Releasing the block: setting differentiation free with mutant IDH inhibitors

Cancer Cell. 2013 May 13;23(5):570-2. doi: 10.1016/j.ccr.2013.04.024.

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.

Publication types

  • Comment

MeSH terms

  • Animals
  • Benzeneacetamides / pharmacology*
  • Cell Differentiation*
  • Enzyme Inhibitors / pharmacology*
  • Glioma / enzymology*
  • Glioma / pathology*
  • Hematopoiesis / drug effects*
  • Humans
  • Imidazoles / pharmacology*
  • Isocitrate Dehydrogenase / antagonists & inhibitors*
  • Isocitrate Dehydrogenase / genetics*
  • Leukemia, Myeloid, Acute / enzymology*
  • Phenylurea Compounds / pharmacology*
  • Sulfonamides / pharmacology*

Substances

  • Benzeneacetamides
  • Enzyme Inhibitors
  • Imidazoles
  • Phenylurea Compounds
  • Sulfonamides
  • Isocitrate Dehydrogenase