释放阻断：用突变 IDH 抑制剂设定分化自由。
Releasing the block: setting differentiation free with mutant IDH inhibitors.
机构信息
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.
出版信息
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.
摘要
IDH1 和 IDH2 热点突变导致分化阻滞，从而促进肿瘤发生。最近有两篇论文报道，靶向突变 IDH1 或突变 IDH2 的小分子可解除这种分化阻滞和/或抑制肿瘤生长，这为突变 IDH 是可治疗的靶点及其作用是可逆的这一观点提供了证据。
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IDH1(R132H) mutation increases murine haematopoietic progenitors and alters epigenetics.IDH1(R132H) 突变增加了小鼠造血祖细胞并改变了表观遗传学。
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