Discovery, development and application of drugs targeting BCL-2 pro-survival proteins in cancer

被引：6

作者：

Lee, Erinna F. ^{[1
,2
,3
]}

Fairlie, W. Douglas ^{[1
,2
,3
]}

机构：

[1] La Trobe Univ, La Trobe Inst Mol Sci, Melbourne, Vic 3086, Australia

[2] Olivia Newton John Canc Res Inst, Cell Death & Survival Lab, Heidelberg, Vic 3084, Australia

[3] La Trobe Univ, Sch Canc Med, Bundoora, Vic 3086, Australia

来源：

BIOCHEMICAL SOCIETY TRANSACTIONS | 2021年 / 49卷 / 05期

基金：

英国医学研究理事会;

关键词：

CHRONIC LYMPHOCYTIC-LEUKEMIA; SELECTIVE SMALL-MOLECULE; STRUCTURE-GUIDED DESIGN; ANTI-APOPTOTIC MCL-1; BH3 MIMETIC ABT-737; X-L; CYTOCHROME-C; IN-VIVO; HIGH-AFFINITY; CELL-DEATH;

D O I：

10.1042/BST20210749

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The discovery of a new class of small molecule compounds that target the BCL-2 family of anti-apoptotic proteins is one of the great success stories of basic science leading to translational outcomes in the last 30 years. The eponymous BCL-2 protein was identified over 30 years ago due to its association with cancer. However, it was the unveiling of the biochemistry and structural biology behind it and its close relatives' mechanism(s)-ofaction that provided the inspiration for what are now known as 'BH3-mimetics', the first clinically approved drugs designed to specifically inhibit protein-protein interactions. Herein, we chart the history of how these drugs were discovered, their evolution and application in cancer treatment.

引用

页码：2381 / 2395

页数：15

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