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Literature summary for 3.4.22.1 extracted from

  • Tomoo, K.
    Development of cathepsin inhibitors and structure-based design of cathepsin B-specific inhibitor (2010), Curr. Top. Med. Chem., 10, 696-707.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
benzylamido-L-trans-epoxysuccinyl-Ile-O-benzyl ester
-
Homo sapiens
benzylamido-L-trans-epoxysuccinyl-Ile-Pro-OH
-
Homo sapiens
CA-074-Me i.e. propylcarbonyl-L-trans-epoxysuccinyl-Ile-Pro-OH, enzyme binding structure at the active site cleft, modelling, overview Homo sapiens
CA030 i.e. ethoxy-L-trans-epoxysuccinyl-Ile-Pro-OH Homo sapiens
E64c the (2S,3S)-3-(L-[N-(3-methylbutyl)amino]leucyl) side chain binds at the S1 and S3 subsites Homo sapiens
ethoxy-L-trans-epoxysuccinyl-Gly-Pro-OH
-
Homo sapiens
ethoxy-L-trans-epoxysuccinyl-Ile-Ala-OH
-
Homo sapiens
ethoxy-L-trans-epoxysuccinyl-Ile-Ile-OH
-
Homo sapiens
ethoxy-L-trans-epoxysuccinyl-Ile-OH
-
Homo sapiens
ethoxy-L-trans-epoxysuccinyl-Thr-Ile-OH
-
Homo sapiens
additional information development of cathepsin inhibitors and structure-based design of cathepsin B-specific inhibitor, binding mode at the active site and structure-activity relationship, overview. Quantitative assesment of inhibitor binding at the SN-site of cathepsin B, overview Homo sapiens
propylcarbonyl-L-trans-epoxysuccinyl-Ile-O-benzyl ester
-
Homo sapiens
propylcarbonyl-L-trans-epoxysuccinyl-Ile-Pro-O-methyl ester
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
Homo sapiens 5764
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Reaction

Reaction Comment Organism Reaction ID
Hydrolysis of proteins with broad specificity for peptide bonds. Preferentially cleaves -Arg-Arg-/- bonds in small molecule substrates (thus differing from cathepsin L). In addition to being an endopeptidase, shows peptidyl-dipeptidase activity, liberating C-terminal dipeptides cathepsin B possesses a long and narrow substrate-binding active site cleft with catalytic residue Cys, the surfaces of the S1 and S1' subsites are negatively charged due to presence of Glu122 and Glu194, the occluding loop of residue 105-125 is a structural feature containing the two positively charged His residues, His110 and His111, overview Homo sapiens

Subunits

Subunits Comment Organism
More three-dimensional structure of cathepsin B in comparison to other cathepsins, it possesses a long and narrow substrate-binding active site cleft with catalytic residue Cys, the surfaces of the S1 and S1' subsites are negatively charged due to presence of Glu122 and Glu194, the occluding loop of residue 105-125 is a structural feature containing the two positively charged His residues, His110 and His111, overview Homo sapiens

Synonyms

Synonyms Comment Organism
More cathepsin B belongs to the lysosomal cysteine protease subgroup of the cathepsin family Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000023
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethoxy-L-trans-epoxysuccinyl-Ile-Ala-OH
0.000024
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethoxy-L-trans-epoxysuccinyl-Ile-Ile-OH
0.000029
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens benzylamido-L-trans-epoxysuccinyl-Ile-Pro-OH
0.000038
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens CA-074-Me
0.00012
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens CA030
0.00041
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethoxy-L-trans-epoxysuccinyl-Thr-Ile-OH
0.0091
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens propylcarbonyl-L-trans-epoxysuccinyl-Ile-O-benzyl ester
0.0153
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethoxy-L-trans-epoxysuccinyl-Gly-Pro-OH
0.024
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethoxy-L-trans-epoxysuccinyl-Ile-OH
0.046
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens benzylamido-L-trans-epoxysuccinyl-Ile-O-benzyl ester
0.068
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens propylcarbonyl-L-trans-epoxysuccinyl-Ile-Pro-O-methyl ester

General Information

General Information Comment Organism
malfunction cathepsin B is a major lysosomal protease, its overactivation is involved in muscular dystrophy, bone resorption, pulmonary emphysem, and tumor metastasis Homo sapiens