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MCL-1 inhibition in cancer treatment

Authors Xiang W, Yang CY, Bai L

Received 8 July 2018

Accepted for publication 10 September 2018

Published 23 October 2018 Volume 2018:11 Pages 7301—7314

DOI https://doi.org/10.2147/OTT.S146228

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Amy Norman

Peer reviewer comments 2

Editor who approved publication: Dr Federico Perche


Weiguo Xiang,1 Chao-Yie Yang,1,2 Longchuan Bai1,2

1Department of Internal Medicine, University of Michigan Medical School, 2Rogel Cancer Center, University of Michigan, Ann Arbor, MI, USA

Abstract: Myeloid cell leukemia-1 (MCL-1), a member of antiapoptotic BCL-2 family proteins, is a key regulator of mitochondrial homeostasis. Frequent overexpression of MCL-1 in human primary and drug-resistant cancer cells makes it an attractive cancer therapeutic target. Significant progress has been made in the development of small-molecule MCL-1 inhibitors in recent years, and three MCL-1 selective inhibitors have advanced to clinical trials. This review briefly discusses recent advances in the development of small molecules targeting MCL-1 for cancer therapy.

Keywords: BCL-2, BAX, BAK, apoptosis, BH3 mimetics

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