Title:Peptide and Small Molecule Inhibitors Targeting Myeloid Cell Leukemia 1 (Mcl-1) as Novel Antitumor Agents
Volume: 21
Issue: 5
关键词:
细胞凋亡、抗肿瘤药物、抗凋亡蛋白、Bcl-2家族蛋白、髓系细胞白血病1抑制剂。
摘要: 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.
