Article
Acquired resistance to IDH inhibition through trans or cis dimer-interface mutations.
Nature - 1 Jul 2018
Intlekofer Andrew M, Shih Alan H, Wang Bo, Nazir Abbas, Rustenburg Ariën S, Albanese Steven K, Patel Minal, Famulare Christopher, Correa Fabian M, Takemoto Naofumi, Durani Vidushi, Liu Hui, Taylor Justin, Farnoud Noushin, Papaemmanuil Elli, Cross Justin R, Tallman Martin S, Arcila Maria E, Roshal Mikhail, Petsko Gregory A, Wu Bin, Choe Sung, Konteatis Zenon D, Biller Scott A, Chodera John D, Thompson Craig B, Levine Ross L, Stein Eytan M
Abstract excerpt
Somatic mutations in the isocitrate dehydrogenase 2 gene (IDH2) contribute to the pathogenesis of acute myeloid leukaemia (AML) through the production of the oncometabolite 2-hydroxyglutarate (2HG)1-8. Enasidenib (AG-221) is an allosteric inhibitor that binds to the IDH2 dimer interface and blocks the production of 2HG by IDH2 mutants9,10. In a phase I/II clinical trial, enasidenib inhibited the production of 2HG...
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