title: Releasing the block: setting differentiation free with mutant IDH inhibitors.
abstract: Hotspot mutations in IDH1 and IDH2 cause a differentiation block that can promote tumorigenesis. Two recent papers reported that small molecules targeting mutant IDH1 or mutant IDH2 release this differentiation block and/or impede tumor growth, providing a proof-of-concept that mutant IDHs are therapeutically targetable and that their effects are reversible.
authors.affiliation: The Preston Robert Tisch Brain Tumor Center at Duke, Pediatric Brain Tumor Foundation Institute at Duke, Department of Pathology, Duke University Medical Center, Durham, NC 27710, USA.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Pirozzi
authors.forename: Zachary J
authors.initials: ZJ
authors.lastname: Reitman
authors.forename: Hai
authors.initials: H
authors.lastname: Yan
mesh_terms: D000818:Animals; D044482:Benzeneacetamides / Q000494:pharmacology*; D002454:Cell Differentiation; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005910:Glioma / Q000201:enzymology* / Q000473:pathology*; D006410:Hematopoiesis / Q000187:drug effects*; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology*; D007521:Isocitrate Dehydrogenase / Q000037:antagonists & inhibitors* / Q000235:genetics*; D015470:Leukemia, Myeloid, Acute / Q000201:enzymology*; D010671:Phenylurea Compounds / Q000494:pharmacology*; D013449:Sulfonamides / Q000494:pharmacology*
chemical_list: D044482:Benzeneacetamides; D004791:Enzyme Inhibitors; D007093:Imidazoles; D010671:Phenylurea Compounds; D013449:Sulfonamides; D007521:Isocitrate Dehydrogenase