Literature summary for 3.4.22.1 extracted from

Huryn, D.M.; Smith, A.B.
The identification, characterization and optimization of small molecule probes of cysteine proteases: experiences of the Penn center for molecular discovery with cathepsin B and cathepsin L (2009), Curr. Top. Med. Chem., 9, 1206-1216.

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Inhibitors

Inhibitors	Comment	Organism	Structure
CID 647501	-	Homo sapiens
CID 653297	-	Homo sapiens
CID 66541	-	Homo sapiens
additional information	screening of pyrimidotriazine-diones and pyrazole sulfonamides as cathepsin B inhibitors, structure-function relationship, overview. Pyrimidotriazine-dione inhibitors, along with several structurally unrelated compounds, are inactive in presence of the reductant cysteine or DTT, thus the inhibitors are acting through a DTT-dependent redox cycling mechanism, rather than through direct inhibition of the enzyme	Homo sapiens

Localization

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
liver	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	the assay uses a modified aminomethylcoumarin dipeptide substrate, which generates a fluorescent signal upon cleavage by cathepsin B	Homo sapiens	?	-	?

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000046	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	CID 66541
0.000071	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	CID 647501
0.000072	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	CID 653297

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Release 2023.1 (January 2023)