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Literature summary for 3.4.22.16 extracted from

  • Garg, S.; Raghav, N.
    Inhibitory potential of some chalcones on cathepsins B, H and L (2015), RSC Adv., 5, 72937-72949 .
No PubMed abstract available

Inhibitors

Inhibitors Comment Organism Structure
3-(2-chlorophenyl)-1-(4-bromophenyl)prop-2-en-1-one
-
Capra hircus
3-(2-chlorophenyl)-1-(naphthalen-3-yl)prop-2-en-1-one
-
Capra hircus
3-(2-chlorophenyl)-1-(pyridin-2-yl)prop-2-en-1-one
-
Capra hircus
3-(2-chlorophenyl)-1-(thien-2-yl)prop-2-en-1-one
-
Capra hircus
3-(3-chlorophenyl)-1-(4-aminophenyl)prop-2-en-1-one
-
Capra hircus
3-(3-chlorophenyl)-1-(4-fluorophenyl)prop-2-en-1-one
-
Capra hircus
3-(3-chlorophenyl)-1-(4-hydroxyphenyl)-prop-2-en-1-one
-
Capra hircus
3-(3-chlorophenyl)-1-(furan-2-yl)prop-2-en-1-one
-
Capra hircus
3-(4-chlorophenyl)-1-(4-(N'-4-nitrophenyl)methylene)aminophenyl)prop-2-en-1-one
-
Capra hircus
3-(4-chlorophenyl)-1-(4-methylphenyl)prop-2-en-1-one
-
Capra hircus
3-(4-chlorophenyl)-1-(4-nitrophenyl)prop-2-en-1-one
-
Capra hircus
additional information synthesis of a small library of chalcones and study of their role as inhibitors of cathepsins, overview. The most potent inhibitors among all compounds are chloro-substituted compounds for cathepsin H. Docking analysis and modeling, overview Capra hircus

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
Capra hircus 5764
-

Organism

Organism UniProt Comment Textmining
Capra hircus A0A060INS8
-
-

Purification (Commentary)

Purification (Comment) Organism
native enzyme from liver homogenate by acetone powder preparation, acid autolysis, ammonium sulfate fractionation, gel filtration, cation exchange and anion exchange chromatography, and again gel filtration Capra hircus

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Capra hircus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.02291
-
purified native enzyme, pH 5.0, 37°C Capra hircus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Leu-2-naphthylamide + H2O
-
Capra hircus leucine + 2-naphthylamine
-
?

Synonyms

Synonyms Comment Organism
CTSH
-
Capra hircus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Capra hircus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5
-
assay at Capra hircus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0133
-
3-(4-chlorophenyl)-1-(4-(N'-4-nitrophenyl)methylene)aminophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.0214
-
3-(2-chlorophenyl)-1-(4-bromophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.0317
-
3-(3-chlorophenyl)-1-(4-fluorophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.0416
-
3-(4-chlorophenyl)-1-(4-methylphenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.0472
-
3-(2-chlorophenyl)-1-(pyridin-2-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.0989
-
3-(2-chlorophenyl)-1-(naphthalen-3-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.128
-
3-(3-chlorophenyl)-1-(4-aminophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.163
-
3-(3-chlorophenyl)-1-(4-hydroxyphenyl)-prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.217
-
3-(2-chlorophenyl)-1-(thien-2-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.298
-
3-(3-chlorophenyl)-1-(furan-2-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
0.405
-
3-(4-chlorophenyl)-1-(4-nitrophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus