.6/2.9 A resolution
crystal structure of the conserved core of HIV-1 Nef in complex with the SH3 domain of a mutant Fyn, tyrosine kinase
crystal structure of the SH3 domain
crystal structure of the SH3 domain of Csk (c-Src specific tyrosine kinase) has been refined at a resolution of 2.5 A, with an R-factor of 22.4%
crystal structure of the tandem SH2 domain of Syk complexed with a dually phosphorylated ITAM peptide. The structure is solved by multiple isomorphous replacement at 3.0 A resolution
crystal structure of the unbound SH3 domain from hemopoietic cell kinase Hck
high-resolution crystal structures of tyrosine kinase SH3 domain complexed with proline-rich peptides
in complex with gleevec
purified recombinant detagged JAK2 kinase domain bound to inhibitor CMP6, hanging drop vapour diffusion method, 20°C, mixing of equal volumes of protein solution, containing 10 mg/ml protein in 20 mM Tris, pH 8.5, 250 mM NaCl, and 1 mM DTT, and reservoir solution, containing 28% PEG 4000, 0.2 M ammonium acetate, and 0.1 M citrate, pH 6.0, 1-3 days, X-ray diffraction structure determination and analysis at 2.0 A
-
purified recombinant His- and FLAG-tagged catalytic domain of Fes, hanging drop vapour diffusion method, 0.002 ml of 10 mg/ml protein solution, phosphate buffered saline, pH 7.4, is mixed with 0.002 ml reservoir solution and equilibrated against 0.4 ml reservoir solution containing 1.6 M magnesium sulfate and 0.1 M MES pH 6.5, 27°C, X-ray diffraction structure determination and analysis at 3.9 A resolution
purified recombinant His-tagged residues 1-531 of splicing variant c-Abl 1b D382N mutant, hanging drop vapor diffusion method, 0.6 ml protein solution mixed with 0.6 ml reservoir solution, in 20% PEG 10000 and 0.1 M HEPES buffer, pH 7.5, at 20ºC, X-ray diffraction structure determination and analysis at 2.27 A resolution, small-angle X-ray scattering data collection and analysis
-
solution structure
solution structure of the C-terminal SH2 domain of the human tyrosine kinase Syk complexed with a phosphotyrosine pentapeptide
solution structure of the human Hck SH3 domain
solution structure of the human pp60c-src SH2 domain complexed with a phosphorylated tyrosine pentapeptide
structure of a large fragment of the c-Src tyrosine kinase, comprising the regulatory and kinase domains and the carboxy-terminal tall, has been determined at 1.7 A resolution in a closed, inactive state
the crystal structure of a Btk fragment consisting of the PH domain and the Btk motif in complex with dibutylyl-phosphatidylinositol-3,4,5-triphosphate is determined
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A356N
the mutation increases enzyme activity
A433T
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
D276G
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E255K
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E355A
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E355G
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E453K
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E459G
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E459K
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E459Q
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F311I
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F317L
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F359C
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F359V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F486S
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
G250E
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
H396P
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
H396R
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
K247L
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
L248V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
L298V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
L364I
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
M244V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
M351T
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
Q252H
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
T315I
T495R
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
V299L
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
Y253F
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
Y253H
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
C616Y
-
the JAK2 mutation is associated with polycythemia vera
C618R
-
the JAK2 mutation is associated with polycythemia vera
D276A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
D332A
-
site-directed mutagenesis of Csk in the DFG motif in front of the activation loop leads to complete loss of kinase activity
D344A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly increased activity with kdSrc and slightly reduced activity with poly(Glu4-Tyr) as substrates compared to the wild-type enzyme
D382N
-
site-directed mutagenesis, catalytically inactive mutant
D518A
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D518E
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D518G
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D518N
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D620E
-
the JAK2 mutation is associated with myeloproliferative syndrome and polycythemia vera
D639Y
missense mutation in the SH1 domain, cG2078->T
dN541-R544
deletion in the SH1 domain, cG1513-G1794
dW281-G325
deletion in the SH2 domain, cG1003-G1137
E225K
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in vivo and in cell culture in vitro
E225V
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro
E255K
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
E300A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
E324A
-
site-directed mutagenesis of Csk, the mutant enzyme shows unaltered interaction with the Src substrate, and slightly reduced activity with the polyEY substrate
E338A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows 40-60% remaining activity compared to the wild-type enzyme
E510A
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
E510R
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
E605G
missense mutation in the SH1 domain, cA1977->G
E627E
-
the JAK2 mutation is associated with myeloproliferative disorder
E864K
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
F183A
-
site-directed mutagenesis, about 70% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
F183L
-
site-directed mutagenesis, about 40% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
F183W
-
site-directed mutagenesis, about 50% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
F382A
-
site-directed mutagenesis, reduced activity with substrate poly(Glu4-Tyr), and highly redcuced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
F540S
mutant, shows absence of Btk phosphorylation on Tyr223
FSdG299X321
deletion in the SH2 domain, cG1058-G1137
FSdN450X457
deletion in the SH1 domain, cG1513-G1729
FSiF583X597
insertion in the SH1 domain, 518 bp insertion between exon 17 and exon 18
FSiG299X312
insertion in the SH2 domain, 579 bp insertion between exon 10 and exon 11
G2A/C3A
mutant lacking the sites for lipid modification
G2A/C3A/K275A
mutant lacking the sites for lipid modification, mutation in the ATP-binding site, kinase-dead
G346A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows decreased activity compared to the wild-type enzyme
G831R
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
G935R
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I. Mutant retains kinase activity exceeding 130 microM JAK inhibitor-I
H384A
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Q
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Q/Y416F
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Y
-
site-directed mutagenesis, the mutant shows reduced activity and no autophosphorylation compared to the wild-type Src
H384Y/Y416F
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Y/Y527F
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H396P
IFiM450+27
insertion in the SH2 domain, 81 bp insertion between exon 14 and exon 15
K222R
-
site-directed mutagenesis, about 80% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
K267M
-
a Hck mutant, the inability of HckK267M to undergo autophosphorylation promotes its phosphorylation at YT by CSK to a higher extent than that of wild type Hck
K274M
-
Lyn mutant, Lyn K274M does not form a stable protein complex with CHK, whereas its unphosphorylated counterpart does
K290M
-
a kinase-inactive Abl mutant
K295M
K298M
-
site-directed mutagenesis, a dominant-negative enzyme mutant
K299M
-
inactive mutant, interacts with TCGAP, coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
K337A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
K361G/K362A
-
the mutant shows reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate poly(Glu4-Tyr)
K374N
mutant, residual kinase activity is present
K430E
mutant, shows absence of Btk phosphorylation on Tyr223
K457A
-
site-directed mutagenesis, mutation leads to increase in phosphorylation sites on the substrate FGFR3
K539L
-
the JAK2 mutation is associated with polycythemia vera
K590E
-
site-directed mutagenesis, inactive mutant enzyme
K607N
-
the JAK2 mutation is associated with acute myelogenous leukemia
K882E
-
kinase-inactive JAK2 mutant
L111P
missense mutation in the PH domain, cT497->C
L111P/R288W/R544S/R562W/S578P/E605G/D639Y/R641H
mutations are due to deletions and insertions of exons and introns, respectively, which suggest splicing defects, leading to development of the X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency, in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
L145P
L145P/L334P
-
site-directed mutagenesis, mutation in the first and second coiled-coil motifs, mutations lead to growth arrest of yeast cells
L145P/R483L
-
mutant enzyme shows low c-Fes colocalization with microtubules
L223A
-
site-directed mutagenesis, about 40% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
L223F
-
site-directed mutagenesis, only slightly reduced Csk tyrosine kinase activity compared to the wild-type enzyme
L296A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate, and reduced activity with the polyEY substrate
L334P
-
site-directed mutagenesis, mutation in the second coiled-coil motif, mutation leads to growth arrest of yeast cells
L611S
-
the JAK2 mutation is associated with acute lymphocytic leukemia
M351I
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
M929I
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
N326A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate, and reduced activity with the polyEY substrate
N391D
-
site-directed mutagenesis, the mutant shows highly reduced enzyme activity and can be well expressed and purified using the Escherichia coli expression system
N909K
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
P1057S
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
P131L
-
a SH3-domain mutant with increased activity compared to wild-type Abl
P134L
-
an SH3-defective mutant, no interaction with TCGAP, coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
Pyk2K457A
-
Pyk2MT, dominant negative Pyk2 mutant, inactive
Q252H
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
Q343A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
R1127K
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
R171K
-
SH2 domain variant containing a mutation
R176K
-
an SH2-defective mutant, interacts with TCGAP, coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
R279A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate
R281A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate
R281A/R283A
-
site-directed mutagenesis, about 90% reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
R283A
R283E
-
site-directed mutagenesis of Csk, the mutant enzyme shows highly reduced interaction with the Src substrate
R283K
-
site-directed mutagenesis of Csk, the mutant enzyme shows highly reduced interaction with the Src substrate
R288W
R28C
mutant
R313A
-
site-directed mutagenesis, activity similar to the wild-type enzyme
R388A/A390R
-
site-directed mutagenesis, mutations in the catalytic loop, the mutant shows slightly reduced enzyme activity and cannot be well expressed and purified using the Escherichia coli expression system
R389A
-
the mutant shows reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate [kdSrc kinase]-L-tyrosine
R483L
-
mutation reverses the c-Fes colocalization with microtubules
R544G
mutant, residual kinase activity is present
R544S
R562W
missense mutation in the SH1 domain, cC1847->T
R641H
missense mutation in the SH1 domain, cG2085->A
R975G
-
mutation is sufficient to support growth and downstream signaling at high oncentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
S273A
-
site-directed mutagenesis, reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S280A
S280A/R281A/R283A/F381A
-
site-directed mutagenesis, about 90% reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S284A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S340A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
S341A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
S381A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S578P
missense mutation in the SH1 domain, cT1895->C
SW445P
mutation causes constitutive activation
T315I
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro
T336A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows increased activity compared to the wild-type enzyme
T342A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows decreased activity compared to the wild-type enzyme
T345A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows decreased activity compared to the wild-type enzyme
T478S
-
the JAK1 mutation is associated with acute myelogenous leukemia
V617F
V617F/C618R
the mutation is associated with polycythemia vera
V623A
-
the JAK1 mutation is associated with acute myelogenous leukemia
V881A
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
W188A
-
the mutant shows increased binding to phosphorylation sites of substrates but reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate poly(Glu4-Tyr)
W188F
-
the mutant shows increased binding to phosphorylation sites of substrates but reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate poly(Glu4-Tyr)
Y223A
-
site-directed mutagenesis of the SH3 domain tyrosine of Btk, the mutant is not phosphorylated
Y253F
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
Y253H
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro
Y315A
-
site-directed mutagenesis, activity is similar to the wild-type ZAP-70
Y315F
-
site-directed mutagenesis, inactive ZAP-70 mutant
Y319A
-
site-directed mutagenesis, activity is similar to the wild-type ZAP-70
Y319F
-
site-directed mutagenesis, inactive ZAP-70 mutant
Y394F
-
Lck F394 mutant cells show reduced tyrosine phosphorylation of the enzyme, expression of recombinant wild-type Lck in the mutant cells increases the autophosphorylation activity 3fold
Y402F
-
site-directed mutagenesis, mutation leads to increase in phosphorylation sites on the substrate FGFR3
Y505F
-
constitutively active Lck mutant, effect on recombinant Kv1.3 current amplitude and O2 sensitivity, overexpressing LckY505F decreased Kv1.3 current from 2.5±0.3 nA to 2.2±0.2 nA, overview
Y511A
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
Y511F
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced slightly interaction with the Csk and reduced inactivation by Csk
Y511I
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
Y511L
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
Y511W
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced slightly interaction with the Csk and reduced inactivation by Csk
Y530F
-
site-directed mutagenesis, a constitutively active mutant
Y531F
-
coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
Y551E
in complex with inhibitor dasatinib, crystal structure
Y551F
-
site-directed mutagenesis, the mutant enzyme cannot be activated by autophosphorylation at Y551, and shows about 10fold reduced activation and activity compared to the wild-type enzyme
Y918H
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
additional information
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-80°C, 20 mM MES buffer, pH 6.0, 200 mM NaCl, 10 mM betaMcEtOH, 10% glycerol, 1 mM benzamidine, 0.2 mM PMSF
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
affinity purified on nickel-nitriloacetic acid agarose and by ion-exchange chromatography using a Mono S column, through chitin affinitive binding and by SP Sepharose cation exchange
-
directed evolution of a highly specific FN3 monobody to the SH3 domain of human Lyn tyrosine kinase. The 2H7 monobody is able to pull down endogenous Lyn from a lysate of Burkitt's lymphoma cells, thereby demonstrating its utility as an affinity reagent for detecting Lyn in a complex biological mixture
HisTrap column chromatography
-
nuclei of THP-1 cells are purified
partial purification of recombinant Csk and FLAG-tagged CHK by specific immunoprecipitation
-
protein extracts from cells, transfected with plasmids containing the HCN4 gene, are prepared
purified on a Ni-NTA column
recombinant GST-fusion JAK2 kinase domain from Sf9 insect cells, glutathione affinity chromatography, afterwards the JAK2 protein is treated with inhibitor CMP6 and the GST-tag is cleaved off by thrombin, followed by gel filtration
-
recombinant GST-fusion-SH3 domains of Tec tyrosine kinase family members from Escherichia coli strain XL-1 Blue, recombinant His-tagged Btk SH3 domain from Sf9 cells, affinity chromatography
-
recombinant His- and FLAG-tagged catalytic domain of Fes from Escherichia coli strain M15 by nickel affinity chromatography and diaflitration
recombinant His-tagged Src kinase from Sf9 insect cells by nickel affinity chromatography
-
