期刊
CURRENT MOLECULAR MEDICINE
卷 21, 期 5, 页码 426-439出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1566524020666200929121016
关键词
Apoptosis; Antitumor agents; Anti-apoptotic proteins; Bcl-2 family proteins; Myeloid cell leukemia 1 inhibitor
资金
- National Natural Science Foundation of China [22077022, 21431001]
- Natural Science Foundation of Guangxi Province [IRT_16R15, 2016GXNSFGA380005, AD17129007]
- Innovation Project of Guangxi Graduate Education [YCBZ2017029]
- BAGUI Scholar program of Guangxi Province of China
Mcl-1, a member of the Bcl-2 family of proteins, plays a key role in regulating the intrinsic pathway of apoptosis and is correlated with cancer progression and drug resistance. Developing inhibitors of Mcl-1 is essential for effective cancer therapy.
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.
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