Information on EC 3.4.21.117 - stratum corneum chymotryptic enzyme

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.21.117
-
RECOMMENDED NAME
GeneOntology No.
stratum corneum chymotryptic enzyme
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
cleavage of proteins with aromatic side chains in the P1 position
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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-
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CAS REGISTRY NUMBER
COMMENTARY hide
155215-90-0
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9001-01-8
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
Boxer and West Highland white terrier, gene KLK7
-
-
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
Abz-AIKFFSA-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-AIKFF + SA-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-ALFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-ALF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-FLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-FLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-GFSPFRSSRI-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-GFSPF + RSSRI-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-GFSPFRSSRIGEIKEETT-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-GFSPF + RSSRIGEIKEETT-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-GLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-GLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-HLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-HLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-ILFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-ILF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KAFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KAF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KFFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KFF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KLFSSE-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KLF + SSE-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KLTWLPL-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KLTW + LPL-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KLYSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KLY + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KPFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KPF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KVFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KVF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-KYFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-KYF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-LLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-LLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
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-
-
-
?
Abz-LMEKWTW-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-LMEKW + TW-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
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-
-
-
?
Abz-MISLMKRP-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-MISLM + KRP-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
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-
-
-
?
Abz-NLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-NLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-PHVMRFP-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-PHVM + RFP-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
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-
-
-
?
Abz-QLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-QLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-RLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-RLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-VARPYYL-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-VARPYY + L-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-VLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-VLF + SSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-VQFYQGP-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-VQFY + QGP-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-VQMRGFA-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-VQM + RGF + A-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-YNPFVFT-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-YNPF + VF + T-Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Abz-YWSIQPF-Q-N-[2,4-dinitrophenyl]-ethylenediamine + H2O
Abz-Y + WSIQPF + Q-N-[2,4-dinitrophenyl]-ethylenediamine
show the reaction diagram
-
-
-
-
?
Ac-ED(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)KPILFRLGK(4-(4-dimethylaminophenylazo)benzoic acid)E-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-EFKPILWRLGC-(6-(9-oxo-9H-acridin-10-yl)-hexanoate)E-NH2 + H2O
?
show the reaction diagram
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-
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?
acetyl-Phe-Val-Arg-4-nitroanilide + H2O
acetyl-Phe-Val-Arg + 4-nitroaniline
show the reaction diagram
-
chromogenic substrate
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-
?
acidic sphingomyelinase + H2O
?
show the reaction diagram
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-
-
-
?
acidic-sphingomyelinase + H2O
?
show the reaction diagram
-
-
-
-
?
AGCKNFFWKTFTSC + H2O
AGCKNFF + WKTFTSC
show the reaction diagram
-
-
-
-
?
Arg-Pro-Tyr-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
ATHPFIIQ + H2O
ATHPF + IIQ
show the reaction diagram
-
-
-
-
?
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-FR-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-FR + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-LR-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-LR + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
beta-amyloid peptide + H2O
?
show the reaction diagram
beta-glucocerebrosidase + H2O
?
show the reaction diagram
-
-
-
-
?
casein + H2O
?
show the reaction diagram
-
-
-
-
?
cathelicidin + H2O
?
show the reaction diagram
-
-
-
-
?
corneodesmosin + H2O
?
show the reaction diagram
D-Ile-Pro-Arg-4-nitroanilide + H2O
D-Ile-Pro-Arg + 4-nitroaniline
show the reaction diagram
desmocollin 1 + H2O
?
show the reaction diagram
-
-
-
-
?
desmoglein 1 + H2O
?
show the reaction diagram
-
kallikrein 7 cleaves both recombinant desmoglein 1 and desmoglein 2 in vitro
-
-
?
desmoglein 2 + H2O
?
show the reaction diagram
-
kallikrein 7 cleaves both recombinant desmoglein 1 and desmoglein 2 in vitro. Ectopic expression of kallikrein 7 in BxPC-3 pancreatic cancer cells which express desoglein 2 but not desmoglein 1 or kallikrein 7 confirms the cleavage of desmoglein 2 in vivo
-
-
?
DYEAGGY + H2O
L-Asp-L-Tyr + EAGGY
show the reaction diagram
-
-
-
-
?
E-cadherin + H2O
?
show the reaction diagram
Fibronectin + H2O
?
show the reaction diagram
GNYDGPD + H2O
GNY + DGPD
show the reaction diagram
-
-
-
-
?
