Targeting cell apoptosis is currently the most promising therapy for cancer treatment. The BH3-only protein, which is a member of Bcl-2 family, can bind to the pro-survival members of the family and neutralize their functional activities to induce apoptosis (ie, to isolate pro-apoptotic members of the Bcl-2 family). BH3 mimetics, a kind of small molecule compounds, has the ability to mimic the BH3-only protein to induce apoptosis. The prototype of BH3 mimetics is ABT-737, who can selectively targets on BCL-XL, BCL-2 and BCL-W (but not MCL-1 and A1). ABT-263, a derivative of ABT-737, has a better performance of inducing apoptosis and inhibiting the growth of tumor in clinical trials. At this stage, some presumably BH3 mimetics has entered the clinical stage, while a large part of them is still being characterized and tested. Basing on the mechanism of BH3-only protein, this review summarize a variety of BH3 mimetics which have been widely recognized, and show the latest developments of newly diagnosed BH3 mimetics in the field.%靶向细胞凋亡是目前癌症治疗中最具发展前景的治疗方法之一。BCL-2家族的BH3-only蛋白（仅含BCL-2同源结构域BH3）可以通过与家族中促存活蛋白结合，使促存活蛋白失效，从而使促凋亡成员发挥作用，最终导致细胞发生程序性凋亡。BH3类似物即一类可以模仿BH3-only蛋白并诱发细胞凋亡的小分子化合物。BH3类似物的原型ABT-737可以选择性靶向BCL-XL、BCL-2和BCL-W 3个促存活蛋白（但不能作用于髓细胞白血病因子-1蛋白或A1蛋白），而它的衍生物ABT-263（navitoclax）在临床试验中有显著的促凋亡与抗肿瘤效应。现阶段，一些推测为BH3类似物的药物已经进入了临床阶段，但很大一部分仍在进行特征鉴定。本文在概述BH3-only蛋白作用机制的基础上，综述了多种已经广泛认可的BH3类似物及正在研究当中的最新BH3类似物。
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