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旨在杀伤:新型 Menin-MLL 抑制剂靶向 MLL 重排白血病。

Designed to kill: novel menin-MLL inhibitors target MLL-rearranged leukemia.

机构信息

Cancer Biology and Genetics Program and Department of Pediatrics, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA.

Cancer Biology and Genetics Program and Department of Pediatrics, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA.

出版信息

Cancer Cell. 2015 Apr 13;27(4):431-3. doi: 10.1016/j.ccell.2015.03.012.

Abstract

The interaction between menin and oncogenic mixed lineage leukemia (MLL) fusion proteins is required for leukemic transformation and may represent a therapeutic opportunity. In this issue of Cancer Cell, Borkin and colleagues describe the development of highly potent small-molecule inhibitors of this interaction that reverse the leukemic phenotype and prolong survival in murine models of MLL-rearranged leukemia.

摘要

Menin 与致癌性混合谱系白血病(MLL)融合蛋白之间的相互作用是白血病转化所必需的,这可能代表了一个治疗机会。在本期《癌细胞》杂志中,Borkin 及其同事描述了这种相互作用的高活性小分子抑制剂的开发,这些抑制剂可逆转白血病表型,并延长 MLL 重排白血病的小鼠模型的生存时间。

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