Small molecule Mcl-1 inhibitors for the treatment of cancer

被引:145
作者
Belmar, Johannes [1 ]
Fesik, Stephen W. [1 ]
机构
[1] Vanderbilt Univ, Sch Med, Dept Biochem, Nashville, TN 37232 USA
关键词
Mcl-1; Myeloid cell leukemia-1; Inhibitors; Small molecule; BH3-mimetic; CELL LUNG-CANCER; BCL-2 FAMILY PROTEINS; ANTI-APOPTOTIC MCL-1; BH3 MIMETIC ABT-737; TARGETING MCL-1; MELANOMA-CELLS; IMMUNOHISTOCHEMICAL ANALYSIS; BIOLOGICAL EVALUATION; RATIONAL DESIGN; RESISTANCE;
D O I
10.1016/j.pharmthera.2014.08.003
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
The Bcl-2 family of proteins serves as primary regulators of apoptosis. Myeloid cell leukemia 1 (Mcl-1), a prosurvival member of the Bcl-2 family of proteins, is overexpressed and the Mcl-1 gene is amplified in many tumor types. Moreover, the overexpression of Mcl-1 is the cause of resistance to several chemotherapeutic agents. Thus, Mcl-1 is a promising cancer target. This review highlights the current progress on the discovery of small molecule Mcl-1 inhibitors. (C) 2014 Elsevier Inc. All rights reserved.
引用
收藏
页码:76 / 84
页数:9
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