GVRPHGF + H2O
GV + RPHGF
show the reaction diagram
-
-
-
-
?
human pro-interleukin 1beta + H2O
human interleukin beta1 + ?
show the reaction diagram
insulin beta chain + H2O
?
show the reaction diagram
-
the most preferred P1 residue of KLK7 is Tyr, followed by Ala and Met, whereas Phe, Arg, and Lys are ranked quite low. Tyr is favored at S2 over the medium-sized hydrophobic residues Leu, Thr, Met, and Phe. In agreement with these findings, KLK7 cleaves the insulin B-chain after Asn-Gln-His-Leu, Glu-Ala-Leu-Tyr, Gly-Phe-Phe-Tyr, and Arg-Gly-Phe-Phe
-
-
?
kallistatin + H2O
?
show the reaction diagram
-
-
-
-
?
L-Phe-7-amido-4-methylcoumarin + H2O
L-Phe + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
L-Tyr-7-amido-4-methylcoumarin + H2O
L-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
LMQHPQD + H2O
LM + QHPQD
show the reaction diagram
-
-
-
-
?
Mca-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 + H2O
?
show the reaction diagram
MeO-succinly-Arg-Pro-Tyr-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
methoxy-succinyl-Ala-Ala-Pro-Met-4-nitroanilide + H2O
methoxy-succinyl-Ala-Ala-Pro-Met + 4-nitroaniline
show the reaction diagram
methoxy-succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
methoxy-succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline
show the reaction diagram
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
show the reaction diagram
methoxy-succinyl-Arg-Pro-Tyr-p-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + p-nitroaniline
show the reaction diagram
-
-
-
?
N-carbobenzoxy-Gly-Pro-Arg-4-nitroanilide + H2O
N-carbobenzoxy-Gly-Pro-Arg + 4-nitroaniline
show the reaction diagram
N-carbobenzoxy-Val-Gly-Arg-4-nitroanilide + H2O
N-carbobenzoxy-Val-Gly-Arg + 4-nitroaniline
show the reaction diagram
o-aminobenzoyl-FRAPR-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
-
low activity
-
-
?
o-aminobenzoyl-FRLVR-(2,4-dinitrophenyl)ethylenediamine + H2O
o-aminobenzoyl-FR + LVR-(2,4-dinitrophenyl)ethylenediamine
show the reaction diagram
-
low activity
-
?
o-aminobenzoyl-SVIRRVQ-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-TSVIRRPQ-(2,4-dinitrophenyl)ethylenediamine + H2O
?
show the reaction diagram
-
low activity
-
-
?
oxidized bovine insulin B chain + H2O
peptides + (Tyr)26
show the reaction diagram
-
recombinant enzyme
product identification, cleavage sites are: Leu6-cysteic acid7, Tyr16-Leu17, Phe25-Tyr26, Tyr26-Tr27
?
PDETYFF + H2O
PDETY + L-Phe-L-Phe
show the reaction diagram
-
-
-
-
?
PFR-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
best substrate
-
-
?
Phe-7-amido-4-methylcoumarin + H2O
Phe + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
pro-matrix metalloproteinase-2 + H2O
?
show the reaction diagram
-
KLK7 degrades, but does not activate, pro-matrix metalloproteinase-2
-
-
?
pro-matrix metalloproteinase-9 + H2O
matrix metalloproteinase-9
show the reaction diagram
-
KLK7 degrades and activates pro-matrix metalloproteinase-9, cleavage occurs between Tyr443 and Gly444
the product is a truncated, active matrix metalloproteinase-9 lacking the C-terminal hemopexin domains which is not generated by other proteases
-
?
QMELPVH + H2O
Gln-Met + ELPVH
show the reaction diagram
-
-
-
-
?
RPKPQQFFGLM + H2O
RPKPQQ + L-Phe + FGLM
show the reaction diagram
-
-
-
-
?
SANSNPAMAPRERKAGCKNFFWKTFTSC + H2O
SANSNPAMAPRERKAGCKNFF + WKTFTSC
show the reaction diagram
-
-
-
-
?
SFPQVHS + H2O
SFPQV + HS
show the reaction diagram
-
-
-
-
?
somatostatin + H2O
?
show the reaction diagram
-
-
-
-
?
STLDWQD + H2O
STLDW + QD
show the reaction diagram
-
-
-
-
?
STLDWQH + H2O
STLDW + QH
show the reaction diagram
-
-
-
-
?