recombinant inactive Src mutants from Escherichia coli strain BL21(DE3) by affinity chromatography, Src mutants with kinase activity above a certain threshold cannot be purified from a bacterial expression system, while a variety of mutants with a kinase activity below this threshold can be expressed and purified, overview
-
recombinant Lyn mutant K274M from Spodoptera frugiperda Sf9 cells by anion exchange and hydroxyapatite chromatography
-
recombinant Strep-tagged GST-fusion Chk from Escherichia coli strain DH5alpha 6fold by glutathione and streptavidin affinity chromatography
-
recombinant wild-type and mutant GST-fusion Csk proteins by glutathione affinity chromatography
-
recombinant wild-type and mutant His-tagged Csk from Escherichia coli strain BL21(DE3) by nickel affinity chromatography
-
using a HiTrap SP, a Mono S, and a HiLoad Superdex75 column
using a Ni-NTA Superflow and a Source 15Q column
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in Sf9 insect cells
expression in Escherichia coli
expression in Sf9 cell
expression of SH1, SH2, SH3 domains of isoform ABL, containing residues 65–534
primary structure of normal abl protein is determined by sequencing the coding region of its cDNA
analysis of c-fes cDNA
blk gene is mapped to chromosome 8 at p22-23
Btk, DNA and amino acid sequence determination of wild-type and mutant enzymes
c-yes cDNA clones are obtained from poly(A)+ RNA of human embryo fibroblasts
cDNAs encoding two forms of the LYN protein tyrosine kinase, expressed in rat mast cells and human myeloid cells
cloning of the cDNA for the deleted syk kinase homologous to ZAP-70 from basophilic leukemia cell line KU812, two different sized cDNA clones of syk, Syk11 and Syk41. Reverse transcribed polymerase chain reaction targeting this region shows that both forms of the polyA RNA are expressed in Jurkat cells, human peripheral leukocytes and also KU812 cells, the inserted form is dominant
co-expression of EGFR and Abl in COS-7 cell surface, expression in HEK-293 cells
-
complete nucleotide sequence of a human DNA fragment of approximately 13 kbp, which contains the entire v-fes/fps cellular homolog
constitutive expression of Brk in a large proportion of cutaneous T-cell lymphomas and other transformed T- and B-cell populations, e.g. Jurkat or JB6 cells. The kinase is expressed in the nuclear localization and activated state, subcellular localization study, overview
-
COS cells transfected with a Bmx expression vector and NIH3T3 cells expressing a Bmx retrovirus contain a tyrosyl phosphorylated Bmx polypeptide
delivery of active Lck into L929 cells and overexpression of GFP-tagged Y505FLck do not decrease recombinant Kv1.3 currents, on the contrary, activation of endogenous src kinases increase wild-type Kv1.3 currents in T lymphocytes, overview
-
expressed in Ba/F3 cells
-
expressed in Escherichia coli BL21-Codon-Plus(DE3) cells
-
expression in COS cells
expression in Escherichia coli
expression in U2O2 cells and in Saos2 cells, quantitative expression analysis
-
expression of activated allele of Fes tyrosine kinase, Fesact, encoded by c-fps/es proto-oncogene, in factor-dependent 32D cells preventing their apoptotic death after interleukin-3 removal followd by granulocytic differentiation, factor dependency remains for proliferation, overview
-
expression of active Src in Escherichia coli strain BL21(DE3) is difficult and ineffective due to toxicity caused by Src kinase activity, effective expression of inactive mutants, e.g. of K295M, is possible, overview
-
expression of Chk as soluble dual affinity tag fusion protein, with a GST-tag at the N-terminus and a Strep-tag at the C-terminus, in Escherichia coli strain DH5alpha
-
expression of GST-tagged active full-length fyn and GST-tagged fyn fragments in HEK-293 cells
-
expression of Hck mutant K267M and Lyn mutant K274M in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system
-
expression of His-tagged residues 1-531 of splicing variant c-Abl 1b D382N mutant in Escherichia coli strain BL21(DE3)
-
expression of His-tagged Src kinase in Spodoptera frugiperda Sf9 cells via baculovirus infection system
-
expression of JAK2 kinase domain, comprisine residues 835-1132, as GST-fusion protein in Spodoptera frugiperda Sf9 cells using baculovirus transfection system
-
expression of SH1, SH2, SH3 domains of isoform ABL, containing residues 65–534
expression of SH3 domains of Tec tyrosine kinase family members in Escherichia coli strain XL-1 Blue as GST-fusion proteins, expression of His-tagged SH3 domain from Btk in Spodoptera frugiperda Sf9 cells using a baculovirus expression system, overview
-
expression of untagged or GFP-fusion wild-type and L145P mutant c-Fes tyrosine kinase in COS-7 cells, coexpression with a Src family kinase or activation via coiled-coil mutation L145P lead to c-Fes colocalization with microtubules in the cytoplasm of COS-7 cells
-
expression of VSV-tagged wild-type Syk and catalytically inactive mutant Syk K- in MCF-10A cells
-
expression of wild-type and mutant Csk in Escherichia coli strain DH5 alpha
-
expression of wild-type and mutant Csk in Escherichia coli strain DH5alpha
-
expression of wild-type and mutant GST-fusion Csk proteins
-
expression of wild-type and mutant His-tagged Csk in Escherichia coli strain BL21(DE3)
-
expression of wild-type and mutant human brain-type Fyns in a two-hybrid system in yeast cells with human or mouse TCGAP, wild-type and mutant, overview, expression of wild-type and mutant enzymes in HEK-293T cells and in PC12 cells
-
expression of wild-type and mutant JAK2
-
expression of wild-type Fyn and mutant enzymes in murine NIH3T3 fibroblasts
-
expression of wild-type Fyn and SH3domain-lacking enzyme in TsA-201 cells using the pCMV5 vector
-
expression of wild-type Lck in Y394F Lck mutant cells
-
feline sarcoma oncogene, c-fps/fes, located at chromosome 15q25-qter, expression of a 281 amino acid sequence fragment as His-Fes-CR-FLAG in Escherichia coli strain M15pREP4
for transfection of DT40 lymphoma cells
for transfection of HEK-293T cells
-
full-length Syk is cloned into pFastBac HTb with an N-terminal 6-histidine tag and rTEV protease cleavage site, Syk protein is expressed in SF9 insect cells
-
Fyn subcloning in Escherichia coli strain DH5alpha, transient functional expression of lymphocyte-specific kinase Fyn in Saccharomyces cerevisiae FY250 leading to tyrosine phosphorylation of co-expressed kinase substrate fused to DNA via LexA, two-hybrid and tribrid system with Grb2-SH2 domain coexpression, overview
-
gene ALK is fused to several other genes, NPM, TPM3, TPM4, TFG, ATIC, CLTC, MSN, ALO17, and the non-muscle myosin heavy chain gene MYH9, resulting in expression of chimeric ALK transcripts translated into fusion proteins with tyrosine kinase activity and oncogenic properties, DNA sequence determination and analysis of ALK-MYH9 fusion gene
-
gene syn identified in the human genome on chromosome 6 and characterized by molecular cloning
genetic analysis of mutations causing myeloid malignancies
-
His-tagged, partially capped, active, nonmyristoylated c-Abl, E46 through C-terminus, isoform 1b numbering, is produced, GST fusions of c-Abl SH3 and SH2 domains are used, the dual domain SH3-SH2 is expressed from plasmid pTXB1
-
HYL gene is assigned to chromosome 19
into the pAlterMAX vector
-
into the pcDNA3.1 TOPO vector
-
into the pcDNA4/TO vector, Lyn118(G2A/C3A)-GFP and Lyn118-GFP are constructed by fusion with GFP obtained from pEGFP-C1
into the pCR2.1 vector for sequencing
into the vector pCDNA3 for transfection of PLC cells
-
is located at chromosome position 1q24-25
isolation and characterisation a cDNA
isolation and sequence analysis of the gene
isolation and sequencing of a full length tyk2 cDNA clone
isolation of a cDNA clone encoding ZAP-70
isolation of a full-length cDNA encoding the human homologue of Syk
isolation of cDNA encoding tyrosine kinase cyl
isolation of cDNA, expression in COS cells
localized to chromosome 5q31-32
lyn gene is located on human chromosome 8 q13-qter
mapping to chromosome 19p13.2
MATK gene is located on chromosome 19
overexpression in Schizosaccharomyces pombe generates very elongated cells as a result of inhibition of the G2-M transition in the cell cycle
overexpression of Csk in HeLa cells, overexpression of FLAG-tagged CHK in COS-1 cells
-
overexpression of Myc-tagged wild-type non-receptor tyrosine kinase Pyk2 and mutant enzyme forms in 293T cells, wild-type enzyme expression leads to increased activation of Stat5B, cotransfection with wild-type FGFR1-4, FGFR3 mutant K650E, a myristoylated FGFR, and truncated FGFR3 in 293T cells
-
overexpression of Syk kinase in MDA-MB-231 cells suppresses cell motility and inhibits the activation of phosphatidylinositol 3'-kinase, antisense expression of Syk kinase in MCF-7 cells or expression of wild-type Syk kinase in MDA-MB-231 cells increases cell motility and activity of phosphatidylinositol 3'-kinase
-
proto-oncogene c-fes, overexpression of wild-type and C-terminally FLAG-tagged mutant enzymes in Saccharomyces cerevisiae strain YPH 499
-
recombinant, replication-deficient adenoviral constructs encoding wild-type human Bmx and HA-tagged Bmx are prepared
SYK locus is mapped to chromosome 9 at band q22
tec gene is mapped to chromosome 4p12
the Btk PH domain is expressed in Spodoptera frugiperda Sf9 insect cells using the baculovirus expression system
the gene is located in chromosome Xp22.2
the kinase domain of tyrosine kinase c-Src is cloned and expressed using the Bac-to-Bac baculovirus expression system
the kinase-inactive Pyk2 mutant is cloned using an AAV vector
-
the mutant V617F is expressed in Ba/F3 cells
the V617F mutant is expressed in Ba/F3 cells
transient co-expression of Btk and Toll-like receptors TLR-8 and TLR-9 in HEK-293 cells, interaction study, overview
-
transient overexpression of the GFP-tagged wild-type Chk and the N-terminal domain, as well as of the inactivated enzyme mutant, in HeLa cells and COS-1 cells, overexpression of the enzyme leads to increased tyrosine phosphorylation of protein especially from the nuclear matrix, expression and subcellular localization analysis, overview
-
TXK is mapped to chromosome position 4p12
ZAP-70 DNA sequence determination and analysis, stable expression of Syk or ZAP-70 in enzyme-deficient Jurkat-cell-derived P116 cells, transient expression in COS or T293 cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
c-Src and Fyn show a modest increase in expression as a function of stem cell differentiation
-
Lck expression levels drop dramatically as a function of embryoid body differentiation
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
the fluorescence properties of bosutinib and related compounds allow inhibitor binding to be measured quantitatively, and the infrared absorption of the nitrile group reveals a different electrostatic environment in the conserved ATP-binding sites of Abl and Src kinases
drug development
the enzyme is a target for development and evaluation of tyrosine kinase inhibitors
medicine
isoform c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor, unable to be phosphorylated by c-Abl, leads to reduced breast cancer cell growth and invasion
analysis
-
peptide photoaffinity probe GAPEVIYA-4-azidophenylalanyl-PGAKKKGK(biotin) based on consensus substrate GAPEVIYATPGAKKK. Incubation of purified recombinant isoform Abl results in covalent incorporation of biotin. The label crosslinks to Abl specifically through binding to the active site cleft into the kinase. Abl activity is enhanced by phosphorylation at multiple sites, the extent of labeling increases with increasing catalytic activity
drug development
medicine
pharmacology
synthesis
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Boeckmann, B.; Bairoch, A.; Apweiler, R.; Blatter, M.C.; Estreicher, A.; Gasteiger, E.; Martin M.J.; Michoud, K.; O'Donovan, C.; Phan, I.; Pilbout, S.; Schneider, M.
The SWISS-PROT protein knowledgebase and its supplement TrEMBL
Nucleic Acids Res.
31
365-370
2003
Danio rerio (O12990), Danio rerio (O93596), Mus musculus (P00520), Mus musculus (Q9R117), Drosophila melanogaster (P00528), Drosophila melanogaster (P18106), Drosophila melanogaster (Q24145), Drosophila melanogaster (Q9V9J3), Homo sapiens (P06239), Homo sapiens (Q06187), Macaca fascicularis (Q95M30), Rattus norvegicus (Q9WUD9)
Manually annotated by BRENDA team
Dalal, I.; Arpaia, E.; Dadi, H.; Kulkarni, S.; Squire, J.; Roifman, C.M.
Cloning and characterization of the human homolog of mouse Jak2
Blood
91
844-851
1998
Homo sapiens (O60674), Homo sapiens
Manually annotated by BRENDA team
Peeters, P.; Raynaud, S.D.; Cools, J.; Wlodarska, I.; Grosgeorge, J.; Philip, P.; Monpoux, F.; Van Rompaey, L.; Baens, M.; Van den Berghe, H.; Marynen, P.
Fusion of TEL, the ETS-variant gene 6 (ETV6), to the receptor-associated kinase JAK2 as a result of t(9;12) in a lymphoid and t(9;15;12) in a myeloid leukemia
Blood
90
2535-2540
1997
Homo sapiens (O60674), Homo sapiens
Manually annotated by BRENDA team
Saltzman, A.; Stone, M.; Franks, C.; Searfoss, G.; Munro, R.; Jaye, M.; Ivashchenko, Y.
Cloning and characterization of human Jak-2 kinase: high mRNA expression in immune cells and muscle tissue
Biochem. Biophys. Res. Commun.
246
627-633
1998
Homo sapiens (O60674), Homo sapiens
Manually annotated by BRENDA team
Chissoe, S.L.; Bodenteich, A.; Wang, Y.F.; Wang, Y.P.; Burian, D.; Clifton, S.W.; Crabtree, J.; Freeman, A.; Iyer, K.; Jian, L.; et al.
Sequence and analysis of the human ABL gene, the BCR gene, and regions involved in the Philadelphia chromosomal translocation
Genomics
27
67-82
1995
Homo sapiens (P00519), Mus musculus (P00520)
Manually annotated by BRENDA team
Fainstein, E.; Einat, M.; Gokkel, E.; Marcelle, C.; Croce, C.M.; Gale, R.P.; Canaani, E.
Nucleotide sequence analysis of human abl and bcr-abl cDNAs
Oncogene
4
1477-1481
1989
Homo sapiens (P00519), Homo sapiens
Manually annotated by BRENDA team
Fainstein, E.; Marcelle, C.; Rosner, A.; Canaani, E.; Gale, R.P.; Dreazen, O.; Smith, S.D.; Croce, C.M.
A new fused transcript in Philadelphia chromosome positive acute lymphocytic leukaemia
Nature
330
386-388
1987
Homo sapiens (P00519), Homo sapiens
Manually annotated by BRENDA team
Gosser, Y.Q.; Zheng, J.; Overduin, M.; Mayer, B.J.; Cowburn, D.
The solution structure of Abl SH3, and its relationship to SH2 in the SH(32) construct
Structure
3
1075-1086
1995
Homo sapiens (P00519)
Manually annotated by BRENDA team
Groffen, J.; Heisterkamp, N.; Reynolds, F.H., Jr.; Stephenson, J.R.
Homology between phosphotyrosine acceptor site of human c-abl and viral oncogene products
Nature
304
167-169
1983
Homo sapiens (P00519), Homo sapiens, Abelson murine leukemia virus (P00521)
Manually annotated by BRENDA team
Inokuchi, K.; Futaki, M.; Dan, K.; Nomura, T.
Sequence analysis of the mutation at codon 834 and the sequence variation of codon 837 of c-abl gene
Leukemia
8
343-344
1994
Homo sapiens (P00519)
Manually annotated by BRENDA team
Nam, H.J.; Haser, W.G.; Roberts, T.M.; Frederick, C.A.
Intramolecular interactions of the regulatory domains of the Bcr-Abl kinase reveal a novel control mechanism
Structure
4
1105-1114
1996
Homo sapiens (P00519), Homo sapiens
Manually annotated by BRENDA team
Overduin, M.; Mayer, B.; Rios, C.B.; Baltimore, D.; Cowburn, D.
Secondary structure of Src homology 2 domain of c-Abl by heteronuclear NMR spectroscopy in solution
Proc. Natl. Acad. Sci. USA
89
11673-11677
1992
Homo sapiens (P00519)
Manually annotated by BRENDA team
Overduin, M.; Rios, C.B.; Mayer, B.J.; Baltimore, D.; Cowburn, D.
Three-dimensional solution structure of the src homology 2 domain of c-abl
Cell
70
697-704
1992
Homo sapiens (P00519)
Manually annotated by BRENDA team
Pisabarro, M.T.; Ortiz, A.R.; Serrano, L.; Wade, R.C.
Homology modeling of the Abl-SH3 domain
Proteins
20
203-215
1994
Homo sapiens (P00519)
Manually annotated by BRENDA team
Pisabarro, M.T.; Serrano, L.; Wilmanns, M.
Crystal structure of the abl-SH3 domain complexed with a designed high-affinity peptide ligand: implications for SH3-ligand interactions
J. Mol. Biol.
281
513-521
1998
Homo sapiens (P00519)
Manually annotated by BRENDA team
Shtivelman, E.; Lifshitz, B.; Gale, R.P.; Roe, B.A.; Canaani, E.
Alternative splicing of RNAs transcribed from the human abl gene and from the bcr-abl fused gene
Cell
47
277-284
1986
Homo sapiens (P00519), Homo sapiens
Manually annotated by BRENDA team
Musacchio, A.; Saraste, M.; Wilmanns, M.
High-resolution crystal structures of tyrosine kinase SH3 domains complexed with proline-rich peptides
Nat. Struct. Biol.
1
546-551
1994
Mus musculus (P00520), Homo sapiens (P06241)
Manually annotated by BRENDA team
Kawakami, T.; Pennington, C.Y.; Robbins, K.C.
Isolation and oncogenic potential of a novel human src-like gene
Mol. Cell. Biol.
6
4195-4201
1986
Homo sapiens (P06241)
Manually annotated by BRENDA team
Lee, C.H.; Saksela, K.; Mirza, U.A.; Chait, B.T.; Kuriyan, J.
Crystal structure of the conserved core of HIV-1 Nef complexed with a Src family SH3 domain
Cell
85
931-942
1996
Homo sapiens (P06241)
Manually annotated by BRENDA team
Morton, C.J.; Pugh, D.J.; Brown, E.L.; Kahmann, J.D.; Renzoni, D.A.; Campbell, I.D.
Solution structure and peptide binding of the SH3 domain from human Fyn
Structure
4
705-714
1996
Homo sapiens (P06241), Homo sapiens
Manually annotated by BRENDA team
Mulhern, T.D.; Shaw, G.L.; Morton, C.J.; Day, A.J.; Campbell, I.D.
The SH2 domain from the tyrosine kinase Fyn in complex with a phosphotyrosyl peptide reveals insights into domain stability and binding specificity
Structure
5
1313-1323
1997
Homo sapiens (P06241)
Manually annotated by BRENDA team
Noble, M.E.; Musacchio, A.; Saraste, M.; Courtneidge, S.A.; Wierenga, R.K.
Crystal structure of the SH3 domain in human Fyn; comparison of the three-dimensional structures of SH3 domains in tyrosine kinases and spectrin
EMBO J.
