一种用于杀死癌细胞的 BH3 模拟物。

A BH3 Mimetic for Killing Cancer Cells.

机构信息

Department of Immunology, St. Jude Children's Research Institute, Memphis, TN 38105, USA.

出版信息

Cell. 2016 Jun 16;165(7):1560. doi: 10.1016/j.cell.2016.05.080.

DOI:10.1016/j.cell.2016.05.080

Abstract

Venetoclax is a BH3 mimetic approved for treating chronic lymphocytic leukemia. Cancer cells are resistant to apoptosis but "primed for death" by elevated BCL-2, which binds to pro-apoptotic proteins and holds them in check. Venetoclax releases this antagonism and is the first approved drug to target a protein-protein interaction.

摘要

维奈托克是一种 BH3 拟肽，获批用于治疗慢性淋巴细胞白血病。癌细胞对细胞凋亡具有抗性，但由于 BCL-2 的升高而“为死亡做好准备”，BCL-2 与促凋亡蛋白结合并抑制它们。维奈托克释放这种拮抗作用，是首个获批靶向蛋白-蛋白相互作用的药物。