Substance P + H2O
?
show the reaction diagram
-
-
-
-
?
Suc-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin + H2O
Suc-Leu-Leu-Val-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-AAPF-7-amido-4-methylcoumarin + H2O
succinyl-AAPF + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline
show the reaction diagram
-
chromogenic substrate
-
-
?
succinyl-Ala-Ala-Pro-Phe-7-amido-4-methylcoumarin + H2O
succinyl-Ala-Ala-Pro-Phe + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-Ala-Val-Pro-Phe 4-nitroanilide + H2O
succinyl-Ala-Val-Pro-Phe + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
succinyl-Leu-Leu-Tyr-7-amido-4-methylcoumarin + H2O
succinyl-Leu-Leu-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin + H2O
succinyl-Leu-Leu-Val-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Leu-Phe-4-nitroanilide + H2O
succinyl-Phe-Leu-Phe + 4-nitroaniline
show the reaction diagram
succinyl-Val-Pro-Phe-4-nitroanilide + H2O
succinyl-Val-Pro-Phe + 4-nitroaniline
show the reaction diagram
tert-butyloxycarbonyl-Leu-Gly-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Leu-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Ser-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
TGQPIGI + H2O
TGQPI + GI
show the reaction diagram
-
-
-
-
?
Tyr-7-amido-4-methylcoumarin + H2O
Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
VQPFHDP + H2O
VQPF + HDP
show the reaction diagram
-
-
-
-
?
VREHMVD + H2O
VREHM + L-Val-L-Asp
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
beta-amyloid peptide + H2O
?
show the reaction diagram
-
degradation, the enzyme cleaves after both Phe residues within the core of Abeta42 in vitro, thereby inhibiting A? fibril formation and promoting the degradation of preformed fibrils
-
-
?
E-cadherin + H2O
?
show the reaction diagram
-
kallikrein 7 degrades extracellular matrix proteins, and enhances pancreatic cancer cell invasion by shedding E-cadherin, overview
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
kallikrein degrades components of the extracellular matrix
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
sodium chloride
-
inhibits the enzyme to over 60% at up to 1 M
Sodium citrate
-
inhibits the enzyme at up to 750 mM, but not at higher concentrations
Sodium sulfate
-
inhibits the enzyme at up to 1000 mM, but not at higher concentrations
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(4R)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-(1-naphthyl)methyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-(4-benzyloxy)benzyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-(4-hydroxyphenyl)-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(2,4-dimethylphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
-
cytotoxic effect
(4S)-4-benzyl-2-(2,5-dihydroxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(2,5-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
-
cytotoxic effect
(4S)-4-benzyl-2-(2-hydroxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(2-methoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(2-methylpropyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(3,4,5-trimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
-
cytotoxic effect
(4S)-4-benzyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
-
mechanism of inhibition, modeling, overview. Cytotoxic effect
(4S)-4-benzyl-2-(3,4-dimethoxyphenyl)-4,5-dihydro-3H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-ol
-
-
(4S)-4-benzyl-2-(3-hydroxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(3-methoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(3-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(4-bromophenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(4-methoxyphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(4-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(4-nitrophenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-(pyridin-3-yl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-2-phenyl-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyl-3,4-dihydro-1H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepine-2,5-dione
-
-
(4S)-4-benzyloxymethyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-benzyloxymethyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-hydroxymethyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2] imi-dazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-methyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]-imidazo[4,5-d][1,3]diazepin-5-one
-
-
(4S)-4-methyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
-
-
(S)-4-benzyl-2-(3,4-dimethoxyphenyl)-3-methyl-3H-pyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5(4H)-one
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-1H-pyrrole-2-carboxamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-methylbenzamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-phenylacetamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-3,4-dimethoxybenzamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-3-phenylpropanamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)benzamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)cinnamamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)isonicotinamide
-
-
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)picolinamide
-
-
2-(2-fluoro-phenyl)-5,6,7,8-tertrahydro-benzol[4,5]thieno[2,3-d][1,3]oxazin-4-one