12
2617-2624
1993
Homo sapiens (P06241)
Manually annotated by BRENDA team
Peters, D.J.; McGrew, B.R.; Perron, D.C.; Liptak, L.M.; Laudano, A.P.
In vivo phosphorylation and membrane association of the fyn proto-oncogene product in IM-9 human lymphoblasts
Oncogene
5
1313-1319
1990
Homo sapiens (P06241), Homo sapiens
Manually annotated by BRENDA team
Renzoni, D.A.; Pugh, D.J.; Siligardi, G.; Das, P.; Morton, C.J.; Rossi, C.; Waterfield, M.D.; Campbell, I.D.; Ladbury, J.E.
Structural and thermodynamic characterization of the interaction of the SH3 domain from Fyn with the proline-rich binding site on the p85 subunit of PI3-kinase
Biochemistry
35
15646-15653
1996
Homo sapiens (P06241)
Manually annotated by BRENDA team
Semba, K.; Nishizawa, M.; Miyajima, N.; Yoshida, M.C.; Sukegawa, J.; Yamanashi, Y.; Sasaki, M.; Yamamoto, T.; Toyoshima, K.
yes-related protooncogene, syn, belongs to the protein-tyrosine kinase family
Proc. Natl. Acad. Sci. USA
83
5459-5463
1986
Homo sapiens (P06241), Homo sapiens
Manually annotated by BRENDA team
Alcalay, M.; Antolini, F.; Van de Ven, W.J.; Lanfrancone, L.; Grignani, F.; Pelicci, P.G.
Characterization of human and mouse c-fes cDNA clones and identification of the 5' end of the gene
Oncogene
5
267-275
1990
Homo sapiens (P07332), Homo sapiens
Manually annotated by BRENDA team
Roebroek, A.J.; Schalken, J.A.; Verbeek, J.S.; Van den Ouweland, A.M.; Onnekink, C.; Bloemers, H.P.; Van de Ven, W.J.
The structure of the human c-fes/fps proto-oncogene
EMBO J.
4
2897-2903
1985
Homo sapiens (P07332), Homo sapiens
Manually annotated by BRENDA team
Sukegawa, J.; Semba, K.; Yamanashi, Y.; Nishizawa, M.; Miyajima, N.; Yamamoto, T.; Toyoshima, K.
Characterization of cDNA clones for the human c-yes gene
Mol. Cell. Biol.
7
41-47
1987
Homo sapiens (P07947), Homo sapiens
Manually annotated by BRENDA team
Rider, L.G.; Raben, N.; Miller, L.; Jelsema, C.
The cDNAs encoding two forms of the LYN protein tyrosine kinase are expressed in rat mast cells and human myeloid cells
Gene
138
219-222
1994
Homo sapiens (P07948), Homo sapiens, Rattus norvegicus (Q07014)
Manually annotated by BRENDA team
Yamanashi, Y.; Fukushige, S.; Semba, K.; Sukegawa, J.; Miyajima, N.; Matsubara, K.; Yamamoto, T.; Toyoshima, K.
The yes-related cellular gene lyn encodes a possible tyrosine kinase similar to p56lck
Mol. Cell. Biol.
7
237-243
1987
Homo sapiens (P07948), Homo sapiens
Manually annotated by BRENDA team
Lee, S.T.; Strunk, K.M.; Spritz, R.A.
A survey of protein tyrosine kinase mRNAs expressed in normal human melanocytes
Oncogene
8
3403-3410
1993
Homo sapiens (P23458), Homo sapiens (Q05397)
Manually annotated by BRENDA team
Lock, P.; Ralph, S.; Stanley, E.; Boulet, I.; Ramsay, R.; Dunn, A.R.
Two isoforms of murine hck, generated by utilization of alternative translational initiation codons, exhibit different patterns of subcellular localization
Mol. Cell. Biol.
11
4363-4370
1991
Mus musculus (P08103), Homo sapiens (P08631)
Manually annotated by BRENDA team
Arold, S.; O'Brien, R.; Franken, P.; Strub, M.P.; Hoh, F.; Dumas, C.; Ladbury, J.E.
RT loop flexibility enhances the specificity of Src family SH3 domains for HIV-1 Nef
Biochemistry
37
14683-14691
1998
Homo sapiens (P08631)
Manually annotated by BRENDA team
Deloukas, P.; Matthews, L.H.; Ashurst, J.; Burton, J.; Gilbert, J.G.; et al.
The DNA sequence and comparative analysis of human chromosome 20
Nature
414
865-871
2001
Homo sapiens (P08631), Homo sapiens (Q13882)
Manually annotated by BRENDA team
Horita, D.A.; Baldisseri, D.M.; Zhang, W.; Altieri, A.S.; Smithgall, T.E.; Gmeiner, W.H.; Byrd, R.A.
Solution structure of the human Hck SH3 domain and identification of its ligand binding site
J. Mol. Biol.
278
253-265
1998
Homo sapiens (P08631), Homo sapiens
Manually annotated by BRENDA team
Hradetzky, D.; Strebhardt, K.; Rubsamen-Waigmann, H.
The genomic locus of the human hemopoietic-specific cell protein tyrosine kinase (PTK)-encoding gene (HCK) confirms conservation of exon-intron structure among human PTKs of the src family
Gene
113
275-280
1992
Homo sapiens (P08631)
Manually annotated by BRENDA team
Quintrell, N.; Lebo, R.; Varmus, H.; Bishop, J.M.; Pettenati, M.J.; Le Beau, M.M.; Diaz, M.O.; Rowley, J.D.
Identification of a human gene (HCK) that encodes a protein-tyrosine kinase and is expressed in hemopoietic cells
Mol. Cell. Biol.
7
2267-2275
1987
Homo sapiens (P08631), Homo sapiens
Manually annotated by BRENDA team
Sicheri, F.; Moarefi, I.; Kuriyan, J.
Crystal structure of the Src family tyrosine kinase Hck
Nature
385
602-609
1997
Homo sapiens (P08631)
Manually annotated by BRENDA team
Zhang, W.; Smithgall, T.E.; Gmeiner, W.H.
Sequential assignment and secondary structure determination for the Src homology 2 domain of hematopoietic cellular kinase
FEBS Lett.
406
131-135
1997
Homo sapiens (P08631)
Manually annotated by BRENDA team
Ziegler, S.F.; Marth, J.D.; Lewis, D.B.; Perlmutter, R.M.
Novel protein-tyrosine kinase gene (hck) preferentially expressed in cells of hematopoietic origin
Mol. Cell. Biol.
7
2276-2285
1987
Homo sapiens (P08631), Homo sapiens
Manually annotated by BRENDA team
Anderson, S.K.; Gibbs, C.P.; Tanaka, A.; Kung, H.J.; Fujita, D.J.
Human cellular src gene: nucleotide sequence and derived amino acid sequence of the region coding for the carboxy-terminal two-thirds of pp60c-src
Mol. Cell. Biol.
5
1122-1129
1985
Homo sapiens (P12931), Homo sapiens
Manually annotated by BRENDA team
Charifson, P.S.; Shewchuk, L.M.; Rocque, W.; Hummel, C.W.; Jordan, S.R.; Mohr, C.; Pacofsky, G.J.; Peel, M.R.; Rodriguez, M.; Sternbach, D.D.; Consler, T.G.
Peptide ligands of pp60(c-src) SH2 domains: a thermodynamic and structural study
Biochemistry
36
6283-6293
1997
Homo sapiens (P12931)
Manually annotated by BRENDA team
Parker, R.C.; Mardon, G.; Lebo, R.V.; Varmus, H.E.; Bishop, J.M.
Isolation of duplicated human c-src genes located on chromosomes 1 and 20
Mol. Cell. Biol.
5
831-838
1985
Homo sapiens (P12931)
Manually annotated by BRENDA team
Tanaka, A.; Gibbs, C.P.; Arthur, R.R.; Anderson, S.K.; Kung, H.J.; Fujita, D.J.
DNA sequence encoding the amino-terminal region of the human c-src protein: implications of sequence divergence among src-type kinase oncogenes
Mol. Cell. Biol.
7
1978-1983
1987
Homo sapiens (P12931)
Manually annotated by BRENDA team
Xu, R.X.; Word, J.M.; Davis, D.G.; Rink, M.J.; Willard, D.H., Jr.; Gampe, R.T., Jr.
Solution structure of the human pp60c-src SH2 domain complexed with a phosphorylated tyrosine pentapeptide
Biochemistry
34
2107-2121
1995
Homo sapiens (P12931), Homo sapiens
Manually annotated by BRENDA team
Xu, W.; Harrison, S.C.; Eck, M.J.
Three-dimensional structure of the tyrosine kinase c-Src
Nature
385
595-602
1997
Homo sapiens (P12931)
Manually annotated by BRENDA team
Hao, Q.L.; Ferris, D.K.; White, G.; Heisterkamp, N.; Groffen, J.
Nuclear and cytoplasmic location of the FER tyrosine kinase
Mol. Cell. Biol.
11
1180-1183
1991
Homo sapiens (P16591)
Manually annotated by BRENDA team
Hao, Q.L.; Heisterkamp, N.; Groffen, J.
Isolation and sequence analysis of a novel human tyrosine kinase gene
Mol. Cell. Biol.
9
1587-1593
1989
Homo sapiens (P16591), Homo sapiens
Manually annotated by BRENDA team
Nishisho, I.; Nakamura, Y.; Miyoshi, Y.; Miki, Y.; Ando, H.; Horii, A.; Koyama, K.; Utsunomiya, J.; Baba, S.; Hedge, P.
Mutations of chromosome 5q21 genes in FAP and colorectal cancer patients
Science
253
665-669
1991
Homo sapiens (P16591)
Manually annotated by BRENDA team
Partanen, J.; Makela, T.P.; Alitalo, R.; Lehvaslaiho, H.; Alitalo, K.
Putative tyrosine kinases expressed in K-562 human leukemia cells
Proc. Natl. Acad. Sci. USA
87
8913-8917
1990
Homo sapiens (P29597)
Manually annotated by BRENDA team
Wilks, A.F.; Harpur, A.G.; Kurban, R.R.; Ralph, S.J.; Zurcher, G.; Ziemiecki, A.
Two novel protein-tyrosine kinases, each with a second phosphotransferase-related catalytic domain, define a new class of protein kinase
Mol. Cell. Biol.
11
2057-2065
1991
Homo sapiens (P23458)
Manually annotated by BRENDA team
Colamonici, O.; Yan, H.; Domanski, P.; Handa, R.; Smalley, D.; Mullersman, J.; Witte, M.; Krishnan, K.; Krolewski, J.
Direct binding to and tyrosine phosphorylation of the alpha subunit of the type I interferon receptor by p135tyk2 tyrosine kinase
Mol. Cell. Biol.
14
8133-8142
1994
Homo sapiens (P29597), Homo sapiens
Manually annotated by BRENDA team
Firmbach-Kraft, I.; Byers, M.; Shows, T.; Dalla-Favera, R.; Krolewski, J.J.
Tyk2, prototype of a novel class of non-receptor tyrosine kinase genes
Oncogene
5
1329-1336
1990
Homo sapiens (P29597), Homo sapiens
Manually annotated by BRENDA team
Borchert, T.V.; Mathieu, M.; Zeelen, J.P.; Courtneidge, S.A.; Wierenga, R.K.
The crystal structure of human CskSH3: structural diversity near the RT-Src and n-Src loop
FEBS Lett.
341
79-85
1994
Homo sapiens (P41240)
Manually annotated by BRENDA team
Brauninger, A.; Karn, T.; Strebhardt, K.; Rubsamen-Waigmann, H.
Characterization of the human CSK locus
Oncogene
8
1365-1369
1993
Homo sapiens (P41240), Homo sapiens
Manually annotated by BRENDA team
Holtrich, U.; Brauninger, A.; Strebhardt, K.; Rubsamen-Waigmann, H.
Two additional protein-tyrosine kinases expressed in human lung: fourth member of the fibroblast growth factor receptor family and an intracellular protein-tyrosine kinase
Proc. Natl. Acad. Sci. USA
88
10411-10415
1991
Homo sapiens (P41240), Homo sapiens
Manually annotated by BRENDA team
Partanen, J.; Armstrong, E.; Bergman, M.; Makela, T.P.; Hirvonen, H.; Huebner, K.; Alitalo, K.
Cyl encodes a putative cytoplasmic tyrosine kinase lacking the conserved tyrosine autophosphorylation site (Y416src)
Oncogene
6
2013-2018
1991
Homo sapiens (P41240)
Manually annotated by BRENDA team
Avraham, S.; Jiang, S.; Ota, S.; Fu, Y.; Deng, B.; Dowler, L.L.; White, R.A.; Avraham, H.
Structural and functional studies of the intracellular tyrosine kinase MATK gene and its translated product
J. Biol. Chem.
270
1833-1842
1995
Homo sapiens (P42679)
Manually annotated by BRENDA team
Bennett, B.D.; Cowley, S.; Jiang, S.; London, R.; Deng, B.; Grabarek, J.; Groopman, J.E.; Goeddel, D.V.; Avraham, H.
Identification and characterization of a novel tyrosine kinase from megakaryocytes
J. Biol. Chem.
269
1068-1074
1994
Homo sapiens (P42679)
Manually annotated by BRENDA team
Hamaguchi, I.; Iwama, A.; Yamaguchi, N.; Sakano, S.; Matsuda, Y.; Suda, T.
Characterization of mouse non-receptor tyrosine kinase gene, HYL
Oncogene
9
3371-3374
1994
Homo sapiens (P42679), Homo sapiens
Manually annotated by BRENDA team
Sakano, S.; Iwama, A.; Inazawa, J.; Ariyama, T.; Ohno, M.; Suda, T.
Molecular cloning of a novel non-receptor tyrosine kinase, HYL (hematopoietic consensus tyrosine-lacking kinase)
Oncogene
9
1155-1161
1994
Homo sapiens (P42679), Homo sapiens
Manually annotated by BRENDA team
Sato, K.; Mano, H.; Ariyama, T.; Inazawa, J.; Yazaki, Y.; Hirai, H.
Molecular cloning and analysis of the human Tec protein-tyrosine kinase
Leukemia
8
1663-1672
1994
Homo sapiens (P42680), Homo sapiens
Manually annotated by BRENDA team
Haire, R.N.; Ohta, Y.; Lewis, J.E.; Fu, S.M.; Kroisel, P.; Litman, G.W.
TXK, a novel human tyrosine kinase expressed in T cells shares sequence identity with Tec family kinases and maps to 4p12
Hum. Mol. Genet.
3
897-901
1994
Homo sapiens (P42681)
Manually annotated by BRENDA team
Ohta, Y.; Haire, R.N.; Amemiya, C.T.; Litman, R.T.; Trager, T.; Riess, O.; Litman, G.W.
Human Txk: genomic organization, structure and contiguous physical linkage with the Tec gene
Oncogene
12
937-942
1996
Homo sapiens (P42681)
Manually annotated by BRENDA team
Kruh, G.D.; Perego, R.; Miki, T.; Aaronson, S.A.
The complete coding sequence of arg defines the Abelson subfamily of cytoplasmic tyrosine kinases
Proc. Natl. Acad. Sci. USA
87
5802-5806
1990
Homo sapiens (P42684), Homo sapiens
Manually annotated by BRENDA team
Cance, W.G.; Craven, R.J.; Bergman, M.; Xu, L.; Alitalo, K.; Liu, E.T.
Rak, a novel nuclear tyrosine kinase expressed in epithelial cells
Cell Growth Differ.
5
1347-1355
1994
Homo sapiens (P42685)
Manually annotated by BRENDA team
Cance, W.G.; Craven, R.J.; Weiner, T.M.; Liu, E.T.
Novel protein kinases expressed in human breast cancer
Int. J. Cancer
54
571-577
1993
Homo sapiens (P42685)
Manually annotated by BRENDA team
Lee, J.; Wang, Z.; Luoh, S.M.; Wood, W.I.; Scadden, D.T.
Cloning of FRK, a novel human intracellular SRC-like tyrosine kinase-encoding gene
Gene
138
247-251
1994
Homo sapiens (P42685), Homo sapiens
Manually annotated by BRENDA team
Chan, A.C.; Iwashima, M.; Turck, C.W.; Weiss, A.
ZAP-70: a 70 kd protein-tyrosine kinase that associates with the TCR zeta chain
Cell
71
649-662
1992
Homo sapiens (P43403)
Manually annotated by BRENDA team
Chan, A.C.; Kadlecek, T.A.; Elder, M.E.; Filipovich, A.H.; Kuo, W.L.; Iwashima, M.; Parslow, T.G.; Weiss, A.
