Article
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315.
Journal of medicinal chemistry - 9 Aug 2018
Jakob Clarissa G, Upadhyay Anup K, Donner Pamela L, Nicholl Emily, Addo Sadiya N, Qiu Wei, Ling Christopher, Gopalakrishnan Sujatha M, Torrent Maricel, Cepa Steven P, Shanley Jason, Shoemaker Alexander R, Sun Chaohong C, Vasudevan Anil, Woller Kevin R, Shotwell J Brad, Shaw Bailin, Bian Zhiguo, Hutti Jessica E
Abstract excerpt
IDH1 plays a critical role in a number of metabolic processes and serves as a key source of cytosolic NADPH under conditions of cellular stress. However, few inhibitors of wild-type IDH1 have been reported. Here we present the discovery and biochemical characterization of two novel inhibitors of wild-type IDH1. In addition, we present the first ligand-bound crystallographic characterization of these novel small...
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