抗凋亡 Bcl-2 家族蛋白选择性抑制剂的兴起。

Rise of the selective inhibitors of anti-apoptotic Bcl-2 family proteins.

机构信息

State Key Laboratory of Bioorganic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China.

出版信息

ChemMedChem. 2013 Sep;8(9):1437-40. doi: 10.1002/cmdc.201300301. Epub 2013 Jul 31.

DOI:10.1002/cmdc.201300301

PMID:23907935

Abstract

No trivial pursuit! It is not trivial to develop effective small-molecule regulators of protein-protein interactions (PPIs). Moreover, anti-apoptotic Bcl-2 family proteins share similar binding grooves, making it particularly difficult to target them selectively. Despite these challenges, potent and selective inhibitors of individual members of the Bcl-2 family have been successfully developed.

摘要

切勿轻视！开发有效的蛋白质-蛋白质相互作用（PPI）小分子调节剂并非易事。此外，抗凋亡 Bcl-2 家族蛋白具有相似的结合凹槽，因此特别难以进行选择性靶向。尽管存在这些挑战，但已经成功开发出针对 Bcl-2 家族个别成员的有效且选择性抑制剂。