ZAP-70 deficiency in an autosomal recessive form of severe combined immunodeficiency
Science
264
1599-1601
1994
Homo sapiens (P43403)
Manually annotated by BRENDA team
Isakov, N.; Wange, R.L.; Burgess, W.H.; Watts, J.D.; Aebersold, R.; Samelson, L.E.
ZAP-70 binding specificity to T cell receptor tyrosine-based activation motifs: the tandem SH2 domains of ZAP-70 bind distinct tyrosine-based activation motifs with varying affinity
J. Exp. Med.
181
375-380
1995
Homo sapiens (P43403)
Manually annotated by BRENDA team
Futterer, K.; Wong, J.; Grucza, R.A.; Chan, A.C.; Waksman, G.
Structural basis for Syk tyrosine kinase ubiquity in signal transduction pathways revealed by the crystal structure of its regulatory SH2 domains bound to a dually phosphorylated ITAM peptide
J. Mol. Biol.
281
523-537
1998
Homo sapiens (P43405)
Manually annotated by BRENDA team
Law, C.L.; Sidorenko, S.P.; Chandran, K.A.; Draves, K.E.; Chan, A.C.; Weiss, A.; Edelhoff, S.; Disteche, C.M.; Clark, E.A.
Molecular cloning of human Syk. A B cell protein-tyrosine kinase associated with the surface immunoglobulin M-B cell receptor complex
J. Biol. Chem.
269
12310-12319
1994
Homo sapiens (P43405), Homo sapiens
Manually annotated by BRENDA team
Muller, B.; Cooper, L.; Terhorst, C.
Molecular cloning of the human homologue to the pig protein-tyrosine kinase syk
Immunogenetics
39
359-362
1994
Homo sapiens (P43405), Homo sapiens
Manually annotated by BRENDA team
Narula, S.S.; Yuan, R.W.; Adams, S.E.; Green, O.M.; Green, J.; Philips, T.B.; Zydowsky, L.D.; Botfield, M.C.; Hatada, M.; Laird, E.R.; et al.
Solution structure of the C-terminal SH2 domain of the human tyrosine kinase Syk complexed with a phosphotyrosine pentapeptide
Structure
3
1061-1073
1995
Homo sapiens (P43405), Homo sapiens
Manually annotated by BRENDA team
Yagi, S.; Suzuki, K.; Hasegawa, A.; Okumura, K.; Ra, C.
Cloning of the cDNA for the deleted syk kinase homologous to ZAP-70 from human basophilic leukemia cell line (KU812)
Biochem. Biophys. Res. Commun.
200
28-34
1994
Homo sapiens (P43405), Homo sapiens
Manually annotated by BRENDA team
Drebin, J.A.; Hartzell, S.W.; Griffin, C.; Campbell, M.J.; Niederhuber, J.E.
Molecular cloning and chromosomal localization of the human homologue of a B-lymphocyte specific protein tyrosine kinase (blk)
Oncogene
10
477-486
1995
Homo sapiens (P51451), Homo sapiens
Manually annotated by BRENDA team
Islam, K.B.; Rabbani, H.; Larsson, C.; Sanders, R.; Smith, C.I.
Molecular cloning, characterization, and chromosomal localization of a human lymphoid tyrosine kinase related to murine Blk
J. Immunol.
154
1265-1272
1995
Homo sapiens (P51451), Homo sapiens
Manually annotated by BRENDA team
Qiu, Y.; Robinson, D.; Pretlow, T.G.; Kung, H.J.
Etk/Bmx, a tyrosine kinase with a pleckstrin-homology domain, is an effector of phosphatidylinositol 3'-kinase and is involved in interleukin 6-induced neuroendocrine differentiation of prostate cancer cells
Proc. Natl. Acad. Sci. USA
95
3644-3649
1998
Homo sapiens (P51813)
Manually annotated by BRENDA team
Tamagnone, L.; Lahtinen, I.; Mustonen, T.; Virtaneva, K.; Francis, F.; Muscatelli, F.; Alitalo, R.; Smith, C.I.; Larsson, C.; Alitalo, K.
BMX, a novel nonreceptor tyrosine kinase gene of the BTK/ITK/TEC/TXK family located in chromosome Xp22.2
Oncogene
9
3683-3688
1994
Homo sapiens (P51813), Homo sapiens
Manually annotated by BRENDA team
Bozzi, F.; Lefranc, G.; Villa, A.; Badolato, R.; Schumacher, R.F.; Khalil, G.; Loiselet, J.; Bresciani, S.; O'Shea, J.J.; Vezzoni, P.; Notarangelo, L.D.; Candotti, F.
Molecular and biochemical characterization of JAK3 deficiency in a patient with severe combined immunodeficiency over 20 years after bone marrow transplantation: implications for treatment
Br. J. Haematol.
102
1363-1366
1998
Homo sapiens (P52333)
Manually annotated by BRENDA team
Candotti, F.; Oakes, S.A.; Johnston, J.A.; Giliani, S.; Schumacher, R.F.; Mella, P.; Fiorini, M.; Ugazio, A.G.; Badolato, R.; Notarangelo, L.D.; Bozzi, F.; Macchi, P.; Strina, D.; Vezzoni, P.; Blaese, R.M.; O'Shea, J.J.; Villa, A.
Structural and functional basis for JAK3-deficient severe combined immunodeficiency
Blood
90
3996-4003
1997
Homo sapiens (P52333), Homo sapiens
Manually annotated by BRENDA team
Kawamura, M.; McVicar, D.W.; Johnston, J.A.; Blake, T.B.; Chen, Y.Q.; Lal, B.K.; Lloyd, A.R.; Kelvin, D.J.; Staples, J.E.; Ortaldo, J.R.; et al.
Molecular cloning of L-JAK, a Janus family protein-tyrosine kinase expressed in natural killer cells and activated leukocytes
Proc. Natl. Acad. Sci. USA
91
6374-6378
1994
Homo sapiens (P52333)
Manually annotated by BRENDA team
Lai, K.S.; Jin, Y.; Graham, D.K.; Witthuhn, B.A.; Ihle, J.N.; Liu, E.T.
A kinase-deficient splice variant of the human JAK3 is expressed in hematopoietic and epithelial cancer cells
J. Biol. Chem.
270
25028-25036
1995
Homo sapiens (P52333)
Manually annotated by BRENDA team
Macchi, P.; Villa, A.; Giliani, S.; Sacco, M.G.; Frattini, A.; Porta, F.; Ugazio, A.G.; Johnston, J.A.; Candotti, F.; O'Shea, J.J.; et al.
Mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency (SCID)
Nature
377
65-68
1995
Homo sapiens (P52333)
Manually annotated by BRENDA team
Schumacher, R.F.; Mella, P.; Badolato, R.; Fiorini, M.; Savoldi, G.; Giliani, S.; Villa, A.; Candotti, F.; Tampalini, A.; O'Shea, J.J.; Notarangelo, L.D.
Complete genomic organization of the human JAK3 gene and mutation analysis in severe combined immunodeficiency by single-strand conformation polymorphism
Hum. Genet.
106
73-79
2000
Homo sapiens (P52333)
Manually annotated by BRENDA team
Verbsky, J.W.; Bach, E.A.; Fang, Y.F.; Yang, L.; Randolph, D.A.; Fields, L.E.
Expression of Janus kinase 3 in human endothelial and other non-lymphoid and non-myeloid cells
J. Biol. Chem.
271
13976-13980
1996
Homo sapiens (P52333), Homo sapiens
Manually annotated by BRENDA team
Gibson, S.; Leung, B.; Squire, J.A.; Hill, M.; Arima, N.; Goss, P.; Hogg, D.; Mills, G.B.
Identification, cloning, and characterization of a novel human T-cell-specific tyrosine kinase located at the hematopoietin complex on chromosome 5q
Blood
82
1561-1572
1993
Homo sapiens (Q08881)
Manually annotated by BRENDA team
Tanaka, N.; Asao, H.; Ohtani, K.; Nakamura, M.; Sugamura, K.
A novel human tyrosine kinase gene inducible in T cells by interleukin 2
FEBS Lett.
324
1-5
1993
Homo sapiens (Q08881)
Manually annotated by BRENDA team
Kamalati, T.; Jolin, H.E.; Mitchell, P.J.; Barker, K.T.; Jackson, L.E.; Dean, C.J.; Page, M.J.; Gusterson, B.A.; Crompton, M.R.
Brk, a breast tumor-derived non-receptor protein-tyrosine kinase, sensitizes mammary epithelial cells to epidermal growth factor
J. Biol. Chem.
271
30956-30963
1996
Homo sapiens (Q13882), Homo sapiens
Manually annotated by BRENDA team
Lee, H.; Kim, M.; Lee, K.H.; Kang, K.N.; Lee, S.T.
Exon-intron structure of the human PTK6 gene demonstrates that PTK6 constitutes a distinct family of non-receptor tyrosine kinase
Mol. Cells
8
401-407
1998
Homo sapiens (Q13882), Homo sapiens
Manually annotated by BRENDA team
Mitchell, P.J.; Barker, K.T.; Martindale, J.E.; Kamalati, T.; Lowe, P.N.; Page, M.J.; Gusterson, B.A.; Crompton, M.R.
Cloning and characterisation of cDNAs encoding a novel non-receptor tyrosine kinase, brk, expressed in human breast tumours
Oncogene
9
2383-2390
1994
Homo sapiens (Q13882), Homo sapiens
Manually annotated by BRENDA team
Whitney, G.S.; Chan, P.Y.; Blake, J.; Cosand, W.L.; Neubauer, M.G.; Aruffo, A.; Kanner, S.B.
Human T and B lymphocytes express a structurally conserved focal adhesion kinase, pp125FAK
DNA Cell Biol.
12
823-830
1993
Homo sapiens (Q05397), Homo sapiens
Manually annotated by BRENDA team
Andre, E.; Becker-Andre, M.
Expression of an N-terminally truncated form of human focal adhesion kinase in brain
Biochem. Biophys. Res. Commun.
190
140-147
1993
Homo sapiens (Q05397), Homo sapiens
Manually annotated by BRENDA team
O'Donovan, C.; Martin, M.J.; Gattiker, A.; Gasteiger, E.; Bairoch, A.; Apweiler, R.
High quality protein knowledge resources: Swiss-Prot and TrEMBL
Brief. Bioinform.
2
275-284
2002
Rattus norvegicus (P70600), Homo sapiens (Q14289)
-
Manually annotated by BRENDA team
Delcommenne, M.; Tan, C.; Gray, V.; Rue, L.; Woodgett, J.; Dedhar, S.
Phosphoinositide-3-OH kinase-dependent regulation of glycogen synthase kinase 3 and protein kinase B/AKT by the integrin-linked kinase
Proc. Natl. Acad. Sci. USA
95
11211-11216
1998
Homo sapiens (Q13418)
Manually annotated by BRENDA team
Perlman, R.; Schiemann, W.P.; Brooks, M.W.; Lodish, H.F.; Weinberg, R.A.
TGF-beta-induced apoptosis is mediated by the adapter protein Daxx that facilitates JNK activation
Nat. Cell Biol.
3
708-714
2001
Homo sapiens (P37173)
Manually annotated by BRENDA team
Howe, J.R.; Bair, J.L.; Sayed, M.G.; Anderson, M.E.; Mitros, F.A.; Petersen, G.M.; Velculescu, V.E.; Traverso, G.; Vogelstein, B.
Germline mutations of the gene encoding bone morphogenetic protein receptor 1A in juvenile polyposis
Nat. Genet.
28
184-187
2001
Homo sapiens (P36894), Homo sapiens
Manually annotated by BRENDA team
Masiakos, P.T.; MacLaughlin, D.T.; Maheswaran, S.; Teixeira, J.; Fuller, A.F., Jr.; Shah, P.C.; Kehas, D.J.; Kenneally, M.K.; Dombkowski, D.M.; Ha, T.U.; Preffer, F.I.; Donahoe, P.K.
Human ovarian cancer, cell lines, and primary ascites cells express the human Mullerian inhibiting substance (MIS) type II receptor, bind, and are responsive to MIS
Clin. Cancer Res.
5
3488-3499
1999
Homo sapiens (Q16671), Homo sapiens
Manually annotated by BRENDA team
Lu, S.L.; Kawabata, M.; Imamura, T.; Akiyama, Y.; Nomizu, T.; Miyazono, K.; Yuasa, Y.
HNPCC associated with germline mutation in the TGF-beta type II receptor gene
Nat. Genet.
19
17-18
1998
Homo sapiens (P37173)
Manually annotated by BRENDA team
Vellucci, V.F.; Reiss, M.
Cloning and genomic organization of the human transforming growth factor-beta type I receptor gene
Genomics
46
278-283
1997
Homo sapiens (P36897), Homo sapiens
Manually annotated by BRENDA team
Ide, H.; Katoh, M.; Sasaki, H.; Yoshida, T.; Aoki, K.; Nawa, Y.; Osada, Y.; Sugimura, T.; Terada, M.
Cloning of human bone morphogenetic protein type IB receptor (BMPR-IB) and its expression in prostate cancer in comparison with other BMPRs
Oncogene
14
1377-1382
1997
Homo sapiens (O00238), Homo sapiens
Manually annotated by BRENDA team
Berg, J.N.; Gallione, C.J.; Stenzel, T.T.; et al.
The activin receptor-like kinase 1 gene: genomic structure and mutations in hereditary hemorrhagic telangiectasia type 2
Am. J. Hum. Genet.
61
60-67
1997
Homo sapiens (P37023)
Manually annotated by BRENDA team
Takenoshita, S.; Hagiwara, K.; Nagashima, M.; Gemma, A.; Bennett, W.P.; Harris, C.C.
The genomic structure of the gene encoding the human transforming growth factor beta type II receptor (TGF-beta RII)
Genomics
36
341-344
1996
Homo sapiens (P37173), Homo sapiens
Manually annotated by BRENDA team
Ogasa, H.; Noma, T.; Murata, H.; Kawai, S.; Nakazawa, A.
Cloning of a cDNA encoding the human transforming growth factor-beta type II receptor: heterogeneity of the mRNA
Gene
181
185-190
1996
Homo sapiens (P37173)
Manually annotated by BRENDA team
Lu, S.L.; Zhang, W.C.; Akiyama, Y.; Nomizu, T.; Yuasa, Y.
Genomic structure of thetransforming growth factor beta type II receptor gene and its mutations in hereditary nonpolyposis colorectal cancers
Cancer Res.
56
4595-4598
1996
Homo sapiens (P37173)
Manually annotated by BRENDA team
Johnson, D.W.; Berg, J.N.; Baldwin, M.A.; Gallione, C.J.; Marondel, I.; Yoon, S.J.; Stenzel, T.T.; Speer, M.; Pericak-Vance, M.A.; Diamond, A.; Guttmacher, A.E.; Jackson, C.E.; Attisano, L.; Kucherlapati, R.; Porteous, M.E.; Marchuk, D.A.
Mutations in the activin receptor-like kinase 1 gene in hereditary haemorrhagic telangiectasia type 2
Nat. Genet.
13
189-195
1996
Homo sapiens (P37023)
Manually annotated by BRENDA team
Visser, J.A.; McLuskey, A.; van Beers, T.; Weghuis, D.O.; van Kessel, A.G.; Grootegoed, J.A.; Themmen, A.P.
Structure and chromosomal localization of the human anti-mullerian hormone type II receptor gene
Biochem. Biophys. Res. Commun.
215
1029-1036
1995
Homo sapiens (Q16671)
Manually annotated by BRENDA team
Jokiranta, T.S.; Tissari, J.; Teleman, O.; Meri, S.
Extracellular domain of type I receptor for transforming growth factor-beta: molecular modelling using protectin (CD59) as a template
FEBS Lett.
376
31-36
1995
Homo sapiens (P36897)
Manually annotated by BRENDA team
Imbeaud, S.; Faure, E.; Lamarre, I.; Mattei, M.G.; di Clemente, N.; Tizard, R.; Carre-Eusebe, D.; Belville, C.; Tragethon, L.; Tonkin, C.; et al.
Insensitivity to anti-mullerian hormone due to a mutation in the human anti-mullerian hormone receptor
Nat. Genet.
11
382-388
1995
Homo sapiens (Q16671)
Manually annotated by BRENDA team
Xu, J.; Matsuzaki, K.; McKeehan, K.; Wang, F.; Kan, M.; McKeehan, W.L.
Genomic structure and cloned cDNAs predict that four variants in the kinase domain of serine/threonine kinase receptors arise by alternative splicing and poly(A) addition
Proc. Natl. Acad. Sci. USA
91
7957-7961
1994
Homo sapiens (P36896)
Manually annotated by BRENDA team
Carcamo, J.; Weis, F.M.; Ventura, F.; Wieser, R.; Wrana, J.L.; Attisano, L.; Massague, J.