-
-
Abz-KLASSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLDSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLESSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLGSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLHSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLISSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLKSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLLSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLMSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLNSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLPSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLQSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLRSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLSSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLTSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLVSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Abz-KLWSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
-
Ala-Ala-Phe-chloromethyl ketone
-
-
Ala-Ala-Phe-chloromethylketone
-
-
alpha1-Antichymotrypsin
-
99.6% inhibition at 0.00015 mM
-
alpha1-Macroglobulin
-
44.2% inhibition at 0.00015 mM
-
Alpha1-proteinase inhibitor
-
89.6% inhibition at 0.00015 mM
-
antileukoprotease
-
Aprotinin
chymostatin
Cu2+
-
inhibition at low micromolar concentrations, structural basis for inhibition, overview; strong inhibitory effect
DMSO
-
catalytic activity of the protease decreases with increasing DMSO concentration
Eglin c
-
99.8% inhibition at 0.00015 mM
elafin
-
33.4% inhibition at 0.0015 mM
-
FEIIKKYQ
-
-
LEKTI
LEKTI domain 6
i.e. lympho-epithelial Kazaltype-related inhibitor domain 6, specific inhibition, interaction and binding structure analysis, overview
-
LEKTI fragments
-
i.e. lympho-epithelial Kazaltype-related inhibitor fragments, furin-derived and secreted in cultured keratinocytes and in the epidermis, specifically inhibit KLK5, KLK7, and KLK14 and control desquamation through a pH-dependent interaction, overview
-
pepstatin A
-
weak inhibition, 23.6% inhibition at 0.1 mM
Soybean trypsin inhibitor
-
Suc-Ala-Ala-Pro-Phe-chloromethylketone
-
-
succinyl-Ala-Ala-Pro-Phe-chloromethyl ketone
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
kallikrein 5
-
activates proform of kallikrein 7
-
plasmin
-
-
-
Thermolysin
-
-
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0009
Abz-AIKFFSA-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0043
Abz-ALFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0032
Abz-FLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.002
Abz-GFSPFRSSRI-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.069
Abz-GFSPFRSSRIGEIKEETT-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0062
Abz-GLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0034
Abz-HLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0027
Abz-ILFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0035
Abz-KAFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.003
Abz-KFFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0018
Abz-KLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0034
Abz-KLYSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0025
Abz-KPFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0019
Abz-KVFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0027
Abz-KYFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0046
Abz-LLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0004
Abz-MISLMKRP-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0017
Abz-NLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0052
Abz-QLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0041
Abz-RLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0021
Abz-VLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0059
Ac-ED(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)KPILFRLGK(4-(4-dimethylaminophenylazo)benzoic acid)E-NH2
-
kcat/KM: 170000/Msec
0.048
Ac-EFKPILWRLGC-(6-(9-oxo-9H-acridin-10-yl)-hexanoate)E-NH2
-
Vmax: 12 nM/sec
0.08
acetyl-Phe-Val-Arg-4-nitroanilide
-
pH 8.0, 37C
0.0443
L-Phe-7-amido-4-methylcoumarin
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25C
0.0402
L-Tyr-7-amido-4-methylcoumarin
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25C
0.0159
Mca-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2
-
0.65
methoxy-Suc-Arg-Pro-Tyr-4-nitroanilide
-
pH 8.0, 37C
0.0402 - 0.0443
Phe-7-amido-4-methylcoumarin
0.22
succinyl-Phe-Leu-Phe-4-nitroanilide
-
pH 8.0, 37C
additional information
additional information
-
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.03
Abz-AIKFFSA-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.1
Abz-ALFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.09
Abz-FLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.03
Abz-GFSPFRSSRI-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
1
Abz-GFSPFRSSRIGEIKEETT-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.03
Abz-GLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.1
Abz-HLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.06
Abz-ILFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.02
Abz-KAFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.02
Abz-KFFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.1
Abz-KLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.85
Abz-KLYSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.02
