Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design

…, Z Fang, W Macchia, L Zhu, MP Capparelli…

文献索引：Greenspan; Clark; Tommasi; Cowen; McQuire; Farley; Van Duzer; Goldberg; Zhou; Du; Fitt; Coppa; Fang; Macchia; Zhu; Capparelli; Goldstein; Wigg; Doughty; Bohacek; Knap Journal of Medicinal Chemistry, 2001 , vol. 44, # 26 p. 4524 - 4534

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被引用次数: 92

摘要

Cathepsin B is a member of the papain superfamily of cysteine proteases and has been implicated in the pathology of numerous diseases, including arthritis and cancer. As part of an effort to identify potent, reversible inhibitors of this protease, we examined a series of dipeptidyl nitriles, starting with the previously reported Cbz-Phe-NH-CH2CN (19, IC50= 62 μM). High-resolution X-ray crystallographic data and molecular modeling were used to ...