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《MEIN 抑制剂:Menin-MLL 抑制可消除 NPM1 突变和 MLL 重排的急性白血病小鼠模型》

It's All About MEis: Menin-MLL Inhibition Eradicates NPM1-Mutated and MLL-Rearranged Acute Leukemias in Mice.

机构信息

Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX, USA.

Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX, USA; Molecular and Human Genetics, Baylor College of Medicine, Houston, TX, USA; Center for Cell and Gene Therapy, Baylor College of Medicine, Houston, TX, USA; Stem Cell and Regenerative Medicine, Baylor College of Medicine, Houston, TX, USA.

出版信息

Cancer Cell. 2020 Mar 16;37(3):267-269. doi: 10.1016/j.ccell.2020.02.011.

Abstract

Several acute myeloid leukemia genetic sub-types converge on high expression of HOX genes, critical for their self-renewal. A new orally bioavailable Menin-MLL inhibitor (VTP-50469) appears to promote their differentiation through direct effects on the HOX cofactor MEIS1, paving the way for clinical trials.

摘要

几种急性髓系白血病的遗传亚型集中在 HOX 基因的高表达上,这些基因对于白血病的自我更新至关重要。一种新的口服生物利用度的 Menin-MLL 抑制剂(VTP-50469)似乎通过对 HOX 共激活因子 MEIS1 的直接作用来促进其分化,为临床试验铺平了道路。

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