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Literature summary for 3.4.22.1 extracted from

  • Casini, A.; Gabbiani, C.; Sorrentino, F.; Rigobello, M.P.; Bindoli, A.; Geldbach, T.J.; Marrone, A.; Re, N.; Hartinger, C.G.; Dyson, P.J.; Messori, L.
    Emerging protein targets for anticancer metallodrugs: inhibition of thioredoxin reductase and cathepsin B by antitumor ruthenium(II)-arene compounds (2008), J. Med. Chem., 51, 6773-6781.
    View publication on PubMed

Application

Application Comment Organism
drug development cathepsin B is a target for anticancer metallodrugs, inhibition of cathepsin B by antitumor ruthenium(II)-arene compounds, overview Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
additional information inhibition of cathepsin B by antitumor ruthenium(II)-arene compounds, mechanisms of binding/inhibition, overview Bos taurus
oxalo-RAPTA ruthenium(II)-arene compound Bos taurus
RAPTA-BC ruthenium(II)-arene compound Bos taurus
RAPTA-BI ruthenium(II)-arene compound Bos taurus
RAPTA-C i.e. carbo-RAPTA, ruthenium(II)-arene compound Bos taurus
RAPTA-H ruthenium(II)-arene compound Bos taurus
RAPTA-Me+C ruthenium(II)-arene compound Bos taurus
RAPTA-NH3 ruthenium(II)-arene compound Bos taurus
RAPTA-OH ruthenium(II)-arene compound Bos taurus
RAPTA-pentaOH binding structure from cyrstal structure of the inhibitor bound to cathepsin B, overview Bos taurus
RAPTA-T ruthenium(II)-arene compound Bos taurus
RAPTA-TBMe ruthenium(II)-arene compound Bos taurus
RAPTA-TBOH ruthenium(II)-arene compound Bos taurus

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
Bos taurus 5764
-

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Bos taurus
-
spleen
-
Bos taurus
-

Synonyms

Synonyms Comment Organism
cat B
-
Bos taurus
More cathepsin B is a cysteine peptidase of the papain family Bos taurus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Bos taurus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
assay at Bos taurus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0015
-
pH 6.0, 30°C Bos taurus RAPTA-T
0.0016
-
pH 6.0, 30°C Bos taurus RAPTA-OH
0.0025
-
pH 6.0, 30°C Bos taurus RAPTA-C
0.003
-
pH 6.0, 30°C Bos taurus RAPTA-NH3
0.005
-
pH 6.0, 30°C Bos taurus RAPTA-BC
0.0065
-
pH 6.0, 30°C Bos taurus RAPTA-Me+C
0.007
-
pH 6.0, 30°C Bos taurus RAPTA-pentaOH
0.0245
-
pH 6.0, 30°C Bos taurus RAPTA-TBOH
0.082
-
pH 6.0, 30°C Bos taurus RAPTA-TBMe
0.1
-
above, pH 6.0, 30°C Bos taurus RAPTA-BI
0.2
-
above, pH 6.0, 30°C Bos taurus oxalo-RAPTA
0.2
-
above, pH 6.0, 30°C Bos taurus RAPTA-H