3.4.21.117: stratum corneum chymotryptic enzyme
This is an abbreviated version!
For detailed information about stratum corneum chymotryptic enzyme, go to the full flat file.
Word Map on EC 3.4.21.117
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3.4.21.117
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klk7
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desquamation
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keratinocytes
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cornified
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corneocyte
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netherton
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corneodesmosomes
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desmogleins
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corneodesmosin
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spink5
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medicine
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desmocollin
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vaspin
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diagnostics
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molecular biology
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desquamatory
- 3.4.21.117
- klk7
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desquamation
- keratinocytes
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cornified
- corneocyte
- netherton
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corneodesmosomes
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desmogleins
- corneodesmosin
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spink5
- medicine
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desmocollin
- vaspin
- diagnostics
- molecular biology
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desquamatory
Reaction
cleavage of proteins with aromatic side chains in the P1 position =
Synonyms
hK7, HSCCE, human stratum corneum chymotryptic enzyme, K7, kallikrein 7, kallikrein-7, kallikrein-related peptidase, kallikrein-related peptidase 7, KLK7, More, S01.300, SCCE, stratum corneum chymotryptic enzyme, tissue kallikrein, tissue kallikrein 7
ECTree
Advanced search results
Inhibitors
Inhibitors on EC 3.4.21.117 - stratum corneum chymotryptic enzyme
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(4R)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(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
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(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
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(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
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(4S)-4-benzyl-2-(2,4-dimethylphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
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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
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(4S)-4-benzyl-2-(2,5-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
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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
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(4S)-4-benzyl-2-(2-methoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(2-methylpropyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(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
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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
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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
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(4S)-4-benzyl-2-(3-hydroxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(3-methoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(3-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(4-bromophenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(4-methoxyphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(4-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-2-(4-nitrophenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(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
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(4S)-4-benzyl-2-phenyl-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-benzyl-3,4-dihydro-1H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepine-2,5-dione
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(4S)-4-benzyloxymethyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
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(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
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(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
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(4S)-4-methyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]-imidazo[4,5-d][1,3]diazepin-5-one
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(4S)-4-methyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
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(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
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-1H-pyrrole-2-carboxamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-methylbenzamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-phenylacetamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-3,4-dimethoxybenzamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-3-phenylpropanamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)benzamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)cinnamamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)isonicotinamide
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(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)picolinamide
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1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
1-(2-chlorobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
2-(2-fluoro-phenyl)-5,6,7,8-tertrahydro-benzol[4,5]thieno[2,3-d][1,3]oxazin-4-one
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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
GKCLFSNPPICFPN
peptide inhibitor based on sunflower trypsin inhibitor-1, displays at least 1000fold selectivity over several proteases that are related by function (KLK5 and KLK14) or specificity (chymotrypsin)
LEKTI domain 6
i.e. lympho-epithelial Kazaltype-related inhibitor domain 6, specific inhibition, interaction and binding structure analysis, overview
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LEKTI fragments
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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
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1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
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1-(2-chlorobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
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chymostatin
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proteolysis of both the desmosomal proteins by kallikrein 7 is effectively inhibited in the presence of chymostatin
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i.e. lympho-epithelial Kazaltype-related inhibitor, a 15-domain serine proteinase inhibitor
LEKTI
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LEKTI is expressed in stratum corneum and in stratum granulosum and is a reversible inhibitor encoded by the SPINK5 (serine protease inhibitor Kazal type 5) gene. LEKTI is a weak inhibitor toward KLK 7 but a much stronger inhibitor toward KLK5
Zn2+
inhibition at low micromolar concentrations, noncompetitive inhibition type, structural basis for inhibition involving His99, overview; strong inhibitory effect
additional information
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inhibition assay: 15 min preincubation of the enzyme with inhibitor at 21°C; no inhibition by Mg2+, E-64, 1,10-phenanthrolin, EDTA
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additional information
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phosphoramidon inhibits thermolysin and thus activation of pro-kallikrein 7
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additional information
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phosphoramidon inhibits thermolysin and thus activation of pro-kallikrein 7
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additional information
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usage of the pyridoimidazodiazepinone core as a potential scaffold to develop selective and competitive reversible inhibitors, analysis of structure-activity relationships, inhibition mechanisms, and selectivity as well as cytotoxicity against selected three human cancer cell lines, i.e. the HeLa cells, prostatic PC-3 cell line, and colorectal adenocarcinoma SW-620 cells, structure-based molecular docking, overview. No inhibition by 1b, 1f, 1g, 1h, 1i, 1j, 1l, 1m, 1q, 1r, 1s, 1t, 1u, 1v, 1w, 1x, 1z, 1aa, 1ab, 1ac, 1ad, 2a, 2b, 2c, 2d, 2f, 2h, and 2i
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