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Information on EC 2.7.11.21 - polo kinase and Organism(s) Danio rerio and UniProt Accession Q6DRK7
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2.7.11.21 polo kinaseIUBMB Comments
The enzyme associates with the spindle pole during mitosis and is thought to play an important role in the dynamic function of the mitotic spindle during chromosome segregation. The human form of the enzyme, Plk1, does not phosphorylate histone H1, enolase and phosvitin but it can phosphorylate myelin basic protein and microtubule-associated protein MAP-2, although to a lesser extent than casein .
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Word Map
- 2.7.11.21
-
mitotic
- centrosome
-
checkpoint
-
cytokinesis
-
aurora
- microtubule
-
anaphase
- sirnas
-
polo-box
- cyclin
- kinetochore
-
cyclin-dependent
-
exit
- centriole
-
interphase
-
chromatid
-
metaphase
-
cell-cycle
-
meiosis
-
m-phase
-
faithful
-
aneuploidy
-
anaphase-promoting
-
pericentriolar
-
prometaphase
- cohesins
-
prophase
-
centromeres
- cdc25c
-
midbody
-
mitosis-specific
-
atp-competitive
- bubr1
-
kinetochore-microtubule
-
misalign
- midzone
- diagnostics
- pharmacology
-
missegregation
-
microtubule-organizing
-
monopolar
- securin
- wee1
- drug development
- cdc14
- analysis
-
condensin
-
metaphase-anaphase
- medicine
- gamma-tubulin
-
furrow
- mps1
- separase
- chk1
-
telophase
The taxonomic range for the selected organisms is: Danio rerio
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
+
a [protein]-(L-serine/L-threonine)
=
+
a [protein]-(L-serine/L-threonine) phosphate
Synonyms
polo-like kinase 1, polo-like kinase, plk-1, polo kinase, polo-like kinase 4, polo-like kinase-1, tbplk, plk1 kinase, cdc5p, polo-like kinase 2, 
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
FGF-inducible kinase
-
-
-
-
Plk1
Polo-like kinase 1
Proliferation-related kinase
-
-
-
-
zPlk1
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phospho group transfer
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (spindle-pole-dependent)
The enzyme associates with the spindle pole during mitosis and is thought to play an important role in the dynamic function of the mitotic spindle during chromosome segregation. The human form of the enzyme, Plk1, does not phosphorylate histone H1, enolase and phosvitin but it can phosphorylate myelin basic protein and microtubule-associated protein MAP-2, although to a lesser extent than casein [2].
CAS REGISTRY NUMBER
COMMENTARY
149433-93-2
Polo kinase
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + casein
ADP + phosphocasein
substrate in biochemical activity assay
-
-
?
ATP + 5FAM-RALMEASFADQAR-NH2
ADP + phosphorylated 5FAM-RALMEASFADQAR-NH2
substrate peptide, based on human Cdc25C, used in biochemical activity assay
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(5-methyl-2-trifluoro-methyl-furan-3-yl)-3-(5-[2-[6-(1H-[1,2,4]triazol-3-ylamino)-pyrimidin-4-ylamino]-ethyl]-thiazol-2-yl)urea
-
1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
-
-
3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
-
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
-
-
N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
-
N-[2-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
-
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.004516
1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.01445
1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000641
1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000149
1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000274
1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000121
1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000464
1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.005928
1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.003241
1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000703
1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000059
1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000977
1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000412
3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
Danio rerio
-
-
0.007685
3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000474
3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.004528
3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.001301
3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.001476
3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000225
3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000032
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
Danio rerio
-
-
0.000021
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
Danio rerio
-
-
0.000048
N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
Danio rerio
-
-
0.000207
N-[2-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
Danio rerio
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). Q6DRK7_DANRE
595
0
67760
TrEMBL
other Location (Reliability: 2)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
35920
expected molecular weight of the protein with the N-terminal Gly-Pro-Leu-Gly-Ser linker residues that separate the GST protein from Plk1 KD
35930
expected molecular weight of the protein with the additional T196D substitution
34390
expected molecular weight of the protein with the N-terminal Gly-Pro-Leu-Gly-Ser linker residues and a T196D substitution
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
the structures of wild-type zPlk KD, mutant T196D, wild-type zPlk KD in complex with ADP and the mutant T196D in complex with wortmannin are determined at resolutions of 2.8, 2.4, 2.6 and 2.6 A, respectively
the structure of zPlk1 KD in complex with the inhibitor is solved to 2.85 A resolution
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
full-length zPlk1 cDNA is inserted into the pME18S-FL3 plasmid and subcloned into pGEX6P-1, the zPlk1 kinase domain sequences for crystallography and activity constructs encompassing amino acids 1-312 or 17-312
full-length zPlk1 cDNA and the zPlk1 kinase domain sequence, encompassing residues 17-312, are cloned, the expression plasmid pGEX6P-1 is used
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Elling, R.A.; Fucini, R.V.; Romanowski, M.J.
Structures of the wild-type and activated catalytic domains of Brachydanio rerio Polo-like kinase 1 (Plk1): changes in the active-site conformation and interactions with ligands
Acta Crystallogr. Sect. D
64
909-918
2008
Homo sapiens, Danio rerio (Q6DRK7), Danio rerio
Elling, R.A.; Fucini, R.V.; Hanan, E.J.; Barr, K.J.; Zhu, J.; Paulvannan, K.; Yang, W.; Romanowski, M.J.
Structure of the Brachydanio rerio Polo-like kinase 1 (Plk1) catalytic domain in complex with an extended inhibitor targeting the adaptive pocket of the enzyme
Acta Crystallogr. Sect. F
64
686-691
2008
Danio rerio (Q4KMI8), Danio rerio
Fucini, R.V.; Hanan, E.J.; Romanowski, M.J.; Elling, R.A.; Lew, W.; Barr, K.J.; Zhu, J.; Yoburn, J.C.; Liu, Y.; Fahr, B.T.; Fan, J.; Lu, Y.; Pham, P.; Choong, I.C.; VanderPorten, E.C.; Bui, M.; Purkey, H.E.; Evanchik, M.J.; Yang, W.
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors
Bioorg. Med. Chem. Lett.
18
5648-5652
2008
Danio rerio
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