New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.

doi:10.1038/nchembio.1930

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Article

New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.

Nature chemical biology - 1 Nov 2015

Okoye-Okafor Ujunwa C, Bartholdy Boris, Cartier Jessy, Gao Enoch N, Pietrak Beth, Rendina Alan R, Rominger Cynthia, Quinn Chad, Smallwood Angela, Wiggall Kenneth J, Reif Alexander J, Schmidt Stanley J, Qi Hongwei, Zhao Huizhen, Joberty Gerard, Faelth-Savitski Maria, Bantscheff Marcus, Drewes Gerard, Duraiswami Chaya, Brady Pat, Groy Arthur, Narayanagari Swathi-Rao, Antony-Debre Iléana, Mitchell Kelly, Wang Heng Rui, Kao Yun-Ruei, Christopeit Maximilian, Carvajal Luis, Barreyro Laura, Paietta Elisabeth, Makishima Hideki, Will Britta, Concha Nestor, Adams Nicholas D, Schwartz Benjamin, McCabe Michael T, Maciejewski Jaroslav, Verma Amit, Steidl Ulrich

Abstract excerpt

Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are driver mutations in acute myeloid leukemia (AML) and other cancers. We report the development of new allosteric inhibitors of mutant IDH1. Crystallographic and biochemical results demonstrated that compounds of this chemical series bind to an allosteric site and lock the enzyme in a catalytically inactive conformation, thereby enabling inhibition of...

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PMID: 26436839
DOI: 10.1038/nchembio.1930
PMCID: PMC5155016

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IDH1

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