Abz-KPFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.04
Abz-KVFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.02
Abz-KYFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.07
Abz-LLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.01
Abz-MISLMKRP-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.28
Abz-NLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.15
Abz-QLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.13
Abz-RLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.13
Abz-VLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
0.48
Ac-EFKPILWRLGC-(6-(9-oxo-9H-acridin-10-yl)-hexanoate)E-NH2
Homo sapiens
-
-
0.04
acetyl-Phe-Val-Arg-4-nitroanilide
Homo sapiens
-
pH 8.0, 37C
0.000016
L-Phe-7-amido-4-methylcoumarin
Homo sapiens
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25C
0.000033
L-Tyr-7-amido-4-methylcoumarin
Homo sapiens
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25C
1.2
methoxy-Suc-Arg-Pro-Tyr-4-nitroanilide
Homo sapiens
-
pH 8.0, 37C
0.000016 - 0.000033
Phe-7-amido-4-methylcoumarin
0.05
succinyl-Phe-Leu-Phe-4-nitroanilide
Homo sapiens
-
pH 8.0, 37C
additional information
additional information
Homo sapiens
-
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
29
Abz-AIKFFSA-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202320
22
Abz-ALFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202331
27
Abz-FLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202328
13
Abz-GFSPFRSSRI-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202339
14
Abz-GFSPFRSSRIGEIKEETT-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202340
5
Abz-GLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202336
30
Abz-HLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202335
21
Abz-ILFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202332
6.3
Abz-KAFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202326
5.7
Abz-KFFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202324
55
Abz-KLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202322
250
Abz-KLYSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202321
6.4
Abz-KPFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202327
20
Abz-KVFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202325
6
Abz-KYFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202323
15
Abz-LLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202329
23
Abz-MISLMKRP-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202338
165
Abz-NLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202334
29
Abz-QLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202337
32
Abz-RLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202333
62
Abz-VLFSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
Homo sapiens
-
pH 7.5, 37C
202330
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.002
Abz-KLASSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0032
Abz-KLDSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.003
Abz-KLESSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0022
Abz-KLGSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0013
Abz-KLHSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0002
Abz-KLISSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0003
Abz-KLKSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0015
Abz-KLLSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.001
Abz-KLMSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0011
Abz-KLNSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0022
Abz-KLPSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0022
Abz-KLQSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0016
Abz-KLRSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0018
Abz-KLSSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0023
Abz-KLTSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.0017
Abz-KLVSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.001
Abz-KLWSSK-Q-N-[2,4-dinitrophenyl]-ethylenediamine
-
pH 7.5, 37C
0.000063
antileukoprotease
-
pH 8.0, 37C
-
0.000027
Aprotinin
-
pH 8.0, 37C
0.0006
Cu2+
-
25C; apparent value
0.00000033
Eglin c
-
pH 8.0, 37C
0.0016
elafin
-
pH 8.0, 37C
-
0.0000348
LEKTI
-
-
0.01
Zn2+
-
25C; apparent value
additional information
additional information
-
inhibition kinetics with LEKTi fragments, overview
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0959
(4R)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.0839
(4S)-4-benzyl-2-(2,4-dimethylphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.0809
(4S)-4-benzyl-2-(2,5-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.057
(4S)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.0557
(4S)-4-benzyl-2-(3,4,5-trimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.0335
(4S)-4-benzyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.1248
(4S)-4-benzyl-2-(3-hydroxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.072
(4S)-4-benzyl-2-(4-methoxyphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.068
(4S)-4-benzyl-2-(4-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
Homo sapiens
-
pH 8..0, 37C
0.1354
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-methylbenzamide
Homo sapiens
-
pH 8..0, 37C
0.1492
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-phenylacetamide
Homo sapiens
-
pH 8..0, 37C
0.00007
2-(2-fluoro-phenyl)-5,6,7,8-tertrahydro-benzol[4,5]thieno[2,3-d][1,3]oxazin-4-one
