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

来源：

PHARMACOLOGY & THERAPEUTICS | 2015年 / 145卷

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

页码：76 / 84

页数：9

共 93 条

[71]

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets [J].

Souers, Andrew J. ;

Leverson, Joel D. ;

Boghaert, Erwin R. ;

Ackler, Scott L. ;

Catron, Nathaniel D. ;

Chen, Jun ;

Dayton, Brian D. ;

Ding, Hong ;

Enschede, Sari H. ;

Fairbrother, Wayne J. ;

Huang, David C. S. ;

Hymowitz, Sarah G. ;

Jin, Sha ;

Khaw, Seong Lin ;

Kovar, Peter J. ;

Lam, Lloyd T. ;

Lee, Jackie ;

Maecker, Heather L. ;

Marsh, Kennan C. ;

Mason, Kylie D. ;

Mitten, Michael J. ;

Nimmer, Paul M. ;

Oleksijew, Anatol ;

Park, Chang H. ;

Park, Cheol-Min ;

Phillips, Darren C. ;

Roberts, Andrew W. ;

Sampath, Deepak ;

Seymour, John F. ;

Smith, Morey L. ;

Sullivan, Gerard M. ;

Tahir, Stephen K. ;

Tse, Chris ;

Wendt, Michael D. ;

Xiao, Yu ;

Xue, John C. ;

Zhang, Haichao ;

Humerickhouse, Rod A. ;

Rosenberg, Saul H. ;

Elmore, Steven W. .

NATURE MEDICINE, 2013, 19 (02) :202-208

[72]

Stewart ML, 2010, NAT CHEM BIOL, V6, P595, DOI [10.1038/NCHEMBIO.391, 10.1038/nchembio.391]

[73]

Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737 [J].

Tahir, Stephen K. ;

Yang, Xiufen ;

Anderson, Mark G. ;

Morgan-Lappe, Susan E. ;

Sarthy, Aparna V. ;

Chen, Jun ;

Warner, Robert B. ;

ng, Shi-Chu Ng ;

Fesik, Stephen W. ;

Elmore, Steve W. ;

Rosenberg, Saul H. ;

Tse, Christin .

CANCER RESEARCH, 2007, 67 (03) :1176-1183

[74]

Discovery of Potent Mcl-1/Bcl-xL Dual Inhibitors by Using a Hybridization Strategy Based on Structural Analysis of Target Proteins [J].

Tanaka, Yuta ;

Aikawa, Katsuji ;

Nishida, Goushi ;

Homma, Misaki ;

Sogabe, Satoshi ;

Igaki, Shigeru ;

Hayano, Yumi ;

Sameshima, Tomoya ;

Miyahisa, Ikuo ;

Kawamoto, Tomohiro ;

Tawada, Michiko ;

Imai, Yumi ;

Inazuka, Masakazu ;

Cho, Nobuo ;

Imaeda, Yasuhiro ;

Ishikawa, Tomoyasu .

JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (23) :9635-9645

[75]

Mcl-1 mediates tumor necrosis factor-related apoptosis-inducing ligand resistance in human cholangiocarcinoma cells [J].

Taniai, M ;

Grambihler, A ;

Higuchi, H ;

Werneburg, N ;

Bronk, SF ;

Farrugia, DJ ;

Kaufmann, SH ;

Gores, GJ .

CANCER RESEARCH, 2004, 64 (10) :3517-3524

[76]

Mcl-1 antisense therapy chemosensitizes human melanoma in a SCID mouse xenotransplantation model [J].

Thallinger, C ;

Wolschek, MF ;

Wacheck, V ;

Maierhofer, H ;

Günsberg, P ;

Polterauer, P ;

Pehamberger, H ;

Monia, BP ;

Selzer, E ;

Wolff, K ;

Jansen, B .

JOURNAL OF INVESTIGATIVE DERMATOLOGY, 2003, 120 (06) :1081-1086

[77]

Mcl-1; the molecular regulation of protein function [J].

Thomas, Luke W. ;

Lam, Connie ;

Edwards, Steven W. .

FEBS LETTERS, 2010, 584 (14) :2981-2989

[78]

ABT-263: A potent and orally bioavailable Bcl-2 family inhibitor [J].

Tse, Christin ;

Shoemaker, Alexander R. ;

Adickes, Jessica ;

Anderson, Mark G. ;

Chen, Jun ;

Jin, Sha ;

Johnson, Eric F. ;

Marsh, Kerman C. ;

Mitten, Michael J. ;

Nimmer, Paul ;

Roberts, Lisa ;

Tahir, Stephen K. ;

Mao, Yu ;

Yang, Xiufen ;

Zhang, Haichao ;

Fesik, Stephen ;

Rosenberg, Saul H. ;

Elmore, Steven W. .

CANCER RESEARCH, 2008, 68 (09) :3421-3428

[79]

The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized [J].

van Delft, Mark F. ;

Wei, Andrew H. ;

Mason, Kylie D. ;

Vandenberg, Cassandra J. ;

Chen, Lin ;

Czabotar, Peter E. ;

Willis, Simon N. ;

Scott, Clare L. ;

Day, Catherine L. ;

Cory, Suzanne ;

Adams, Jerry M. ;

Roberts, Andrew W. ;

Huang, David C. S. .

CANCER CELL, 2006, 10 (05) :389-399

[80]

How the Bcl-2 family of proteins interact to regulate apoptosis [J].

van Delft, MF ;

Huang, DC .

CELL RESEARCH, 2006, 16 (02) :203-213

← 1 2 3 4 5 6 7 8 9 10 →