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Literature summary for 3.4.22.15 extracted from

  • Ramalho, S.D.; De Sousa, L.R.; Nebo, L.; Maganhi, S.H.; Caracelli, I.; Zukerman-Schpector, J.; Lima, M.I.; Alves, M.F.; Da Silva, M.F.; Fernandes, J.B.; Vieira, P.C.
    Triterpenoids as novel natural inhibitors of human cathepsin L (2014), Chem. Biodivers., 11, 1354-1363.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Pichia pastoris Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oic acid competitive inhibition Homo sapiens
(13alpha,17alpha,20S,24Z)-3-oxolanosta-7,24-dien-26-oic acid competitive inhibition Homo sapiens
(2E)-[(3E)-28-methoxy-28-oxours-12-en-3-ylidene]acetic acid competitive inhibition Homo sapiens
(3E)-3-(carboxymethylidene)olean-12-en-28-oic acid competitive inhibition Homo sapiens
(3E)-3-(carboxymethylidene)urs-12-en-28-oic acid competitive inhibition Homo sapiens
3-(hydroxyimino)masticadienoic acid competitive inhibition Homo sapiens
3-(hydroxyimino)oleanolic acid competitive inhibition Homo sapiens
3-epiursolic acid competitive inhibition Homo sapiens
3-hydroxyolean-12-en-28-oic acid competitive inhibition Homo sapiens
3-hydroxyurs-12-en-28-oic acid competitive inhibition Homo sapiens
3-oxoolean-12-en-28-oic acid competitive inhibition Homo sapiens
3-oxours-12-en-28-oic acid competitive inhibition Homo sapiens
E-64 i.e. 1-[N-[(L-3-trans-carboxyoxirane-2-carbonyl)-L-leucyl]amino]-4-guanidinobutane Homo sapiens
methyl (13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oate competitive inhibition Homo sapiens
methyl (3Z,13alpha,17alpha,20S,24Z)-3-(hydroxyimino)lanosta-7,24-dien-26-oate competitive inhibition 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
-
?

Synonyms

Synonyms Comment Organism
CatL
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.002
-
3-(hydroxyimino)oleanolic acid at pH 5.5 and 37°C Homo sapiens
0.00923
-
3-(hydroxyimino)masticadienoic acid at pH 5.5 and 37°C Homo sapiens
0.0195
-
3-epiursolic acid at pH 5.5 and 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00003
-
at pH 5.5 and 37°C Homo sapiens E-64
0.0024
-
at pH 5.5 and 37°C Homo sapiens 3-(hydroxyimino)oleanolic acid
0.0026
-
at pH 5.5 and 37°C Homo sapiens 3-(hydroxyimino)masticadienoic acid
0.0065
-
at pH 5.5 and 37°C Homo sapiens 3-epiursolic acid
0.0072
-
at pH 5.5 and 37°C Homo sapiens 3-hydroxyolean-12-en-28-oic acid
0.0082
-
at pH 5.5 and 37°C Homo sapiens (13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oic acid
0.0083
-
at pH 5.5 and 37°C Homo sapiens 3-oxours-12-en-28-oic acid
0.0091
-
at pH 5.5 and 37°C Homo sapiens (13alpha,17alpha,20S,24Z)-3-oxolanosta-7,24-dien-26-oic acid
0.0097
-
at pH 5.5 and 37°C Homo sapiens (3E)-3-(carboxymethylidene)olean-12-en-28-oic acid
0.0123
-
at pH 5.5 and 37°C Homo sapiens (3E)-3-(carboxymethylidene)urs-12-en-28-oic acid
0.0147
-
at pH 5.5 and 37°C Homo sapiens 3-oxoolean-12-en-28-oic acid
0.0395
-
at pH 5.5 and 37°C Homo sapiens 3-hydroxyurs-12-en-28-oic acid
0.25
-
IC50 above 0.25 mM, at pH 5.5 and 37°C Homo sapiens methyl (13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oate
0.5
-
IC50 above 0.5 mM, at pH 5.5 and 37°C Homo sapiens (2E)-[(3E)-28-methoxy-28-oxours-12-en-3-ylidene]acetic acid
0.5
-
IC50 above 0.5 mM, at pH 5.5 and 37°C Homo sapiens methyl (3Z,13alpha,17alpha,20S,24Z)-3-(hydroxyimino)lanosta-7,24-dien-26-oate