Type I receptors specify growth-inhibitory and transcriptional responses to transforming growth factor beta and activin
Mol. Cell. Biol.
14
3810-3821
1994
Homo sapiens (P36896)
Manually annotated by BRENDA team
ten Dijke, P.; Ichijo, H.; Franzen, P.; Schulz, P.; Saras, J.; Toyoshima, H.; Heldin, C.H.; Miyazono, K.
Activin receptor-like kinases: a novel subclass of cell-surface receptors with predicted serine/threonine kinase activity
Oncogene
8
2879-2887
1993
Homo sapiens (P36894), Homo sapiens (P37023), Homo sapiens (Q04771), Homo sapiens, Mus musculus (P36898)
Manually annotated by BRENDA team
Matsuzaki, K.; Xu, J.; Wang, F.; McKeehan, W.L.; Krummen, L.; Kan, M.
A widely expressed transmembrane serine/threonine kinase that does not bind activin, inhibin, transforming growth factor beta, or bone morphogenic factor
J. Biol. Chem.
268
12719-12723
1993
Homo sapiens (Q04771), Homo sapiens
Manually annotated by BRENDA team
Franzen, P.; ten Dijke, P.; Ichijo, H.; Yamashita, H.; Schulz, P.; Heldin, C.H.; Miyazono, K.
Cloning of a TGF beta type I receptor that forms a heteromeric complex with the TGF beta type II receptor
Cell
75
681-692
1993
Homo sapiens (P36897)
Manually annotated by BRENDA team
Attisano, L.; Carcamo, J.; Ventura, F.; Weis, F.M.; Massague, J.; Wrana, J.L.
Identification of human activin and TGF beta type I receptors that form heteromeric kinase complexes with type II receptors
Cell
75
671-680
1993
Homo sapiens (P37023)
Manually annotated by BRENDA team
Matzuk, M.M.; Bradley, A.
Cloning of the human activin receptor cDNA reveals high evolutionary conservation
Biochim. Biophys. Acta
1130
105-108
1992
Homo sapiens (P27037)
Manually annotated by BRENDA team
Lin, H.Y.; Wang, X.F.; Ng-Eaton, E.; Weinberg, R.A.; Lodish, H.F.
Expression cloning of the TGF-beta type II receptor, a functional transmembrane serine/threonine kinase
Cell
68
775-785
1992
Homo sapiens (P37173)
Manually annotated by BRENDA team
Donaldson, C.J.; Mathews, L.S.; Vale, W.W.
Molecular cloning and binding properties of the human type II activin receptor
Biochem. Biophys. Res. Commun.
184
310-316
1992
Homo sapiens (P27037)
Manually annotated by BRENDA team
Watson, R.; Oskarsson, M.; Vande Woude, G.F.
Human DNA sequence homologous to the transforming gene (mos) of Moloney murine sarcoma virus
Proc. Natl. Acad. Sci. USA
79
4078-4082
1982
Homo sapiens (P00540)
Manually annotated by BRENDA team
Janji, B.; Melchior, C.; Vallar, L.; Kieffer, N.
Cloning of an isoform of integrin-linked kinase (ILK) that is upregulated in HT-144 melanoma cells following TGF-beta1 stimulation
Oncogene
19
3069-3077
2000
Homo sapiens (Q13418)
Manually annotated by BRENDA team
Li, F.; Liu, J.; Mayne, R.; Wu, C.
Identification and characterization of a mouse protein kinase that is highly homologous to human integrin-linked kinase
Biochim. Biophys. Acta
1358
215-220
1997
Homo sapiens (Q13418), Mus musculus (O55222)
Manually annotated by BRENDA team
Dedhar, S.
Cell-substrate interactions and signaling through ILK
Curr. Opin. Cell Biol.
12
250-256
2000
Homo sapiens (Q13418)
Manually annotated by BRENDA team
Hannigan, G.E.; Leung-Hagesteijn, C.; Fitz-Gibbon, L.; Coppolino, M.G.; Radeva, G.; Filmus, J.; Bell, J.C.; Dedhar, S.
Regulation of cell adhesion and anchorage-dependent growth by a new beta 1-integrin-linked protein kinase
Nature
379
91-96
1996
Homo sapiens (Q13418)
Manually annotated by BRENDA team
Muzio, M.; Ni, J.; Feng, P.; Dixit, V.M.
IRAK (Pelle) family member IRAK-2 and MyD88 as proximal mediators of IL-1 signaling
Science
278
1612-1615
1997
Homo sapiens (O43187)
Manually annotated by BRENDA team
Cao, Z.; Henzel, W.J.; Gao, X.
IRAK: a kinase associated with the interleukin-1 receptor
Science
271
1128-1131
1996
Homo sapiens (P51617)
Manually annotated by BRENDA team
Okano, I.; Hiraoka, J.; Otera, H.; Nunoue, K.; Ohashi, K.; Iwashita, S.; Hirai, M.; Mizuno, K.
Identification and characterization of a novel family of serine/threonine kinases containing two N-terminal LIM motifs
J. Biol. Chem.
270
31321-31330
1995
Homo sapiens (P53671)
Manually annotated by BRENDA team
Toshima, J.; Ohashi, K.; Okano, I.; Nunoue, K.; Kishioka, M.; Kuma, K.; Miyata, T.; Hirai, M.; Baba, T.; Mizuno, K.
Identification and characterization of a novel protein kinase, TESK1, specifically expressed in testicular germ cells
J. Biol. Chem.
270
31331-31337
1995
Homo sapiens (Q15569), Homo sapiens, Rattus norvegicus (Q63572)
Manually annotated by BRENDA team
Toshima, J.; Toshima, J.Y.; Takeuchi, K.; Mori, R.; Mizuno, K.
Cofilin phosphorylation and actin reorganization activities of testicular protein kinase 2 and its predominant expression in testicular Sertoli cells
J. Biol. Chem.
276
31449-31458
2001
Rattus norvegicus (Q924U5), Homo sapiens (Q96S53)
Manually annotated by BRENDA team
Rosok, O.; Pedeutour, F.; Ree, A.H.; Aasheim, H.C.
Identification and characterization of TESK2, a novel member of the LIMK/TESK family of protein kinases, predominantly expressed in testis
Genomics
61
44-54
1999
Homo sapiens (Q96S53), Homo sapiens
Manually annotated by BRENDA team
McCarthy, J.V.; Ni, J.; Dixit, V.M.
RIP2 is a novel NF-kappaB-activating and cell death-inducing kinase
J. Biol. Chem.
273
16968-16975
1998
Homo sapiens (O43353)
Manually annotated by BRENDA team
Thome, M.; Hofmann, K.; Burns, K.; Martinon, F.; Bodmer, J.L.; Mattmann, C.; Tschopp, J.
Identification of CARDIAK, a RIP-like kinase that associates with caspase-1
Curr. Biol.
8
885-888
1998
Homo sapiens (O43353)
Manually annotated by BRENDA team
King, A.J.; Sun, H.; Diaz, B.; Barnard, D.; Miao, W.; Bagrodia, S.; Marshall, M.S.
The protein kinase Pak3 positively regulates Raf-1 activity through phosphorylation of serine 338
Nature
396
180-183
1998
Homo sapiens (P04049)
Manually annotated by BRENDA team
Mott, H.R.; Carpenter, J.W.; Zhong, S.; Ghosh, S.; Bell, R.M.; Campbell, S.L.
The solution structure of the Raf-1 cysteine-rich domain: a novel ras and phospholipid binding site
Proc. Natl. Acad. Sci. USA
93
8312-8317
1996
Homo sapiens (P04049)
Manually annotated by BRENDA team
Nassar, N.; Horn, G.; Herrmann, C.; Block, C.; Janknecht, R.; Wittinghofer, A.
Ras/Rap effector specificity determined by charge reversal
Nat. Struct. Biol.
3
723-729
1996
Homo sapiens (P04049)
Manually annotated by BRENDA team
Nassar, N.; Horn, G.; Herrmann, C.; Scherer, A.; McCormick, F.; Wittinghofer, A.
The 2.2 A crystal structure of the Ras-binding domain of the serine/threonine kinase c-Raf1 in complex with Rap1A and a GTP analogue
Nature
375
554-560
1995
Homo sapiens (P04049)
Manually annotated by BRENDA team
Lee, J.E.; Beck, T.W.; Brennscheidt, U.; DeGennaro, L.J.; Rapp, U.R.
The complete sequence and promoter activity of the human A-raf-1 gene (ARAF1)
Genomics
20
43-55
1994
Homo sapiens (P10398), Homo sapiens
Manually annotated by BRENDA team
Mark, G.E.; Seeley, T.W.; Shows, T.B.; Mountz, J.D.
Pks, a raf-related sequence in humans
Proc. Natl. Acad. Sci. USA
83
6312-6316
1986
Homo sapiens (P10398)
Manually annotated by BRENDA team
Sithanandam, G.; Kolch, W.; Duh, F.M.; Rapp, U.R.
Complete coding sequence of a human B-raf cDNA and detection of B-raf protein kinase with isozyme specific antibodies
Oncogene
5
1775-1780
1990
Homo sapiens (P15056)
Manually annotated by BRENDA team
Stephens, R.M.; Sithanandam, G.; Copeland, T.D.; Kaplan, D.R.; Rapp, U.R.; Morrison, D.K.
95-Kilodalton B-Raf serine/threonine kinase: identification of the protein and its major autophosphorylation site
Mol. Cell. Biol.
12
3733-3742
1992
Homo sapiens (P15056)
Manually annotated by BRENDA team
Stanger, B.Z.; Leder, P.; Lee, T.H.; Kim, E.; Seed, B.
RIP: a novel protein containing a death domain that interacts with Fas/APO-1 (CD95) in yeast and causes cell death
Cell
81
513-523
1995
Homo sapiens (Q13546), Mus musculus (Q60855)
Manually annotated by BRENDA team
Sun, X.; Lee, J.; Navas, T.; Baldwin, D.T.; Stewart, T.A.; Dixit, V.M.
RIP3, a novel apoptosis-inducing kinase
J. Biol. Chem.
274
16871-16875
1999
Homo sapiens (Q9Y572)
Manually annotated by BRENDA team
Yu, P.W.; Huang, B.C.; Shen, M.; Quast, J.; Chan, E.; Xu, X.; Nolan, G.P.; Payan, D.G.; Luo, Y.
Identification of RIP3, a RIP-like kinase that activates apoptosis and NFkappaB
Curr. Biol.
9
539-542
1999
Homo sapiens (Q9Y572)
Manually annotated by BRENDA team
Watanabe, N.; Broome, M.; Hunter, T.
Regulation of the human WEE1Hu CDK tyrosine 15-kinase during the cell cycle
EMBO J.
14
1878-1891
1995
Homo sapiens (P30291), Homo sapiens
Manually annotated by BRENDA team
McGowan, C.H.; Russell, P.
Human Wee1 kinase inhibits cell division by phosphorylating p34cdc2 exclusively on Tyr15
EMBO J.
12
75-85
1993
Homo sapiens (P30291)
Manually annotated by BRENDA team
Igarashi, M.; Nagata, A.; Jinno, S.; Suto, K.; Okayama, H.
Wee1(+)-like gene in human cells
Nature
353
80-83
1991
Homo sapiens (P30291), Homo sapiens
Manually annotated by BRENDA team
Roskoski, R.Jr.
Src protein-tyrosine kinase structure and regulation
Biochem. Biophys. Res. Commun.
324
1155-1164
2004
Gallus gallus, Homo sapiens, Rous sarcoma virus
Manually annotated by BRENDA team
Bain, J.; McLauchlan, H.; Elliott, M.; Cohen, P.
The specificities of protein kinase inhibitors: an update
Biochem. J.
371
199-204
2003
Homo sapiens
Manually annotated by BRENDA team
Piccardoni, P.; Manarini, S.; Federico, L.; Bagoly, Z.; Pecce, R.; Martelli, N.; Piccoli, A.; Totani, L.; Cerletti, C.; Evangelista, V.
SRC-dependent outside-in signalling is a key step in the process of autoregulation of beta2 integrins in polymorphonuclear cells
Biochem. J.
380
57-65
2004
Homo sapiens
Manually annotated by BRENDA team
Takashima, Y.; Delfino, F.J.; Engen, J.R.; Superti-Furga, G.; Smithgall, T.E.
Regulation of c-Fes tyrosine kinase activity by coiled-coil and SH2 domains: analysis with Saccharomyces cerevisiae
Biochemistry
42
3567-3574
2003
Homo sapiens
Manually annotated by BRENDA team
Lin, X.; Ayrapetov, M.K.; Lee, S.; Parang, K.; Sun, G.
Probing the communication between the regulatory and catalytic domains of a protein tyrosine kinase, Csk
Biochemistry
44
1561-1567
2005
Homo sapiens
Manually annotated by BRENDA team
Nore, B.F.; Mattsson, P.T.; Antonsson, P.; Backesjo, C.M.; Westlund, A.; Lennartsson, J.; Hansson, H.; Low, P.; Ronnstrand, L.; Smith, C.I.
Identification of phosphorylation sites within the SH3 domains of Tec family tyrosine kinases
Biochim. Biophys. Acta
1645
123-132
2003
Homo sapiens
Manually annotated by BRENDA team
Chong, Y.P.; Ia, K.K.; Mulhern, T.D.; Cheng, H.C.
Endogenous and synthetic inhibitors of the Src-family protein tyrosine kinases
Biochim. Biophys. Acta
1754
210-220
2005
Homo sapiens
Manually annotated by BRENDA team
Nam, N.H.; Lee, S.; Ye, G.; Sun, G.; Parang, K.
ATP-phosphopeptide conjugates as inhibitors of Src tyrosine kinases
Bioorg. Med. Chem.
12
5753-5766
2004
Homo sapiens (P12931)
Manually annotated by BRENDA team
Xu, J.; Sun, L.; Ghosh, I.; Xu, M.Q.
Western blot analysis of Src kinase assays using peptide substrates ligated to a carrier protein
Biotechniques
36; 976-978
980-971
2004
Homo sapiens
Manually annotated by BRENDA team
Lucet, I.S.; Fantino, E.; Styles, M.; Bamert, R.; Patel, O.; Broughton, S.E.; Walter, M.; Burns, C.J.; Treutlein, H.; Wilks, A.F.; Rossjohn, J.
The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor
Blood
107
176-183
2006
Homo sapiens
Manually annotated by BRENDA team
Lin, X.; Ayrapetov, M.K.; Sun, G.
Characterization of the interactions between the active site of a protein tyrosine kinase and a divalent metal activator
BMC Biochem.
6
25
2005
Homo sapiens
Manually annotated by BRENDA team
Ruschel, A.; Ullrich, A.
Protein tyrosine kinase Syk modulates EGFR signalling in human mammary epithelial cells
Cell. Signal.
16
1249-1261
2004
Homo sapiens
Manually annotated by BRENDA team
Backlund, M.; Ingelman-Sundberg, M.
Regulation of aryl hydrocarbon receptor signal transduction by protein tyrosine kinases
Cell. Signal.
17
39-48
2005
Homo sapiens
Manually annotated by BRENDA team
Clark, D.D.; Peterson, B.R.
Fluorescence-based cloning of a protein tyrosine kinase with a yeast tribrid system
ChemBioChem
6
1442-1448
2005
Homo sapiens
Manually annotated by BRENDA team
Hollosy, F.; Keri, G.
Plant-derived protein tyrosine kinase inhibitors as anticancer agents
Curr. Med. Chem. Anticancer Agents
4
173-197
2004
Homo sapiens
Manually annotated by BRENDA team
Anastasiadou, E.; Schwaller, J.
Role of constitutively activated protein tyrosine kinases in malignant myeloproliferative disorders: an update
Curr. Opin. Hematol.
10
40-48
2003
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Mikkola, E.T.; Bergman, M.
Conserved hydrophobicity in the SH2-kinase linker is required for catalytic activity of Csk and CHK
FEBS Lett.
544
11-14
2003
Homo sapiens
Manually annotated by BRENDA team
Grossmann, A.H.; Kolibaba, K.S.; Willis, S.G.; Corbin, A.S.; Langdon, W.S.; Deininger, M.W.; Druker, B.J.
Catalytic domains of tyrosine kinases determine the phosphorylation sites within c-Cbl
FEBS Lett.
577
555-562
2004
Homo sapiens
Manually annotated by BRENDA team
Lamant, L.; Gascoyne, R.D.; Duplantier, M.M.; Armstrong, F.; Raghab, A.; Chhanabhai, M.; Rajcan-Separovic, E.; Raghab, J.; Delsol, G.; Espinos, E.
