Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.22.15 extracted from

  • Shah, P.P.; Myers, M.C.; Beavers, M.P.; Purvis, J.E.; Jing, H.; Grieser, H.J.; Sharlow, E.R.; Napper, A.D.; Huryn, D.M.; Cooperman, B.S.; Smith, A.B.; Diamond, S.L.
    Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L (2008), Mol. Pharmacol., 74, 34-41.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking study with inhibitor S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate using the structure of papain/CLIK-148, PDB entry 1cvz Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate slow binding and slowly reversible inhibitor. 7- to 151fold greater selectivity towards cathepsin L then papain and cathepsins B, K, V, and S with no activity against cathepsin G. Inhibitor lacks toxicitiy in human aortic endothelial cells and inhibits in vitro propagation of Plasmodium falciparum with an IC50 value of 15.4 microM and of Leishmania major with an IC50 value of 12.5 microM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
pH 5.5, preincubation with enzyme 4 h before substrate addition Homo sapiens S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
0.0000075
-
pH 5.5, preincubation with enzyme 1 h before substrate addition Homo sapiens S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
0.000056
-
pH 5.5 Homo sapiens S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate