Aza-Peptide Epoxides: A New Class of Inhibitors Selective for Clan CD Cysteine Proteases
| Autor: | Wendy Carter, Zhao Zhao Li, Jowita Mikolajczyk, Alan J. Barrett, James C. Powers, Juliana L. Asgian, Guy S. Salvesen, Karen Ellis James |
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| Rok vydání: | 2002 |
| Předmět: |
Proteases
Stereochemistry medicine.medical_treatment Cysteine Proteinase Inhibitors Crystallography X-Ray Legumain Cathepsin B Structure-Activity Relationship chemistry.chemical_compound Papain Drug Discovery medicine Caspase Plant Proteins chemistry.chemical_classification Cathepsin Aza Compounds Protease Chymotrypsin biology Stereoisomerism General Medicine Caspase Inhibitors Cysteine Endopeptidases Kinetics Enzyme chemistry Biochemistry Enzyme inhibitor biology.protein Epoxy Compounds Molecular Medicine Oligopeptides Cysteine |
| Zdroj: | Journal of Medicinal Chemistry. 45:4958-4960 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | Aza-peptide epoxides, a new class of irreversible protease inhibitors, are specific for the clan CD cysteine proteases. The inhibitors have second-order rate constants up to 10(5) M(-1) s(-1), with the most potent epoxides having the S,S stereochemistry. The aza-Asn derivatives are effective legumain inhibitors, while the aza-Asp epoxides were specific for caspases. The inhibitors have little or no inhibition with other proteases such as chymotrypsin, papain, or cathepsin B. |
| Databáze: | OpenAIRE |
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