期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 23, 页码 4958-4960出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm025581c
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资金
- NIGMS NIH HHS [GM54401, GM61964] Funding Source: Medline
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 SS 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.
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