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…

Index: 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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Citation Number: 92

Abstract

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 ...

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