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Acquired resistance to IDH inhibition through trans or cis dimer-interface mutations

Somatic mutations in isocitrate dehydrogenase 2 (IDH2) contribute to the pathogenesis of acute myeloid leukemia (AML) through 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 2HG productio...

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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6121718/
https://www.ncbi.nlm.nih.gov/pubmed/29950729
http://dx.doi.org/10.1038/s41586-018-0251-7