Uttarkar Sagar, Frampton Jon, Klempnauer Karl-Heinz
Institute of Oncology Research, Bellinzona, Switzerland.
Institute of Cancer and Genomic Sciences, College of Medical and Dental Sciences, University of Birmingham, Edgbaston, Birmingham, United Kingdom.
Exp Hematol. 2017 Mar;47:31-35. doi: 10.1016/j.exphem.2016.12.003. Epub 2016 Dec 23.
The transcription factor Myb is a key regulator of hematopoietic cell proliferation, differentiation, and survival and has been implicated in the development of leukemia and several other human cancers. Pharmacological inhibition of Myb is therefore emerging as a potential therapeutic strategy. Recently, the first low-molecular-weight compounds that show Myb inhibitory activity have been identified. Characterization of these compounds suggests disruption of the protein-protein-interaction of Myb and the coactivator p300 as a suitable strategy to inhibit Myb.
转录因子Myb是造血细胞增殖、分化和存活的关键调节因子,与白血病和其他几种人类癌症的发生有关。因此,对Myb的药理学抑制正成为一种潜在的治疗策略。最近,已鉴定出首批具有Myb抑制活性的低分子量化合物。对这些化合物的特性分析表明,破坏Myb与共激活因子p300之间的蛋白质-蛋白质相互作用是抑制Myb的一种合适策略。