3.4.21.118: kallikrein 8
This is an abbreviated version!
For detailed information about kallikrein 8, go to the full flat file.
Word Map on EC 3.4.21.118
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3.4.21.118
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kallikreins
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klk8
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melanopsin
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desquamation
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photopigment
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iprgcs
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non-visual
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peropsin
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medicine
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biotechnology
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molecular biology
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pharmacology
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analysis
- 3.4.21.118
- kallikreins
- klk8
- melanopsin
-
desquamation
-
photopigment
-
iprgcs
-
non-visual
-
peropsin
- medicine
- biotechnology
- molecular biology
- pharmacology
- analysis
Reaction
cleavage of amide substrates following the basic amino acids Arg or Lys at the P1 position, with a preference for Arg over Lys =
Synonyms
Alzheimers associated protease, brain serine protease 1, GK-8, hK8, kallikrein 8, kallikrein 8 protease, kallikrein-8, kallikrein-related peptidase, kallikrein-related peptidase 8, kallikrein-related peptidase-8, KLK8, KRP/hK8, mK8, neuropsin, NP, ovasin, P1 kallikrein, PRSS19, RGK-8, S01.244, TADG-14, TADG14, tissue kallikrein, type I neuropsin, type II neuropsin
ECTree
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Inhibitors
Inhibitors on EC 3.4.21.118 - kallikrein 8
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1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
compound is a promising lead for development of novel kallikrein-8 inhibitors. It binds stably to the kallikrein-8 S1 binding site
1-(3,5-difluorophenyl)-5-hydroxy-7-(4-hydroxy-3,5-dimethoxyphenyl)-6,7-dihydro-1H-pyrrolo[3,2-b] pyridine-3-carboxylic acid
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i.e. ZINC61720639
2-[[5-(2-chlorophenyl)-4-imino-3-methyl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]sulfanyl]-N-(2,5-dimethoxyphenyl)acetamide
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4-amino-N3-[(2R)-1-(tert-butylamino)-1-oxopropan-2-yl]-N3-(3-chloro-4-fluorophenyl)-2H-pyrrole-3,5-dicarboxamide
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murinoglobulin I
24% inhibition at enzyme-inhibitor ratio of 1:2; formation of a SDS-stable complex; i.e. MUG I
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N-[[5-([2-[(4-bromo-2-fluorophenyl)amino]-2-oxoethyl]sulfanyl)-4-methyl-4H-1,2,4-triazol-3-yl]methyl]furan-2-carboxamide
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NP STOP
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neuropsin-specific inhibitor. Single stimulus in S1 during application of NP STOP completely eliminates the late associativity between S0 and S1 synapses. When a strong (four) stimulus in S0 is followed by the application of NP STOP, the late associativity between S0 and S1 synapses is not eliminated
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serine protease inhibitor-3
formation of a SDS-stable complex, bimolecular kinetics; from pyramidal neurons; slowly and tightly binding inhibitor
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shRNA
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inhibition of endogenous KLK8 expression, reduces cancer cell invasiveness
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trans-epoxysuccinyl-L-leucylamido(4-guanidinobutane)
i.e. E-64, 15% inhibition at 0.1 mM
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is a physiologically relevant inhibitor of hK8 in skin. SerpinB6 protects the intracellular compartment of keratinocytes from ectopic hK8
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not inhibitory: Nalpha-p-tosyl-L-phenylalanine chloromethyl ketone, pepstatin, o-phenynthroline, E-64
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additional information
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not inhibitory: Nalpha-p-tosyl-L-phenylalanine chloromethyl ketone, pepstatin, o-phenynthroline, E-64
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additional information
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KLK8 is not inhibited by EDTA and alpha1-antitrypsin; mature KLK8 activity is attenuated by autocleavage after Arg164
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additional information
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inhibitor screening by molecular modeling and ligand docking study, interactions with the active site, overview
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additional information
enzyme is strongly inhibited by low molecular weight protease inhibitors that bind to His and Ser residues in the active center of serine proteases; no or very slight inhibition by pepstatin A, trypsin inhibitor, Ca2+, Mg2+, and metal chelators
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additional information
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enzyme is strongly inhibited by low molecular weight protease inhibitors that bind to His and Ser residues in the active center of serine proteases; no or very slight inhibition by pepstatin A, trypsin inhibitor, Ca2+, Mg2+, and metal chelators
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