Non-Peptidic Small Molecule Inhibitors Against Bcl-2 for Cancer Therapy

被引：109

作者：

Azmi, Asfar S. ^{[2
]}

Mohammad, Ramzi M. ^{[1
]}

机构：

[1] Wayne State Univ, Sch Med, Dept Internal Med, Div Hematol & Oncol & Internal Med,Karmanos Canc, Detroit, MI 48201 USA

[2] Wayne State Univ, Sch Med, Dept Pathol, Detroit, MI 48201 USA

来源：

JOURNAL OF CELLULAR PHYSIOLOGY | 2009年 / 218卷 / 01期

基金：

芬兰科学院;

关键词：

FAMILY PROTEINS; BH3; DOMAIN; CELL-DEATH; BH3-ONLY PROTEINS; ANTIMYCIN-A; IN-VIVO; APOPTOSIS; BAX; CHELERYTHRINE; BINDING;

D O I：

10.1002/jcp.21567

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

A critical regulator of the apoptotic machinery is the Bcl-2 family proteins whose over expression confers a protective effect on malignant cells against death signals of apoptosis. Cancer cells that are resistant to various anti-cancer drugs and treatment regimen are found to over express these Bcl-2 proteins such as Bcl-2, Bcl-X-L, Mcl-1, Bcl-w, and AI/Bfl1. In recent years there has been an exponential growth in the identification as well as synthesis of non-peptidic cell permeable small-molecule inhibitors (SMIs) of protein-protein interaction. The focus of this article is on inhibitors of anti-apoptotic protein Bcl-2. This review summarizes an up to date knowledge of the available SMIs their mode of action as well as their current status in preclinical as well as clinical development.

引用

页码：13 / 21

页数：9

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