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Literature summary for 3.4.22.15 extracted from

  • Takahashi, K.; Ueno, T.; Tanida, I.; Minematsu-Ikeguchi, N.; Murata, M.; Kominami, E.
    Characterization of CAA0225, a novel inhibitor specific for cathepsin L, as a probe for autophagic proteolysis (2009), Biol. Pharm. Bull., 32, 475-479.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide] i.e. CAA0225. Significantly inhibits degradation of long-lived proteins in HeLa and Huh-7 cells cultured under nutrient-deprived conditions. CAA0225 effectively inhibits degradation of microtubule-associated protein IA/IB light chain 3-II and gamma-aminobutyric acid (A) receptor-associated protein Homo sapiens
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide] i.e. CAA0225. IC50 value for rat liver cathepsin B above 1 microM Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens contributions of cathepsin L and cathepsin B to autophagic protein degradation of cytoplasmic proteins in HeLa and Huh-7 cells are nearly equal. Cathepsin L does not play a general role in the degradation of proteins in the lumen of autophagosomes, but rather is involved specifically in the degradation of autophagosomal membrane markers ?
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?

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Rattus norvegicus
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Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
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Homo sapiens
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Huh-7 cell
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Homo sapiens
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liver
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Rattus norvegicus
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O substrate for both cathepsin L and cathepsin B Homo sapiens benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
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?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O substrate for both cathepsin L and cathepsin B Rattus norvegicus benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
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?
additional information contributions of cathepsin L and cathepsin B to autophagic protein degradation of cytoplasmic proteins in HeLa and Huh-7 cells are nearly equal. Cathepsin L does not play a general role in the degradation of proteins in the lumen of autophagosomes, but rather is involved specifically in the degradation of autophagosomal membrane markers Homo sapiens ?
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000019
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-
Rattus norvegicus (2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]