Non-muscle myosin heavy chain (MYH9): a new partner fused to ALK in anaplastic large cell lymphoma
Genes Chromosomes Cancer
37
427-432
2003
Homo sapiens
Manually annotated by BRENDA team
Kim, J.; Ogata, Y.; Feldman, R.A.
Fes tyrosine kinase promotes survival and terminal granulocyte differentiation of factor-dependent myeloid progenitors (32D) and activates lineage-specific transcription factors
J. Biol. Chem.
278
14978-14984
2003
Homo sapiens
Manually annotated by BRENDA team
Lin, X.; Lee, S.; Sun, G.
Functions of the activation loop in Csk protein-tyrosine kinase
J. Biol. Chem.
278
24072-24077
2003
Homo sapiens
Manually annotated by BRENDA team
Crosby, D.; Poole, A.W.
Physical and functional interaction between protein kinase C delta and Fyn tyrosine kinase in human platelets
J. Biol. Chem.
278
24533-24541
2003
Homo sapiens
Manually annotated by BRENDA team
Mahabeleshwar, G.H.; Kundu, G.C.
Tyrosine kinase p56lck regulates cell motility and nuclear factor kappaB-mediated secretion of urokinase type plasminogen activator through tyrosine phosphorylation of IkappaBalpha following hypoxia/reoxygenation
J. Biol. Chem.
278
52598-52612
2003
Homo sapiens
Manually annotated by BRENDA team
Mahabeleshwar, G.H.; Kundu, G.C.
Syk, a protein-tyrosine kinase, suppresses the cell motility and nuclear factor kappa B-mediated secretion of urokinase type plasminogen activator by inhibiting the phosphatidylinositol 3'-kinase activity in breast cancer cells
J. Biol. Chem.
278
6209-6221
2003
Homo sapiens
Manually annotated by BRENDA team
Meyer, A.N.; Gastwirt, R.F.; Schlaepfer, D.D.; Donoghue, D.J.
The cytoplasmic tyrosine kinase Pyk2 as a novel effector of fibroblast growth factor receptor 3 activation
J. Biol. Chem.
279
28450-28457
2004
Homo sapiens
Manually annotated by BRENDA team
Du, X.L.; Gao, Z.; Lau, C.P.; Chiu, S.W.; Tse, H.F.; Baumgarten, C.M.; Li, G.R.
Differential effects of tyrosine kinase inhibitors on volume-sensitive chloride current in human atrial myocytes: evidence for dual regulation by Src and EGFR kinases
J. Gen. Physiol.
123
427-439
2004
Homo sapiens
Manually annotated by BRENDA team
Kim, H.Y.; Park, E.J.; Joe, E.H.; Jou, I.
Curcumin suppresses Janus kinase-STAT inflammatory signaling through activation of Src homology 2 domain-containing tyrosine phosphatase 2 in brain microglia
J. Immunol.
171
6072-6079
2003
Homo sapiens
Manually annotated by BRENDA team
Puder, C.; Wagner, K.; Vettermann, R.; Hauptmann, R.; Potterat, O.
Terphenylquinone inhibitors of the Src protein tyrosine kinase from Stilbella sp
J. Nat. Prod.
68
323-326
2005
Homo sapiens
Manually annotated by BRENDA team
Calvert-Evers, J.L.; Hammond, K.D.
Temporal variations in protein tyrosine kinase activity in leukaemic cells: response to all-trans retinoic acid
Mol. Cell. Biochem.
245
23-30
2003
Homo sapiens
Manually annotated by BRENDA team
Laurent, C.E.; Delfino, F.J.; Cheng, H.Y.; Smithgall, T.E.
The human c-Fes tyrosine kinase binds tubulin and microtubules through separate domains and promotes microtubule assembly
Mol. Cell. Biol.
24
9351-9358
2004
Homo sapiens
Manually annotated by BRENDA team
Brdicka, T.; Kadlecek, T.A.; Roose, J.P.; Pastuszak, A.W.; Weiss, A.
Intramolecular regulatory switch in ZAP-70: analogy with receptor tyrosine kinases
Mol. Cell. Biol.
25
4924-4933
2005
Homo sapiens
Manually annotated by BRENDA team
Merciris, P.; Claussen, W.J.; Joiner, C.H.; Giraud, F.
Regulation of K-Cl cotransport by Syk and Src protein tyrosine kinases in deoxygenated sickle cells
Pflugers Arch.
446
232-238
2003
Homo sapiens
Manually annotated by BRENDA team
Lee, S.; Lin, X.; Nam, N.H.; Parang, K.; Sun, G.
Determination of the substrate-docking site of protein tyrosine kinase C-terminal Src kinase
Proc. Natl. Acad. Sci. USA
100
14707-14712
2003
Homo sapiens
Manually annotated by BRENDA team
Ayrapetov, M.K.; Lee, S.; Sun, G.
Expression, purification, and biochemical characterization of Chk, a soluble protein tyrosine kinase
Protein Expr. Purif.
29
148-155
2003
Homo sapiens
Manually annotated by BRENDA team
Ovrevik, J.; Lag, M.; Schwarze, P.; Refsnes, M.
p38 and Src-ERK1/2 pathways regulate crystalline silica-induced chemokine release in pulmonary epithelial cells
Toxicol. Sci.
81
480-490
2004
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Gnemmi, I.; Scotti, C.; Cappelletti, D.; Canonico, P.L.; Condorelli, F.; Rosano, C.
Expression, purification and preliminary crystallographic studies on the catalytic region of the nonreceptor tyrosine kinase Fes
Acta Crystallogr. Sect. F
63
18-20
2007
Homo sapiens (P07332)
Manually annotated by BRENDA team
Kasprzycka, M.; Majewski, M.; Wang, Z.J.; Ptasznik, A.; Wysocka, M.; Zhang, Q.; Marzec, M.; Gimotty, P.; Crompton, M.R.; Wasik, M.A.
Expression and oncogenic role of Brk (PTK6/Sik) protein tyrosine kinase in lymphocytes
Am. J. Pathol.
168
1631-1641
2006
Homo sapiens
Manually annotated by BRENDA team
Okutani, D.; Lodyga, M.; Han, B.; Liu, M.
Src protein tyrosine kinase family and acute inflammatory responses
Am. J. Physiol. Lung Cell Mol. Physiol.
291
L129-L141
2006
Homo sapiens, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Kemble, D.J.; Wang, Y.H.; Sun, G.
Bacterial expression and characterization of catalytic loop mutants of SRC protein tyrosine kinase
Biochemistry
45
14749-14754
2006
Homo sapiens
Manually annotated by BRENDA team
Shi, Y.; Tohyama, Y.; Kadono, T.; He, J.; Shahjahan Miah, S.M.; Hazama, R.; Tanaka, C.; Tohyama, K.; Yamamura, H.
Protein-tyrosine kinase Syk is required for pathogen engulfment in complement-mediated phagocytosis
Blood
107
4554-4562
2006
Homo sapiens
Manually annotated by BRENDA team
Cortes, J.; Jabbour, E.; Kantarjian, H.; Yin, C.C.; Shan, J.; Obrien, S.; Garcia-Manero, G.; Giles, F.; Breeden, M.; Reeves, N.; Wierda, W.G.; Jones, D.
Dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors
Blood
110
4005-4011
2007
Homo sapiens (P00519), Homo sapiens
Manually annotated by BRENDA team
Wallace, T.A.; Sayeski, P.P.
Jak2 tyrosine kinase: a mediator of both housekeeping and ligand-dependent gene expression?
Cell Biochem. Biophys.
44
213-222
2006
Drosophila melanogaster, Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Tang, X.; Feng, Y.; Ye, K.
Src-family tyrosine kinase fyn phosphorylates phosphatidylinositol 3-kinase enhancer-activating Akt, preventing its apoptotic cleavage and promoting cell survival
Cell Death Differ.
14
368-377
2007
Homo sapiens
Manually annotated by BRENDA team
Hu, X.; Dang, Y.; Tenney, K.; Crews, P.; Tsai, C.W.; Sixt, K.M.; Cole, P.A.; Liu, J.O.
Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases
Chem. Biol.
14
764-774
2007
Homo sapiens
Manually annotated by BRENDA team
Angelucci, A.; Bologna, M.
Targeting vascular cell migration as a strategy for blocking angiogenesis: the central role of focal adhesion protein tyrosine kinase family
Curr. Pharm. Des.
13
2129-2145
2007
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Ortolano, S.; Hwang, I.Y.; Han, S.B.; Kehrl, J.H.
Roles for phosphoinositide 3-kinases, Brutons tyrosine kinase, and Jun kinases in B lymphocyte chemotaxis and homing
Eur. J. Immunol.
36
1285-1295
2006
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Nakayama, Y.; Kawana, A.; Igarashi, A.; Yamaguchi, N.
Involvement of the N-terminal unique domain of Chk tyrosine kinase in Chk-induced tyrosine phosphorylation in the nucleus
Exp. Cell Res.
312
2252-2263
2006
Homo sapiens
Manually annotated by BRENDA team
Xu, D.; Kishi, H.; Kawamichi, H.; Kajiya, K.; Takada, Y.; Kobayashi, S.
Involvement of Fyn tyrosine kinase in actin stress fiber formation in fibroblasts
FEBS Lett.
581
5227-5233
2007
Homo sapiens
Manually annotated by BRENDA team
Nguyen, J.; Gogusev, J.; Knapnougel, P.; Bauvois, B.
Protein tyrosine kinase and p38 MAP kinase pathways are involved in stimulation of matrix metalloproteinase-9 by TNF-alpha in human monocytes
Immunol. Lett.
106
34-41
2006
Homo sapiens
Manually annotated by BRENDA team
Tauchi, T.; Ohyashiki, K.
The second generation of BCR-ABL tyrosine kinase inhibitors
Int. J. Hematol.
83
294-300
2006
Homo sapiens
Manually annotated by BRENDA team
Jing, Y.; Wang, M.; Tang, W.; Qi, T.; Gu, C.; Hao, S.; Zeng, X.
c-Abl tyrosine kinase activates p21 transcription via interaction with p53
J. Biochem.
141
621-626
2007
Homo sapiens
Manually annotated by BRENDA team
Liu, H.; Nakazawa, T.; Tezuka, T.; Yamamoto, T.
Physical and functional interaction of Fyn tyrosine kinase with a brain-enriched Rho GTPase-activating protein TCGAP
J. Biol. Chem.
281
23611-23619
2006
Homo sapiens
Manually annotated by BRENDA team
Tanos, B.; Pendergast, A.M.
Abl tyrosine kinase regulates endocytosis of the epidermal growth factor receptor
J. Biol. Chem.
281
32714-32723
2006
Homo sapiens
Manually annotated by BRENDA team
Chong, Y.P.; Chan, A.S.; Chan, K.C.; Williamson, N.A.; Lerner, E.C.; Smithgall, T.E.; Bjorge, J.D.; Fujita, D.J.; Purcell, A.W.; Scholz, G.; Mulhern, T.D.; Cheng, H.C.
C-terminal Src kinase-homologous kinase (CHK), a unique inhibitor inactivating multiple active conformations of Src family tyrosine kinases
J. Biol. Chem.
281
32988-32999
2006
Homo sapiens
Manually annotated by BRENDA team
Lee, S.; Ayrapetov, M.K.; Kemble, D.J.; Parang, K.; Sun, G.
Docking-based substrate recognition by the catalytic domain of a protein tyrosine kinase, C-terminal Src kinase (Csk)
J. Biol. Chem.
281
8183-8189
2006
Homo sapiens
Manually annotated by BRENDA team
Rider, L.; Shatrova, A.; Feener, E.P.; Webb, L.; Diakonova, M.
JAK2 tyrosine kinase phosphorylates PAK1 and regulates PAK1 activity and functions
J. Biol. Chem.
282
30985-30996
2007
Homo sapiens
Manually annotated by BRENDA team
Doyle, S.L.; Jefferies, C.A.; Feighery, C.; Oneill, L.A.
Signaling by Toll-like receptors -8 and -9 requires Brutons tyrosine kinase
J. Biol. Chem.
282
36953-36960
2007
Homo sapiens
Manually annotated by BRENDA team
Dinh, M.; Grunberger, D.; Ho, H.; Tsing, S.Y.; Shaw, D.; Lee, S.; Barnett, J.; Hill, R.J.; Swinney, D.C.; Bradshaw, J.M.
Activation mechanism and steady state kinetics of Brutons tyrosine kinase
J. Biol. Chem.
282
8768-8776
2007
Homo sapiens
Manually annotated by BRENDA team
Ulanova, M.; Asfaha, S.; Stenton, G.; Lint, A.; Gilbertson, D.; Schreiber, A.; Befus, D.
Involvement of Syk protein tyrosine kinase in LPS-induced responses in macrophages
J. Endotoxin Res.
13
117-125
2007
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Gururajan, M.; Dasu, T.; Shahidain, S.; Jennings, C.D.; Robertson, D.A.; Rangnekar, V.M.; Bondada, S.
Spleen tyrosine kinase (Syk), a novel target of curcumin, is required for B lymphoma growth
J. Immunol.
178
111-121
2007
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Beacham, D.; Ahn, M.; Catterall, W.A.; Scheuer, T.
Sites and molecular mechanisms of modulation of Na(V)1.2 channels by Fyn tyrosine kinase
J. Neurosci.
27
11543-11551
2007
Homo sapiens
Manually annotated by BRENDA team
Szigligeti, P.; Neumeier, L.; Duke, E.; Chougnet, C.; Takimoto, K.; Lee, S.M.; Filipovich, A.H.; Conforti, L.
Signalling during hypoxia in human T lymphocytes - critical role of the src protein tyrosine kinase p56Lck in the O2 sensitivity of Kv1.3 channels
J. Physiol.
573
357-370
2006
Homo sapiens
Manually annotated by BRENDA team
Nagar, B.; Hantschel, O.; Seeliger, M.; Davies, J.M.; Weis, W.I.; Superti-Furga, G.; Kuriyan, J.
Organization of the SH3-SH2 unit in active and inactive forms of the c-Abl tyrosine kinase
Mol. Cell
21
787-798
2006
Homo sapiens
Manually annotated by BRENDA team
Lopez-Herrera, G.; Berron-Ruiz, L.; Mogica-Martinez, D.; Espinosa-Rosales, F.; Santos-Argumedo, L.
Characterization of Brutons tyrosine kinase mutations in Mexican patients with X-linked agammaglobulinemia
Mol. Immunol.
45
1094-1098
2007
Homo sapiens, Homo sapiens (Q06187)
Manually annotated by BRENDA team
Sirvent, A.; Boureux, A.; Simon, V.; Leroy, C.; Roche, S.
The tyrosine kinase Abl is required for Src-transforming activity in mouse fibroblasts and human breast cancer cells
Oncogene
26
7313-7323
2007
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Hantschel, O.; Rix, U.; Schmidt, U.; Buerckstuemmer, T.; Kneidinger, M.; Schuetze, G.; Colinge, J.; Bennett, K.L.; Ellmeier, W.; Valent, P.; Superti-Furga, G.
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib
Proc. Natl. Acad. Sci. USA
104
13283-13288
2007
Homo sapiens
Manually annotated by BRENDA team
Yu, J.H.; Wang, H.J.; Li, X.R.; Tashiro, S.; Onodera, S.; Ikejima, T.
Protein tyrosine kinase, JNK, and ERK involvement in pseudolaric acid B-induced apoptosis of human breast cancer MCF-7 cells
Acta Pharmacol. Sin.
29
1069-1076
2008
Homo sapiens
Manually annotated by BRENDA team
Li, C.H.; Zhang, Q.; Teng, B.; Mustafa, S.J.; Huang, J.Y.; Yu, H.G.
Src tyrosine kinase alters gating of hyperpolarization-activated HCN4 pacemaker channel through Tyr531
Am. J. Physiol. Cell Physiol.
294
C355-C362
2008
Mus musculus, Homo sapiens (P12931)
Manually annotated by BRENDA team
Jeulin, C.; Seltzer, V.; Bailbe, D.; Andreau, K.; Marano, F.
EGF mediates calcium-activated chloride channel activation in the human bronchial epithelial cell line 16HBE14o-: involvement of tyrosine kinase p60c-src
Am. J. Physiol. Lung Cell Mol. Physiol.
295
L489-L496
2008
Homo sapiens
Manually annotated by BRENDA team
Li, M.; Luraghi, P.; Amour, A.; Qian, X.D.; Carter, P.S.; Clark, C.J.; Deakin, A.; Denyer, J.; Hobbs, C.I.; Surby, M.; Patel, V.K.; Schaefer, E.M.