Homo sapiens
-
-
0.026
LEKTI domain 6
Homo sapiens
P49862
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.5
-
proteolysis of corneodesmosin
5.6
-
assay at
7
-
assay at
7.2
-
assay at
7.4
-
assay at
7.5 - 8.5
-
assay at
7.5
-
assay at
9
-
assay at
additional information
-
enzyme shows optimal activity at neutral pH, and retains significant activity at acidic pH
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.5 - 8
-
no activity at pH 4.0, highest activity at 8.0
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
-
assay at
25 - 37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
from ovarian cancer patients
Manually annotated by BRENDA team
-
breast cancer patients with KLK7 positive tumors have relatively shorter disease-free survival and overall survival than patients with KLK7 negative tumors
Manually annotated by BRENDA team
-
breast carcinoma cell line, enzyme is upregulated by estrogens and slightly by glucocorticoids
Manually annotated by BRENDA team
-
increased expression of kallikrein 7 and decreased expression of its inhibitor antileukoprotease might play an important role in cervical adenocarcinoma development
Manually annotated by BRENDA team
-
50% of the primary and 50% of the established cervical cancer cell lines express kallikrein 7
Manually annotated by BRENDA team
-
cervical intraepithelial neoplasia, cervicitis, squamous cervical carcinomas, and cervical adenocarcinomas
Manually annotated by BRENDA team
-
high expression of the enzyme
Manually annotated by BRENDA team
-
colon cancer cell lines and colonic tumors
Manually annotated by BRENDA team
-
semi-quantitative RT-PCR determination and immunohistochemical analysis
Manually annotated by BRENDA team
-
recombinant pro-kallikrein 7
Manually annotated by BRENDA team
-
plantar
Manually annotated by BRENDA team
-
microglial and oligodendroglia
Manually annotated by BRENDA team
-
the transcriptional changes 3 and 60 h after TNF treatment of normal, human papillomaviruses 16- and human papillomaviruses 18-immortalized keratinocytes is analyzed by microarray analysis. KLK7 shows a differential expression pattern associated with the differential response to TNF. KLK7 expression pattern is is equally expressed in TNF-treated or untreated human papillomaviruses 18-immortalized cells but it is not detected in normal primary keratinocytes or human papillomaviruses 16-immortalized cells
Manually annotated by BRENDA team
-
KLK7 shows strong expression in low grade in contrast to high grade clear cell renal cell carcinoma, RCC, overview. The expression of KLK7 can distinguish between oncocytoma and chromophobe RCC
Manually annotated by BRENDA team
-
KLK7 is strongly expressed in the tissue of patients with squamous cell carcinoma and differentiated tumors
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
low content
Manually annotated by BRENDA team
-
ALP is significantly decreased in prostate cancers compared with that in benign prostate epithelial cells. Immunohistochemical expression of kallikrein 7 is observed in prostate epithelial cells, whereas little or no staining is observed in prostate cancer. Western blot analysis reveals that hK7 and antileukoprotease are decreased in malignant prostate epithelium
Manually annotated by BRENDA team
-
low content
Manually annotated by BRENDA team
-
low content
Manually annotated by BRENDA team
-
low content
Manually annotated by BRENDA team
-
low content
Manually annotated by BRENDA team
-
low content
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
the enzyme is secreted
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
9000
-
x * 9000 + x * 19000, SDS-PAGE
19000
-
x * 9000 + x * 19000, SDS-PAGE
25000
-
x * 25000, SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
proteolytic modification
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
analysis of crystal structure of KLK7: owing to the conformational restrictions of the relatively narrow S1 pocket, the formation of a stabilizing hydrogen bond between the P1-Tyr-OH and the carboxamide of Asn189 has to be mediated by a water molecule. The S2 subsite is less separated from the S4 subsite than in KLK4-6 and less limited in size owing to a different position of the His99 imidazole side chain, which may also contribute to the capacity for the adaptation to P2 side chains of various size; two crystal structures of KLK7 are solved with either of two covalently bound chloromethyl ketone (CMK) inhibitors. Overall, the S1 pocket of KLK7 is larger and more hydrophobic than those of the tryptic KLK4, 5, and 6. The hydrophobicity of the S1 pocket is enhanced by the presence of Ala190 instead of Ser190, and at the bottom of the pocket, Asn189, a polar residue, replaces Asp189, a negatively charged residue. Consistent with specificity, Asn189 insteadof Asp189 would reduce the affinity of KLK7 for basic P1 side chains and allow binding of non-polar residues. The size and shape of the S1 pocket is well suited to accommodate residues with medium and large side chains, explaining the modified chymotryptic specificity. Tyr may be favored over Phe at P1 because of the potential of the carboxyamide group of Asn189 to hydrogen bond to a buried hydroxyl group
-
