Tethering identifies fragment that yields potent inhibitors of human caspase-1

…, T O'Brien, P Pham, ND Waal, S Baskaran…

Index: Fahr, Bruce T.; O'Brien, Tom; Pham, Phuongly; Waal, Nathan D.; Baskaran, Subramanian; Raimundo, Brian C.; Lam, Joni W.; Sopko, Michelle M.; Purkey, Hans E.; Romanowski, Michael J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 3 p. 559 - 562

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Citation Number: 22

Abstract

Disulfide Tethering® was applied to the active site of human caspase-1, resulting in the discovery of a novel, tricyclic molecular fragment that selectively binds in S4. This fragment was developed into a class of potent inhibitors of human caspase-1. Several key ...