B-cell lymphoma-2 (Bcl-2) family proteins, comprising proapoptotic proteins (Bax and Bak), antiapoptotic proteins (Bcl-2, Bcl-X_L, Bcl-w, Mcl-1, and A1) and BCL-2 homology domain 3 (BH3)-only proteins (Bid, Noxa, and Puma), have long been identified as pivotal apoptosis regulators. As an antiapoptotic member, myeloid cell leukemin-1 (Mcl-1) can bind with proapoptotic proteins and inhibit apoptosis. Mcl-1 is frequently overexpressed and closely associated with oncogenesis and poor prognosis in several cancers, posing a tremendous obstacle for cancer therapy. Recently, an increasing number of Mcl-1-selective small-molecule inhibitors have entered preclinical studies and advanced into clinical trials. In this review, we briefly introduce the role of Mcl-1 in apoptosis and highlight the recent development of Mcl-1 small-molecule inhibitors.

B 细胞淋巴瘤 2 (Bcl-2) 家族蛋白，包括促凋亡蛋白（Bax 和 Bak）、抗凋亡蛋白（Bcl-2、Bcl-X _L、Bcl-w、Mcl-1 和 A1) 和 BCL-2 同源结构域 3 (BH3)-only 蛋白（Bid、Noxa 和 Puma）长期以来被确定为关键的细胞凋亡调节因子。作为抗凋亡成员，骨髓细胞 leukemin-1 (Mcl-1) 可以与促凋亡蛋白结合并抑制凋亡。Mcl-1 在几种癌症中经常过表达并与肿瘤发生和预后不良密切相关，对癌症治疗构成了巨大障碍。最近，越来越多的 Mcl-1 选择性小分子抑制剂已进入临床前研究并进入临床试验。在这篇综述中，我们简要介绍了 Mcl-1 在细胞凋亡中的作用，并重点介绍了 Mcl-1 小分子抑制剂的最新进展。