kallikrein 7 bound to inhibitors succinyl-Ala-Ala-Pro-Phe-chloromethyl ketone and Ala-Ala-Phe-chloromethyl ketone, sitting-drop vapor diffusion method at 18C, 0.001 ml protein solution, containing 7 mg/ml enzyme-inhibitor complex, is mixed with 0.001 ml reservoir solution containing 100 mM [bis(2-hydroxyethyl)amino]tris(hydroxymethyl)-methane-HCl, pH 6.0, 25% PEG 3350, and 2.5 M Li2SO4, equilibration against reservoir solution, X-ray diffraction structure determination and analysis at 1.0-2.5 A resolution; sitting drop vapour diffusion method, with 100 mM [bis(2-hydroxyethyl)amino]tris(hydroxymethyl)-methane-HCl, pH 6.0, 25% PEG 3350, and 2.5 M Li2SO4 or with 100 mM sodium cacodylate, pH 6.5, 200 mM magnesium acetate, and 30% (v/v) 2-methyl-2,4-pentanediol
-
purified recombinant enzyme bound to specific inhibitor LEKTI domain 6, 8 mg/ml protein in sodium phosphate buffer, pH 7.5, with a reservoir solution containing 3.2 M ammonium sulfate in 0.1 M HEPES, pH 7.0, X-ray diffraction structure determination and anaylsis at 2.8 A resolution
purified recombinant His-tagged enzyme, sitting-drop vapour-diffusion method, 22C, 0.0001 ml of 8 mg/ml protein in 50 mM sodium phosphate buffer, pH 7.5, mixed with 0.0001 ml of reservoir solution, X-ray diffraction structure determination and anaylsis at 2.8 A resolution
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
nickel-nitrilotriacetic acid-Sepharose column chromatography and benzamidine-Sepharose column chromatography
partially
-
recombinant
-
recombinant and native enzyme
recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3)SS periplasm by nickel affinity chromatography
-
recombinant kallikrein 7 from HEK-293F cell culture supernatant by ultrafiltration and dialysis, anion exchange chromatography, and heparin affinity chromatography, followed by metal affinity on an iminodiacetic acid epoxy resin column, elution with L-histidine from the latter column, to homogeneity
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cloning from keratinocyte library, DNA and RNA sequence determination and analysis, expression of the enzyme in its proform in murine C127 cells, enzyme activation by trypsin
development of an in situ quantitative method of protein expression detection
-
DNA sequence determination and analysis, gene KLK7 mapps to chromosomal locus 19q13.3-13.4, human kallikrein gene family locus
enzyme overexpression in HT-29 cells resulting in increased cell proliferation
-
expressed as a His-tagged fusionprotein in Escherichia coli
-
expressed in Escherichia coli and in a baculovirus-insect cell system
-
expressed in Escherichia coli M15(pREP4) cells
expressed in the neuroblastoma cell line SH-SY5Y
-
expression analysis by quantitative RT PCR analysis
gene KLK7, DNA and amino acid sequence determination and analysis, expression anaysis and microsatellite-based association mapping, allele sizes and distribution of KLK7, overview
-
gene KLK7, encoded on chromosome 19, expression of His-tagged enzyme in Escherichia coli strain BL21(DE3)SS with secretion to the the bacterial periplasm
-
gene KLK7, expression in Escherichia coli with secretion to the the bacterial periplasm
gene KLK7, expression profiling in BxPC-3 cells from pancreatic adenocarcinomas
-
gene KLK7, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4
-
gene KLK7, overexpression in breast cancer cell lines aMCF-7, OVMZ-6, and MDA-231, quantitative expression analysis in wild-type native cells and in transfected cells, overview
gene KLK7, stable expression of pro-kallikrein 7 in HEK-293F cells, secretion of the recombinant protein to the cell culture supernatant, activation of the recombinant enzyme by thermolysin
-
KLK genes are located on chromosome 19q13.4
-
recombinant kallikrein 7 is produced in HEK 293T cells
-
stable overexpression of KLK7-253 in SKOV-3 cells, leading to formation of multicellular aggregates, MCAs, that promote cell survival and chemoresistance, with involvement of KLK7 and integrin-regulated cell adhesion. KLK7-253 cells form MCAs invade into mesothelial cell monolayers
-
the gene encoding the enzyme is localized at chromosome locus 19q13.4, recombinant expression in an insect cell line using the baculovirus transfection system
-
transgenic mice overexpressing human scce-gene. Epidermal hyperproliferation and decreased skin barrier function in mice overexpressing stratum corneum chymotryptic enzyme
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
increased extracellular calcium-induced KLK7 mRNA expression and protein release in epidermal keratinocyte. Increased protease activity and differential processing of cathelicidin accompanies increased KLK expression. 1,25(OH)2VD3 increases KLK expression independently of differentiation in keratinocytes
-
KLK7 expression is decreased in prostate cancer cells compared to normal benign prostate cells
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
-
ELISA-type immunoassay for human kallikrein quantification
H41F
-
mutant is inhibited by Zn2+ as the wild type enzyme; site-directed mutagenesis, the mutant is inhibited by Zn2+ like the wild-type enzyme
H99A
-
mutant exhibits virtually no Zn2+ inhibition; site-directed mutagenesis, the mutant shows resistance against inhibition by Zn2+ in contrast to the wild-type enzyme
additional information
Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
diagnostics
medicine
molecular biology