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Literature summary for 3.4.22.1 extracted from

  • Spencer, J.; Casini, A.; Zava, O.; Rathnam, R.P.; Velhanda, S.K.; Pfeffer, M.; Callear, S.K.; Hursthouse, M.B.; Dyson, P.J.
    Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles (2009), Dalton Trans., 2009, 10731-10735.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
additional information correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles, that show in vitro activity as cytotoxic agents on A2780/S cells and also as cathepsin B inhibitors, synthesis and crystal structure of palladacycles, overview Bos taurus
additional information correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles, that show in vitro activity as cytotoxic agents on A2780/S cells and also as cathepsin B inhibitors, synthesis and crystal structure of palladacycles, overview Homo sapiens
[(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
-
Bos taurus
[(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)Pd(1,3,5-triaza-7-phosphoadamantane)Cl]
-
Homo sapiens
[(benzyl(methyl)sulfane)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
-
Bos taurus
[(benzyl(methyl)sulfane)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
-
Homo sapiens
[(N,N-dimethyl-1-phenylmethanamine)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
-
Bos taurus
[(N,N-dimethyl-1-phenylmethanamine)Pd(1,3,5-triaza-7-phosphoadamantane)Cl]
-
Homo sapiens
[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
-
Bos taurus
[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
-
Homo sapiens
[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
-
Bos taurus
[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
-
Homo sapiens
[Pd2((S)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
-
Bos taurus
[Pd2((S)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
-
Homo sapiens
[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
-
Bos taurus
[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
-
Homo sapiens
[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
-
Bos taurus
[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
-
Homo sapiens

Localization

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

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A2780/S cell an ovarian cancer cell line Homo sapiens
-
commercial preparation
-
Bos taurus
-
spleen
-
Bos taurus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-benzyloxycarbonyl-L-lysine 4-nitrophenyl ester + H2O
-
Homo sapiens ?
-
?
N-benzyloxycarbonyl-L-lysine 4-nitrophenyl ester + H2O
-
Bos taurus ?
-
?

Synonyms

Synonyms Comment Organism
More cathespsin B belongs to the papain-family of cysteine proteases Homo sapiens
More cathespsin B belongs to the papain-family of cysteine proteases Bos taurus

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
IC50 values of palladacycles in cytotoxicity assay, overview Homo sapiens additional information
0.0000095
-
pH 6.0, 30°C Bos taurus [Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
0.000012
-
pH 6.0, 30°C Bos taurus [Pd2((S)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
0.000023
-
pH 6.0, 30°C Bos taurus [Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
0.00003
-
pH 6.0, 30°C Bos taurus [Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
0.000038
-
pH 6.0, 30°C Bos taurus [Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
0.00007
-
pH 6.0, 30°C Bos taurus [(N,N-dimethyl-1-phenylmethanamine)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
0.00015
-
pH 6.0, 30°C Bos taurus [(benzyl(methyl)sulfane)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
0.0002
-
pH 6.0, 30°C Bos taurus [(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]

General Information

General Information Comment Organism
malfunction cathepsin B is involved in several cancers Homo sapiens
malfunction cathepsin B is involved in several cancers Bos taurus