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Selective inhibition of mutant isocitrate dehydrogenase 1 (IDH1) via disruption of a metal binding network by an allosteric small molecule.

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第一作者： Gejing,Deng

第一单位： From Division of Oncology Drug Discovery and Preclinical Development, Sanofi, Cambridge, Massachusetts 02139, gejing.deng@sanofi.com.

作者： Gejing,Deng ^[1] ; Junqing,Shen ^[2] ; Ming,Yin ^[2] ; Jessica,McManus ^[2] ; Magali,Mathieu ^[3] ; Patricia,Gee ^[2] ; Timothy,He ^[2] ; Chaomei,Shi ^[2] ; Olivier,Bedel ^[2] ; Larry R,McLean ^[4] ; Frank,Le-Strat ^[5] ; Ying,Zhang ^[4] ; Jean-Pierre,Marquette ^[3] ; Qiang,Gao ^[2] ; Bailin,Zhang ^[2] ; Alexey,Rak ^[3] ; Dietmar,Hoffmann ^[2] ; Eamonn,Rooney ^[3] ; Aurelie,Vassort ^[3] ; Walter,Englaro ^[3] ; Yi,Li ^[4] ; Vinod,Patel ^[4] ; Francisco,Adrian ^[2] ; Stefan,Gross ^[2] ; Dmitri,Wiederschain ^[2] ; Hong,Cheng ^[2] ; Stuart,Licht ^[2]

作者单位： From Division of Oncology Drug Discovery and Preclinical Development, Sanofi, Cambridge, Massachusetts 02139, gejing.deng@sanofi.com. ^[1] From Division of Oncology Drug Discovery and Preclinical Development, Sanofi, Cambridge, Massachusetts 02139. ^[2] Division of Lead Generation & Compound Realization, Sanofi, Vitry 94403, France. ^[3] Division of Lead Generation & Compound Realization, Sanofi, Waltham, Massachusetts 02452, and. ^[4] Department of Disposition, Safety & Animal Research, Sanofi, Chilly-Mazarin 91385, France. ^[5]

关键词 Anticancer Drug Cancer Metabolism Drug Action Drug Discovery Enzyme Inhibitor IDH1 Inhibitor Mechanism of Inhibition Metalloenzyme