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
相关论文
共 93 条
[81]
Evaluation and critical assessment of putative MCL-1 inhibitors [J].
Varadarajan, S. ;
Vogler, M. ;
Butterworth, M. ;
Dinsdale, D. ;
Walensky, L. D. ;
Cohen, G. M. .
CELL DEATH AND DIFFERENTIATION, 2013, 20 (11) :1475-1484
[82]
Different forms of cell death induced by putative BCL2 inhibitors [J].
Vogler, M. ;
Weber, K. ;
Dinsdale, D. ;
Schmitz, I. ;
Schulze-Osthoff, K. ;
Dyer, M. J. S. ;
Cohen, G. M. .
CELL DEATH AND DIFFERENTIATION, 2009, 16 (07) :1030-1039
[83]
The rheostat in the membrane: BCL-2 family proteins and apoptosis [J].
Volkmann, N. ;
Marassi, F. M. ;
Newmeyer, D. D. ;
Hanein, D. .
CELL DEATH AND DIFFERENTIATION, 2014, 21 (02) :206-215
[84]
Chemical Genomics Identifies Small-Molecule MCL1 Repressors and BCL-xL as a Predictor of MCL1 Dependency [J].
Wei, Guo ;
Margolin, Adam A. ;
Haery, Leila ;
Brown, Emily ;
Cucolo, Lisa ;
Julian, Bina ;
Shehata, Shyemaa ;
Kung, Andrew L. ;
Beroukhim, Rameen ;
Golub, Todd R. .
CANCER CELL, 2012, 21 (04) :547-562
[85]
Inducing apoptosis and enhancing chemosensitivity to Gemcitabine via RNA interference targeting Mcl-1 gene in pancreatic carcinoma cell [J].
Wei, San-Hua ;
Dong, Ke ;
Lin, Fang ;
Wang, Xi ;
Li, Bin ;
Shen, Jian-jun ;
Zhang, Qing ;
Wang, Rui ;
Zhang, Hui-Zhong .
CANCER CHEMOTHERAPY AND PHARMACOLOGY, 2008, 62 (06) :1055-1064
[86]
Sensitivity to antitubulin chemotherapeutics is regulated by MCL1 and FBW7 [J].
Wertz, Ingrid E. ;
Kusam, Saritha ;
Lam, Cynthia ;
Okamoto, Toru ;
Sandoval, Wendy ;
Anderson, Daniel J. ;
Helgason, Elizabeth ;
Ernst, James A. ;
Eby, Mike ;
Liu, Jinfeng ;
Belmont, Lisa D. ;
Kaminker, Josh S. ;
O'Rourke, Karen M. ;
Pujara, Kanan ;
Kohli, Pawan Bir ;
Johnson, Adam R. ;
Chiu, Mark L. ;
Lill, Jennie R. ;
Jackson, Peter K. ;
Fairbrother, Wayne J. ;
Seshagiri, Somasekar ;
Ludlam, Mary J. C. ;
Leong, Kevin G. ;
Dueber, Erin C. ;
Maecker, Heather ;
Huang, David C. S. ;
Dixit, Vishva M. .
NATURE, 2011, 471 (7336) :110-114
[87]
Mcl-1: a highly regulated cell death and survival controller [J].
Yang-Yen, HF .
JOURNAL OF BIOMEDICAL SCIENCE, 2006, 13 (02) :201-204
[88]
The BCL-2 protein family: opposing activities that mediate cell death [J].
Youle, Richard J. ;
Strasser, Andreas .
NATURE REVIEWS MOLECULAR CELL BIOLOGY, 2008, 9 (01) :47-59
[89]
Novel Bcl-2 inhibitors: Discovery and mechanism study of small organic apoptosis-inducing agents [J].
Zhang, Zhichao ;
Jin, Liji ;
Qian, Xuhong ;
Wei, Meijiao ;
Wang, Yuanyuan ;
Wang, Jing ;
Yang, Yuanyuan ;
Xu, Qin ;
Xu, Yongting ;
Liu, Fengyu .
CHEMBIOCHEM, 2007, 8 (01) :113-121
[90]
Fragment-based design, synthesis, and biological evaluation of N-substituted-5-(4-isopropylthiophenol)-2-hydroxynicotinamide derivatives as novel Mcl-1 inhibitors [J].
Zhang, Zhichao ;
Liu, Chengwu ;
Li, Xiangqian ;
Song, Ting ;
Wu, Zhiyong ;
Liang, Xiaomeng ;
Zhao, Yan ;
Shen, Xiaoyun ;
Chen, Hongbo .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 60 :410-420