化学
融合蛋白
癌症研究
蛋白质-蛋白质相互作用
融合基因
小分子
白血病
计算生物学
基因
生物化学
遗传学
生物
重组DNA
作者
Hao Lei,San‐Qi Zhang,Songqing Fan,Huanrong Bai,Hongshan Zhao,Shuai Mao,Minhang Xin
标识
DOI:10.1021/acs.jmedchem.1c00872
摘要
Mixed lineage leukemia (MLL) gene rearrangements are associated with acute leukemia. The protein menin is regarded as a critical oncogenic cofactor of the resulting MLL fusion proteins in acute leukemia. A direct interaction between menin and the MLL amino terminal sequences is necessary for MLL fusion protein-mediated leukemogenesis. Thus, inhibition of the interaction between menin and MLL has emerged as a novel therapeutic strategy. Recent improvements in structural biology and chemical reactivity have promoted the design and development of selective and potent menin-MLL interaction inhibitors. In this Perspective, different classes of menin-MLL interaction inhibitors are comprehensively summarized. Further research potential, challenges, and opportunities in the field are also discussed.
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