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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*   Pages 1 - 14 ( 14 )

Abstract:


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. Whilst 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

Affiliation:

State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, 15 Yu Cai Road, Guilin 541004, State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, 15 Yu Cai Road, Guilin 541004, Department of Chemistry, Faculty of Science, The University of British Columbia, 2036 Main Mall Vancouver, BC, State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, 15 Yu Cai Road, Guilin 541004



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