Kinetic assay for characterization of spleen tyrosine kinase activity and inhibition with recombinant kinase and crude cell lysates
Anal. Biochem.
384
56-67
2009
Homo sapiens
Manually annotated by BRENDA team
Murayama, K.; Kato-Murayama, M.; Mishima, C.; Akasaka, R.; Shirouzu, M.; Fukui, Y.; Yokoyama, S.
Crystal structure of the Brutons tyrosine kinase PH domain with phosphatidylinositol
Biochem. Biophys. Res. Commun.
377
23-28
2008
Homo sapiens (Q06187)
Manually annotated by BRENDA team
Xiong, X.; Cui, P.; Hossain, S.; Xu, R.; Warner, B.; Guo, X.; An, X.; Debnath, A.K.; Cowburn, D.; Kotula, L.
Allosteric inhibition of the nonMyristoylated c-Abl tyrosine kinase by phosphopeptides derived from Abi1/Hssh3bp1
Biochim. Biophys. Acta
1783
737-747
2008
Homo sapiens
Manually annotated by BRENDA team
Sirvent, A.; Benistant, C.; Roche, S.
Cytoplasmic signalling by the c-Abl tyrosine kinase in normal and cancer cells
Biol. Cell.
100
617-631
2008
Homo sapiens
Manually annotated by BRENDA team
Radi, M.; Crespan, E.; Botta, G.; Falchi, F.; Maga, G.; Manetti, F.; Corradi, V.; Mancini, M.; Santucci, M.A.; Schenone, S.; Botta, M.
Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents
Bioorg. Med. Chem. Lett.
18
1207-1211
2008
Homo sapiens (P00519), Homo sapiens
Manually annotated by BRENDA team
Wang, Y.; Shakespeare, W.C.; Huang, W.S.; Sundaramoorthi, R.; Lentini, S.; Das, S.; Liu, S.; Banda, G.; Wen, D.; Zhu, X.; Xu, Q.; Keats, J.; Wang, F.; Wardwell, S.; Ning, Y.; Snodgrass, J.T.; Broudy, M.I.; Russian, K.; Dalgarno, D.; Clackson, T.; Sawyer, T.K.
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors
Bioorg. Med. Chem. Lett.
18
4907-4912
2008
Homo sapiens, Homo sapiens (P12931)
Manually annotated by BRENDA team
Farmer, L.J.; Bemis, G.; Britt, S.D.; Cochran, J.; Connors, M.; Harrington, E.M.; Hoock, T.; Markland, W.; Nanthakumar, S.; Taslimi, P.; Haar, E.T.; Wang, J.; Zhaveri, D.; Salituro, F.G.
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK)
Bioorg. Med. Chem. Lett.
18
6231-6235
2008
Homo sapiens
Manually annotated by BRENDA team
Palmer, C.D.; Mutch, B.E.; Workman, S.; McDaid, J.P.; Horwood, N.J.; Foxwell, B.M.
Bmx tyrosine kinase regulates TLR4-induced IL-6 production in human macrophages independently of p38 MAPK and NFkappaB activity
Blood
111
1781-1788
2008
Homo sapiens, Homo sapiens (P51813)
Manually annotated by BRENDA team
Huang, Y.; Comiskey, E.O.; Dupree, R.S.; Li, S.; Koleske, A.J.; Burkhardt, J.K.
The c-Abl tyrosine kinase regulates actin remodeling at the immune synapse
Blood
112
111-119
2008
Homo sapiens
Manually annotated by BRENDA team
Aubele, M.; Walch, A.K.; Ludyga, N.; Braselmann, H.; Atkinson, M.J.; Luber, B.; Auer, G.; Tapio, S.; Cooke, T.; Bartlett, J.M.
Prognostic value of protein tyrosine kinase 6 (PTK6) for long-term survival of breast cancer patients
Br. J. Cancer
99
1089-1095
2008
Homo sapiens (Q13882), Homo sapiens
Manually annotated by BRENDA team
Sun, C.K.; Man, K.; Ng, K.T.; Ho, J.W.; Lim, Z.X.; Cheng, Q.; Lo, C.M.; Poon, R.T.; Fan, S.T.
Proline-rich tyrosine kinase 2 (Pyk2) promotes proliferation and invasiveness of hepatocellular carcinoma cells through c-Src/ERK activation
Carcinogenesis
29
2096-2105
2008
Homo sapiens
Manually annotated by BRENDA team
Perez de Diego, R.; Lopez-Granados, E.; Rivera, J.; Ferreira, A.; Fontan, G.; Bravo, J.; Garcia Rodriguez, M.C.; Bolland, S.
Naturally occurring Brutons tyrosine kinase mutations have no dominant negative effect in an X-linked agammaglobulinaemia cellular model
Clin. Exp. Immunol.
152
33-38
2008
Homo sapiens (Q06187), Homo sapiens
Manually annotated by BRENDA team
Ikeda, K.; Nakayama, Y.; Togashi, Y.; Obata, Y.; Kuga, T.; Kasahara, K.; Fukumoto, Y.; Yamaguchi, N.
Nuclear localization of Lyn tyrosine kinase mediated by inhibition of its kinase activity
Exp. Cell Res.
314
3392-3404
2008
Homo sapiens (P07948)
Manually annotated by BRENDA team
Shimizu, A.; Mammoto, A.; Italiano, J.E.; Pravda, E.; Dudley, A.C.; Ingber, D.E.; Klagsbrun, M.
ABL2/ARG tyrosine kinase mediates SEMA3F-induced RhoA inactivation and cytoskeleton collapse in human glioma cells
J. Biol. Chem.
283
27230-27238
2008
Homo sapiens
Manually annotated by BRENDA team
Agrawal, R.; Carpino, N.; Tsygankov, A.
TULA proteins regulate activity of the protein tyrosine kinase Syk
J. Cell. Biochem.
104
953-964
2008
Homo sapiens
Manually annotated by BRENDA team
Semaan, N.; Alsaleh, G.; Gottenberg, J.E.; Wachsmann, D.; Sibilia, J.
Etk/BMX, a Btk family tyrosine kinase, and Mal contribute to the cross-talk between MyD88 and FAK pathways
J. Immunol.
180
3485-3491
2008
Homo sapiens (P51813)
Manually annotated by BRENDA team
Anand, A.R.; Cucchiarini, M.; Terwilliger, E.F.; Ganju, R.K.
The tyrosine kinase Pyk2 mediates lipopolysaccharide-induced IL-8 expression in human endothelial cells
J. Immunol.
180
5636-5644
2008
Homo sapiens
Manually annotated by BRENDA team
Lin, L.G.; Xie, H.; Li, H.L.; Tong, L.J.; Tang, C.P.; Ke, C.Q.; Liu, Q.F.; Lin, L.P.; Geng, M.Y.; Jiang, H.; Zhao, W.M.; Ding, J.; Ye, Y.
Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening
J. Med. Chem.
51
4419-4429
2008
Homo sapiens (P12931)
Manually annotated by BRENDA team
Amanchy, R.; Zhong, J.; Molina, H.; Chaerkady, R.; Iwahori, A.; Kalume, D.E.; Gr?nborg, M.; Joore, J.; Cope, L.; Pandey, A.
Identification of c-Src tyrosine kinase substrates using mass spectrometry and peptide microarrays
J. Proteome Res.
7
3900-3910
2008
Homo sapiens
Manually annotated by BRENDA team
Gianni, D.; Bohl, B.; Courtneidge, S.A.; Bokoch, G.M.
The involvement of the tyrosine kinase c-Src in the regulation of reactive oxygen species generation mediated by NADPH oxidase-1
Mol. Biol. Cell
19
2984-2994
2008
Homo sapiens
Manually annotated by BRENDA team
Parsa, K.V.; Butchar, J.P.; Rajaram, M.V.; Cremer, T.J.; Tridandapani, S.
The tyrosine kinase Syk promotes phagocytosis of Francisella through the activation of Erk
Mol. Immunol.
45
3012-3021
2008
Mus musculus, Homo sapiens (P43405)
Manually annotated by BRENDA team
Lin, J.; Arlinghaus, R.
Activated c-Abl tyrosine kinase in malignant solid tumors
Oncogene
27
4385-4391
2008
Homo sapiens
Manually annotated by BRENDA team
Sandilands, E.; Frame, M.C.
Endosomal trafficking of Src tyrosine kinase
Trends Cell Biol.
18
322-329
2008
Homo sapiens
Manually annotated by BRENDA team
Busque, S.; Leventhal, J.; Brennan, D.C.; Steinberg, S.; Klintmalm, G.; Shah, T.; Mulgaonkar, S.; Bromberg, J.S.; Vincenti, F.; Hariharan, S.; Slakey, D.; Peddi, V.R.; Fisher, R.A.; Lawendy, N.; Wang, C.; Chan, G.
Calcineurin-inhibitor-free immunosuppression based on the JAK inhibitor CP-690,550: a pilot study in de novo kidney allograft recipients
Am. J. Transplant.
9
1936-1945
2009
Homo sapiens
Manually annotated by BRENDA team
Coaxum, S.D.; Garnovskaya, M.N.; Gooz, M.; Baldys, A.; Raymond, J.R.
Epidermal growth factor activates Na(+/)H(+) exchanger in podocytes through a mechanism that involves Janus kinase and calmodulin
Biochim. Biophys. Acta
1793
1174-1181
2009
Homo sapiens
Manually annotated by BRENDA team
Jedidi, A.; Marty, C.; Oligo, C.; Jeanson-Leh, L.; Ribeil, J.A.; Casadevall, N.; Galy, A.; Vainchenker, W.; Villeval, J.L.
Selective reduction of JAK2V617F-dependent cell growth by siRNA/shRNA and its reversal by cytokines
Blood
114
1842-1851
2009
Homo sapiens (O60674), Homo sapiens
Manually annotated by BRENDA team
Wang, Y.; Fiskus, W.; Chong, D.G.; Buckley, K.M.; Natarajan, K.; Rao, R.; Joshi, A.; Balusu, R.; Koul, S.; Chen, J.; Savoie, A.; Ustun, C.; Jillella, A.P.; Atadja, P.; Levine, R.L.; Bhalla, K.N.
Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells
Blood
114
5024-5033
2009
Homo sapiens (O60674), Homo sapiens
Manually annotated by BRENDA team
Yoo, J.H.; Park, T.S.; Maeng, H.Y.; Sun, Y.K.; Kim, Y.A.; Kie, J.H.; Cho, E.H.; Song, J.; Lee, K.A.; Suh, B.; Choi, J.R.
JAK2 V617F/C618R mutation in a patient with polycythemia vera: a case study and review of the literature
Cancer Genet. Cytogenet.
189
43-47
2009
Homo sapiens (O60674), Homo sapiens
Manually annotated by BRENDA team
Apostolidou, E.; Kantarjian, H.M.; Verstovsek, S.
JAK2 inhibitors: A reality? A hope?
Clin. Lymphoma Myeloma
9
S340-S345
2009
Homo sapiens (O60674), Homo sapiens
Manually annotated by BRENDA team
de Heer, P.; Koudijs, M.M.; van de Velde, C.J.; Aalbers, R.I.; Tollenaar, R.A.; Putter, H.; Morreau, J.; van de Water, B.; Kuppen, P.J.
Combined expression of the non-receptor protein tyrosine kinases FAK and Src in primary colorectal cancer is associated with tumor recurrence and metastasis formation
Eur. J. Surg. Oncol.
34
1253-1261
2008
Homo sapiens
Manually annotated by BRENDA team
Pesu, M.; Laurence, A.; Kishore, N.; Zwillich, S.H.; Chan, G.; OShea, J.J.
Therapeutic targeting of Janus kinases
Immunol. Rev.
223
132-142
2008
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Ghoreschi, K.; Laurence, A.; OShea, J.J.
Janus kinases in immune cell signaling
Immunol. Rev.
228
273-287
2009
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Lee, W.H.; Liu, F.H.; Lin, J.Y.; Huang, S.Y.; Lin, H.; Liao, W.J.; Huang, H.M.
JAK pathway induction of c-Myc critical to IL-5 stimulation of cell proliferation and inhibition of apoptosis
J. Cell. Biochem.
106
929-936
2009
Homo sapiens
Manually annotated by BRENDA team
Walz, C.; Cross, N.C.; Van Etten, R.A.; Reiter, A.
Comparison of mutated ABL1 and JAK2 as oncogenes and drug targets in myeloproliferative disorders
Leukemia
22
1320-1334
2008
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Lipka, D.B.; Hoffmann, L.S.; Heidel, F.; Markova, B.; Blum, M.C.; Breitenbuecher, F.; Kasper, S.; Kindler, T.; Levine, R.L.; Huber, C.; Fischer, T.
LS104, a non-ATP-competitive small-molecule inhibitor of JAK2, is potently inducing apoptosis in JAK2V617F-positive cells
Mol. Cancer Ther.
7
1176-1184
2008
Homo sapiens (O60674)
Manually annotated by BRENDA team
Burger, R.; Le Gouill, S.; Tai, Y.T.; Shringarpure, R.; Tassone, P.; Neri, P.; Podar, K.; Catley, L.; Hideshima, T.; Chauhan, D.; Caulder, E.; Neilan, C.L.; Vaddi, K.; Li, J.; Gramatzki, M.; Fridman, J.S.; Anderson, K.C.
Janus kinase inhibitor INCB20 has antiproliferative and apoptotic effects on human myeloma cells in vitro and in vivo
Mol. Cancer Ther.
8
26-35
2009
Homo sapiens
Manually annotated by BRENDA team
Li, J.; Favata, M.; Kelley, J.A.; Caulder, E.; Thomas, B.; Wen, X.; Sparks, R.B.; Arvanitis, A.; Rogers, J.D.; Combs, A.P.; Vaddi, K.; Solomon, K.A.; Scherle, P.A.; Newton, R.; Fridman, J.S.
INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support
Neoplasia
12
28-38
2010
Homo sapiens
Manually annotated by BRENDA team
Monroe, R.K.; Halvorsen, S.W.
Environmental toxicants inhibit neuronal Jak tyrosine kinase by mitochondrial disruption
Neurotoxicology
30
589-598
2009
Homo sapiens
Manually annotated by BRENDA team
Yamaoka, K.; Tanaka, Y.
Jak inhibitor: possibility and mechanism as a new disease modifying anti-rheumatic drug
Nihon Rinsho Meneki Gakkai Kaishi
32
85-91
2009
Homo sapiens
Manually annotated by BRENDA team
Barua, D.; Faeder, J.R.; Haugh, J.M.
A bipolar clamp mechanism for activation of Jak-family protein tyrosine kinases
PLoS Comput. Biol.
5
e1000364
2009
Homo sapiens
Manually annotated by BRENDA team
Wilks, A.F.
The JAK kinases: not just another kinase drug discovery target
Semin. Cell Dev. Biol.
19
319-328
2008
Homo sapiens
Manually annotated by BRENDA team
Vainchenker, W.; Dusa, A.; Constantinescu, S.N.
JAKs in pathology: role of Janus kinases in hematopoietic malignancies and immunodeficiencies
Semin. Cell Dev. Biol.
19
385-393
2008
Homo sapiens
Manually annotated by BRENDA team
Constantinescu, S.N.; Girardot, M.; Pecquet, C.
Mining for JAK-STAT mutations in cancer
Trends Biochem. Sci.
33
122-131
2008
Homo sapiens (O60674)
Manually annotated by BRENDA team
Kim, R.K.; Yoon, C.H.; Hyun, K.H.; Lee, H.; An, S.; Park, M.J.; Kim, M.J.; Lee, S.J.
Role of lymphocyte-specific protein tyrosine kinase (LCK) in the expansion of glioma-initiating cells by fractionated radiation
Biochem. Biophys. Res. Commun.
402
631-636
2010
Homo sapiens
Manually annotated by BRENDA team
Lin, Q.; Wang, J.; Childress, C.; Yang, W.
The activation mechanism of ACK1 (activated Cdc42-associated tyrosine kinase 1)
Biochem. J.
445
255-264
2012
Homo sapiens (Q07912)
Manually annotated by BRENDA team
Yang, X.; Kinoshita, T.; Gouda, M.; Yokota, K.; Tada, T.
A silent mutation made possible efficient production of active human Frk tyrosine kinase in Escherichia coli
Biosci. Biotechnol. Biochem.
74
125-128
2010
Homo sapiens (P42685), Homo sapiens
Manually annotated by BRENDA team
Fei, F.; Kweon, S.; Haataja, L.; De Sepulveda, P.; Groffen, J.; Heisterkamp, N.
