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Current Molecular Medicine


ISSN (Print): 1566-5240
ISSN (Online): 1875-5666

Mini-Review Article

Peptide and Small Molecule Inhibitors Targeting Myeloid Cell Leukemia 1 (Mcl-1) as Novel Antitumor Agents

Author(s): Xing Lu, Hong Liang*, Chris Orvig and Zhen-Feng Chen*

Volume 21, Issue 5, 2021

Published on: 29 September, 2020

Page: [426 - 439] Pages: 14

DOI: 10.2174/1566524020666200929121016

Price: $65


Myeloid cell leukemia 1 (Mcl-1) is a member of the Bcl-2 family of proteins with anti-apoptotic activity. It plays a key role in the regulation of the intrinsic pathway of apoptosis. Moreover, Mcl-1 is correlated with the progression and drug-resistance of various cancers. The development of inhibitors of Mcl-1 may provide effective cancer therapies. While the inhibitors of other Bcl-2 anti-apoptotic proteins have been well explored, the discovery of Mcl-1inhibitors with high selectivity has been challenging. In this review, we summarize the recent literature on small molecule and peptide inhibitors of Mcl-1, which are divided into different types including peptide inhibitors, gossypol derivatives, marinopyrrole derivatives, S1 derivatives, indole derivatives, quinoline derivatives, S63845, AZD5991, AMG176, etc. Their biological activities are also summarized. Mcl-1 is a valid drug target and inhibition of Mcl-1 with a small molecule inhibitor is a promising strategy for cancer therapy.

Keywords: Apoptosis, Antitumor agents, Anti-apoptotic proteins, Bcl-2 family proteins, Myeloid cell leukemia 1 inhibitor.

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