Recent advances in the development of Mcl-1 inhibitors for cancer therapy

被引：102

作者：

Hird, Alexander W. ^{[1
]}

Tron, Adriana E. ^{[1
]}

机构：

[1] AstraZeneca Boston, IMED Biotech Unit, Oncol, 35 Gatehouse Dr, Waltham, MA 02451 USA

来源：

PHARMACOLOGY & THERAPEUTICS | 2019年 / 198卷

关键词：

Apoptosis; Protein-protein interactions; Mcl-1; BH-3 mimetic drugs; Drug development; Cancer; DEPENDENT KINASE INHIBITOR; ANTI-APOPTOTIC MCL-1; MULTIPLE-MYELOMA CELLS; DOWN-REGULATION; ACQUIRED-RESISTANCE; SIGNALING PATHWAY; FAMILY PROTEINS; HIGH-AFFINITY; BCL-2; SURVIVAL;

D O I：

10.1016/j.pharmthera.2019.02.007

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Dysregulation of the mitochondrial apoptotic pathway controlled by members of the Bcl-2 protein family plays a central role in cancer development and resistance to conventional cytotoxic as well as targeted therapies. Hence, selective inhibition of pro-survival Bcl-2 family of proteins to activate apoptosis in malignant cells represents an exciting anti-cancer strategy. The remarkable clinical performance of the selective Bcl-2 antagonist venetoclax has highlighted the potential for selective inhibitors of the other pro-survival members of the Bcl-2 family, particularly Mc1-1. Here we review the latest progress on the discovery and development of selective inhibitors of Mc1-1 that are undergoing clinical evaluation for cancer therapy. (C) 2019 The Author(s). Published by Elsevier Inc. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

引用

页码：59 / 67

页数：9

共 94 条

[1] Suppression of myeloid cell leukemia-1 (Mcl-1) enhances chemotherapy-associated apoptosis in gastric cancer cells [J].

Akagi, Hideko ;

Higuchi, Hajime ;

Sumimoto, Hidetoshi ;

Igarashi, Toru ;

Kabashima, Ayano ;

Mizuguchi, Hiroyuki ;

Izumiya, Motoko ;

Sakai, Gen ;

Adachi, Masayuki ;

Funakoshi, Shinsuke ;

Nakamura, Shoko ;

Hamamoto, Yasuo ;

Kanai, Takanori ;

Takaishi, Hiromasa ;

Kawakami, Yutaka ;

Hibi, Toshifumi .

GASTRIC CANCER, 2013, 16 (01) :100-110

[2]

Akçay G, 2016, NAT CHEM BIOL, V12, P931, DOI [10.1038/NCHEMBIO.2174, 10.1038/nchembio.2174]

[3] Mcl-1 is a potential therapeutic target in multiple types of cancer [J].

Akgul, C. .

CELLULAR AND MOLECULAR LIFE SCIENCES, 2009, 66 (08) :1326-1336

[4] Mutant B-RAF-Mcl-1 survival signaling depends on the STAT3 transcription factor [J].

Becker, T. M. ;

Boyd, S. C. ;

Mijatov, B. ;

Gowrishankar, K. ;

Snoyman, S. ;

Pupo, G. M. ;

Scolyer, R. A. ;

Mann, G. J. ;

Kefford, R. F. ;

Zhang, X. D. ;

Rizos, H. .

ONCOGENE, 2014, 33 (09) :1158-1166

[5] Pathways and mechanisms of venetoclax resistance [J].

Bose, Prithviraj ;

Gandhi, Varsha ;

Konopleva, Marina .

LEUKEMIA & LYMPHOMA, 2017, 58 (09) :2026-2039

[6] Humanized Mcl-1 mice enable accurate preclinical evaluation of MCL-1 inhibitors destined for clinical use [J].

Brennan, Margs S. ;

Chang, Catherine ;

Tai, Lin ;

Lessene, Guillaume ;

Strasser, Andreas ;

Dewson, Grant ;

Kelly, Gemma L. ;

Herold, Marco J. .

BLOOD, 2018, 132 (15) :1573-1583

[7]

Bruncko M, 2008, 7 NONSUBSTITUTED IND

[8] Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity [J].

Bruncko, Milan ;

Wang, Le ;

Sheppard, George S. ;

Phillips, Darren C. ;

Tahir, Stephen K. ;

Xue, John ;

Erickson, Scott ;

Fidanze, Steve ;

Fry, Elizabeth ;

Hasvold, Lisa ;

Jenkins, Gary J. ;

Jin, Sha ;

Judge, Russell A. ;

Kovar, Peter J. ;

Madar, David ;

Nimmer, Paul ;

Park, Chang ;

Petros, Andrew M. ;

Rosenberg, Saul H. ;

Smith, Morey L. ;

Song, Xiaohong ;

Sun, Chaohong ;

Tao, Zhi-Fu ;

Wang, Xilu ;

Xiao, Yu ;

Zhang, Haichao ;

Tse, Chris ;

Leverson, Joel D. ;

Elmore, Steven W. ;

Souers, Andrew J. .

JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (05) :2180-2194

[9] AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies [J].

Caenepeel, Sean ;

Brown, Sean P. ;

Belmontes, Brian ;

Moody, Gordon ;

Keegan, Kathleen S. ;

Chui, Danny ;

Whittington, Douglas A. ;

Huang, Xin ;

Poppe, Leszek ;

Cheng, Alan C. ;

Cardozom, Mario ;

Houze, Jonathan ;

Li, Yunxiao ;

Lucas, Brian ;

Paras, Nick A. ;

Wang, Xianghong ;

Taygerly, Joshua P. ;

Vimolratana, Marc ;

Zancanella, Manuel ;

Zhu, Liusheng ;

Cajulis, Elaina ;

Osgood, Tao ;

Sun, Jan ;

Damon, Leah ;

Egan, Regina K. ;

Greninger, Patricia ;

McClanaghan, Joseph D. ;

Gong, Jianan ;

Moujalled, Donia ;

Pomilio, Giovanna ;

Beltran, Pedro ;

Benes, Cyril H. ;

Roberts, Andrew W. ;

Huang, David C. ;

Wei, Andrew ;

Canon, Jude ;

Coxon, Angela ;

Hughes, Paul E. .

CANCER DISCOVERY, 2018, 8 (12) :1582-1597

[10] mcl-1 is an immediate-early gene activated by the granulocyte-macrophage colony-stimulating factor (GM-CSF) signaling pathway and is one component of the GM-CSF viability response [J].

Chao, JR ;

Wang, JM ;

Lee, SF ;

Peng, HW ;

Lin, YH ;

Chou, CH ;

Li, JC ;

Huang, HM ;

Chou, CK ;

Kuo, ML ;

Yen, JJY ;

Yang-Yen, HF .

MOLECULAR AND CELLULAR BIOLOGY, 1998, 18 (08) :4883-4898

← 1 2 3 4 5 6 7 8 9 10 →