The Fer tyrosine kinase regulates interactions of Rho GDP-dissociation inhibitor alpha with the small GTPase Rac
BMC Biochem.
11
48
2010
Homo sapiens (P16591)
Manually annotated by BRENDA team
Chan, W.; Wise, S.; Kaufman, M.; Ahn, Y.; Ensinger, C.; Haack, T.; Hood, M.; Jones, J.; Lord, J.; Lu, W.; Miller, D.; Patt, W.; Smith, B.; Petillo, P.; Rutkoski, T.; Telikepalli, H.; Vogeti, L.; Yao, T.; Chun, L.; Clark, R.; Evangelista, P.; Gavrilescu, L
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036
Cancer Cell
19
556-568
2011
Homo sapiens (P00519), Homo sapiens
Manually annotated by BRENDA team
Deng, Y.; Couch, B.; Koleske, A.; Turk, B.
A Peptide photoaffinity probe specific for the active conformation of the Abl tyrosine kinase
ChemBioChem
13
2510-2512
2012
Homo sapiens
Manually annotated by BRENDA team
Lysechko, T.L.; Cheung, S.M.; Ostergaard, H.L.
Regulation of the tyrosine kinase Pyk2 by calcium is through production of reactive oxygen species in cytotoxic T lymphocytes
J. Biol. Chem.
285
31174-31184
2010
Homo sapiens (Q14289)
Manually annotated by BRENDA team
Bao, Y.; Zheng, J.; Han, C.; Jin, J.; Han, H.; Liu, Y.; Lau, Y.; Tu, W.; Cao, X.
Tyrosine kinase Btk is required for NK cell activation
J. Biol. Chem.
287
23769-23778
2012
Mus musculus (P35991), Mus musculus, Homo sapiens (Q06187), Homo sapiens
Manually annotated by BRENDA team
Tong, H.; Zhao, B.; Shi, H.; Ba, X.; Wang, X.; Jiang, Y.; Zeng, X.
c-Abl tyrosine kinase plays a critical role in beta2 integrin-dependent neutrophil migration by regulating Vav1 activity
J. Leukoc. Biol.
93
611-622
2013
Homo sapiens
Manually annotated by BRENDA team
Moody, T.W.; Di Florio, A.; Jensen, R.T.
PYK-2 is tyrosine phosphorylated after activation of pituitary adenylate cyclase activating polypeptide receptors in lung cancer cells
J. Mol. Neurosci.
48
660-666
2012
Homo sapiens (Q14289)
Manually annotated by BRENDA team
Hill, Z.B.; Perera, B.G.; Maly, D.J.
Bivalent inhibitors of the tyrosine kinases ABL and SRC: determinants of potency and selectivity
Mol. Biosyst.
7
447-456
2011
Homo sapiens (P00519), Homo sapiens (P12931)
Manually annotated by BRENDA team
He, X.; Zheng, Z.; Song, T.; Wei, C.; Ma, H.; Ma, Q.; Zhang, Y.; Xu, Y.; Shi, W.; Ye, Q.; Zhong, H.
c-Abl regulates estrogen receptor alpha transcription activity through its stabilization by phosphorylation
Oncogene
29
2238-2251
2010
Homo sapiens (P00519)
Manually annotated by BRENDA team
Harper, M.T.; Sage, S.O.
Src family tyrosine kinases activate thrombin-induced non-capacitative cation entry in human platelets
Platelets
21
445-450
2010
Homo sapiens
Manually annotated by BRENDA team
Kuka, M.; Baronio, R.; Valentini, S.; Monaci, E.; Muzzi, A.; Aprea, S.; De Gregorio, E.; DOro, U.
Src kinases are required for a balanced production of IL-12/IL-23 in human dendritic cells activated by Toll-like receptor agonists
PLoS ONE
5
e11491
2010
Homo sapiens
Manually annotated by BRENDA team
Sancier, F.; Dumont, A.; Sirvent, A.; Paquay de Plater, L.; Edmonds, T.; David, G.; Jan, M.; de Montrion, C.; Coge, F.; Leonce, S.; Burbridge, M.; Bruno, A.; Boutin, J.A.; Lockhart, B.; Roche, S.; Cruzalegui, F.
Specific oncogenic activity of the Src-family tyrosine kinase c-Yes in colon carcinoma cells
PLoS ONE
6
e17237
2011
Homo sapiens (P07947)
Manually annotated by BRENDA team
Levinson, N.; Boxer, S.
Structural and spectroscopic analysis of the kinase inhibitor bosutinib and an isomer of bosutinib binding to the Abl tyrosine kinase domain
PLoS ONE
7
e29828
2012
Homo sapiens (P00519)
Manually annotated by BRENDA team
Ma, Y.C.; Shi, C.; Zhang, Y.N.; Wang, L.G.; Liu, H.; Jia, H.T.; Zhang, Y.X.; Sarkar, F.H.; Wang, Z.S.
The tyrosine kinase c-Src directly mediates growth factor-induced Notch-1 and Furin interaction and Notch-1 activation in pancreatic cancer cells
PLoS ONE
7
e33414
2012
Homo sapiens
Manually annotated by BRENDA team
Marit, M.R.; Chohan, M.; Matthew, N.; Huang, K.; Kuntz, D.A.; Rose, D.R.; Barber, D.L.
Random mutagenesis reveals residues of JAK2 critical in evading inhibition by a tyrosine kinase inhibitor
PLoS ONE
7
e43437
2012
Homo sapiens
Manually annotated by BRENDA team
Ko, H.S.; Lee, Y.; Shin, J.H.; Karuppagounder, S.S.; Gadad, B.S.; Koleske, A.J.; Pletnikova, O.; Troncoso, J.C.; Dawson, V.L.; Dawson, T.M.
Phosphorylation by the c-Abl protein tyrosine kinase inhibits parkin's ubiquitination and protective function
Proc. Natl. Acad. Sci. USA
107
16691-16696
2010
Homo sapiens
Manually annotated by BRENDA team
Emmons, T.L.; Wrightstone, A.D.; Baima, E.T.; Brown, S.; Sommers, C.D.; Hirsch, J.L.; Pegg, L.E.; Weinberg, R.A.; Fischer, H.D.; Wittwer, A.J.; Tomasselli, A.G.
Differential kinetics and inhibition of purified recombinant tyrosine kinase 2 (TYK-2) and its catalytic domain JH-1
Protein Pept. Lett.
19
485-491
2012
Homo sapiens (P29597)
Manually annotated by BRENDA team
Marcotte, D.; Liu, Y.; Arduini, R.; Hession, C.; Miatkowski, K.; Wildes, C.; Cullen, P.; Hong, V.; Hopkins, B.; Mertsching, E.; Jenkins, T.; Romanowski, M.; Baker, D.; Silvian, L.
Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases
Protein Sci.
19
429-439
2010
Homo sapiens (Q06187), Homo sapiens
Manually annotated by BRENDA team
Hari, S.B.; Perera, B.G.; Ranjitkar, P.; Seeliger, M.A.; Maly, D.J.
Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src
ACS Chem. Biol.
8
2734-2743
2013
Homo sapiens
Manually annotated by BRENDA team
Badger, J.; Grover, P.; Shi, H.; Panjarian, S.B.; Engen, J.R.; Smithgall, T.E.; Makowski, L.
c-Abl tyrosine kinase adopts multiple active conformational states in solution
Biochemistry
55
3251-3260
2016
Homo sapiens (P00519)
Manually annotated by BRENDA team
Baldwin, G.S.; Lio, D.S.; Ferrand, A.; Catimel, B.; Shehan, B.P.; Norton, R.S.; Cheng, H.C.
Activation of Src family tyrosine kinases by ferric ions
Biochim. Biophys. Acta
1844
487-496
2014
Homo sapiens
Manually annotated by BRENDA team
Toubiana, J.; Rossi, A.L.; Belaidouni, N.; Grimaldi, D.; Pene, F.; Chafey, P.; Comba, B.; Camoin, L.; Bismuth, G.; Claessens, Y.E.; Mira, J.P.; Chiche, J.D.
Src-family-tyrosine kinase Lyn is critical for TLR2-mediated NF-kappaB activation through the PI 3-kinase signaling pathway
Innate Immun.
21
685-697
2015
Homo sapiens
Manually annotated by BRENDA team
Gelman, I.H.
Androgen receptor activation in castration-recurrent prostate cancer: the role of Src-family and Ack1 tyrosine kinases
Int. J. Biol. Sci.
10
620-626
2014
Homo sapiens
Manually annotated by BRENDA team
Lin, Y.L.; Roux, B.
Computational analysis of the binding specificity of Gleevec to Abl, c-Kit, Lck, and c-Src tyrosine kinases
J. Am. Chem. Soc.
135
14741-14753
2013
Mus musculus (P00520), Gallus gallus (P00523), Homo sapiens (P06239)
Manually annotated by BRENDA team
Wu, Y.; Span, L.M.; Nygren, P.; Zhu, H.; Moore, D.T.; Cheng, H.; Roder, H.; DeGrado, W.F.; Bennett, J.S.
The tyrosine kinase c-Src specifically binds to the active integrin alphaIIbbeta3 to initiate outside-in signaling in platelets
J. Biol. Chem.
290
15825-15834
2015
Homo sapiens
Manually annotated by BRENDA team
Reuven, N.; Adler, J.; Porat, Z.; Polonio-Vallon, T.; Hofmann, T.G.; Shaul, Y.
The tyrosine kinase c-Abl promotes homeodomain-interacting protein kinase 2 (HIPK2) accumulation and activation in response to DNA damage
J. Biol. Chem.
290
16478-16488
2015
Homo sapiens
Manually annotated by BRENDA team
Montresor, A.; Bolomini-Vittori, M.; Toffali, L.; Rossi, B.; Constantin, G.; Laudanna, C.
JAK tyrosine kinases promote hierarchical activation of Rho and Rap modules of integrin activation
J. Cell Biol.
203
1003-1019
2013
Homo sapiens
Manually annotated by BRENDA team
Mizuguchi, Y.; Specht, S.; Isse, K.; Sasatomi, E.; Lunz, J.G.; Takizawa, T.; Demetris, A.J.
Breast tumor kinase/protein tyrosine kinase 6 (Brk/PTK6) activity in normal and neoplastic biliary epithelia
J. Hepatol.
63
399-407
2015
Homo sapiens (Q13882), Homo sapiens
Manually annotated by BRENDA team
Huang, Y.; Yoon, M.; Otieno, S.; Lelli, M.; Kriwacki, R.
The activity and stability of the intrinsically disordered Cip/Kip protein family are regulated by non-receptor tyrosine kinases
J. Mol. Biol.
427
371-386
2015
Homo sapiens
Manually annotated by BRENDA team
Zhang, X.; Simerly, C.; Hartnett, C.; Schatten, G.; Smithgall, T.E.
Src-family tyrosine kinase activities are essential for differentiation of human embryonic stem cells
Stem Cell Res.
13
379-389
2014
Homo sapiens
Manually annotated by BRENDA team
Nelin, L.; White, H.; Jin, Y.; Trittmann, J.; Chen, B.; Liu, Y.
The Src family tyrosine kinases src and yes have differential effects on inflammation-induced apoptosis in human pulmonary microvascular endothelial cells
Am. J. Physiol. Lung Cell Mol. Physiol.
310
L880-L888
2016
Homo sapiens (P12931), Homo sapiens
Manually annotated by BRENDA team
Nelin, L.; White, H.; Jin, Y.; Trittmann, J.; Chen, B.; Liu, Y.
The Src family tyrosine kinases src and yes have differential effects on inflammation-induced apoptosis in human pulmonary microvascular endothelial cells
Am. J. Physiol. Lung Cell. Mol. Physiol.
310
L880-L888
2016
Homo sapiens (P07947), Homo sapiens
Manually annotated by BRENDA team
Liu, H.; Cui, Y.; Wang, G.; Dong, Q.; Yao, Y.; Li, P.; Cao, C.; Liu, X.
The nonreceptor tyrosine kinase c-Abl phosphorylates Runx1 and regulates Runx1-mediated megakaryocyte maturation
Biochim. Biophys. Acta Mol. Cell Res.
1865
1060-1072
2018
Homo sapiens (Q9QVP9), Homo sapiens
Manually annotated by BRENDA team
Johnson, T.; Soellner, M.
Bivalent inhibitors of c-Src tyrosine kinase that bind a regulatory domain
Bioconjug. Chem.
27
1745-1749
2016
Homo sapiens (P06239), Homo sapiens (P07948), Homo sapiens (P08631), Homo sapiens (P09769), Homo sapiens (P12931), Homo sapiens (P42685), Homo sapiens (P51451)
Manually annotated by BRENDA team
Li, Y.; Wang, P.; Chen, C.; Ye, T.; Han, Y.; Hou, Y.; Liu, Y.; Gong, P.; Qin, M.; Zhao, Y.
Discovery and rational design of 2-aminopyrimidine-based derivatives targeting Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3)
Bioorg. Chem.
104
104361
2020
Homo sapiens (O60674)
Manually annotated by BRENDA team
Zou, Y.; Xiao, J.; Tu, Z.; Zhang, Y.; Yao, K.; Luo, M.; Ding, K.; Zhang, Y.; Lai, Y.
Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Brutons tyrosine kinase inhibitors
Bioorg. Med. Chem. Lett.
26
3052-3059
2016
Homo sapiens (Q06187)
Manually annotated by BRENDA team
Dasari, T.; Geiger, R.; Karki, R.; Banoth, B.; Sharma, B.; Gurung, P.; Burton, A.; Kanneganti, T.
The nonreceptor tyrosine kinase SYK drives caspase-8/NLRP3 inflammasome-mediated autoinflammatory osteomyelitis
J. Biol. Chem.
295
3394-3400
2020
Homo sapiens (P43405), Homo sapiens, Mus musculus (P48025), Mus musculus
Manually annotated by BRENDA team
Yan, Z.; Shanmugasundaram, K.; Ma, D.; Luo, J.; Luo, S.; Rao, H.
The N-terminal domain of the non-receptor tyrosine kinase ABL confers protein instability and suppresses tumorigenesis
J. Biol. Chem.
295
9069-9075
2020
Homo sapiens (P00519)
Manually annotated by BRENDA team
Yogo, T.; Nagamiya, H.; Seto, M.; Sasaki, S.; Shih-Chung, H.; Ohba, Y.; Tokunaga, N.; Lee, G.N.; Rhim, C.Y.; Yoon, C.H.; Cho, S.Y.; Skene, R.; Yamamoto, S.; Satou, Y.; Kuno, M.; Miyazaki, T.; Nakagawa, H.; Okabe, A.; Marui, S.; Aso, K.; Yoshida, M.
Structure-based design and synthesis of 3-amino-1,5-dihydro-4H-pyrazolopyridin-4-one derivatives as tyrosine kinase 2 inhibitors
J. Med. Chem.
59
733-749
2016
Homo sapiens (O60674), Homo sapiens (P23458), Homo sapiens (P29597), Homo sapiens (P52333), Homo sapiens
Manually annotated by BRENDA team
Myers, S.; Temps, C.; Houston, D.; Brunton, V.; Unciti-Broceta, A.
Development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
J. Med. Chem.
61
2104-2110
2018
Homo sapiens (P12931)
Manually annotated by BRENDA team
Goel, R.; Paczkowska, M.; Reimand, J.; Napper, S.; Lukong, K.
Phosphoproteomics analysis identifies novel candidate substrates of the nonreceptor tyrosine kinase, Src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristoylation sites (SRMS)
Mol. Cell. Proteomics
17
925-947
2018
Homo sapiens (Q9H3Y6)
Manually annotated by BRENDA team
Huang, R.; Fang, P.; Hao, Z.; Kay, B.K.
Directed evolution of a highly specific FN3 monobody to the SH3 domain of human Lyn tyrosine kinase
PLoS ONE
11
e0145872
2016
Homo sapiens (P07948), Homo sapiens
Manually annotated by BRENDA team
Yamada, H.; Tsutsumi, K.; Nakazawa, Y.; Shibagaki, Y.; Hattori, S.; Ohta, Y.
Src family tyrosine kinase signaling regulates FilGAP through association with RBM10
PLoS ONE
11
e0146593
2016
Homo sapiens (P06241), Homo sapiens
Manually annotated by BRENDA team
Wang, Y.; Hu, Y.; Wang, F.; Liu, S.; Wang, Y.; Chen, X.
Role and mechanism of nonreceptor tyrosine kinase Tec in endotoxin/lipopolysaccharide-induced interleukin-8 production in human alveolar epithelial cells A549
Zhonghua Shao Shang Za Zhi
35
580-586
2019
Homo sapiens (P42680), Homo sapiens
Manually annotated by BRENDA team