Mcl-1小分子抑制剂在肿瘤治疗中的应用进展

Research progress of small-molecule Mcl-1 inhibitors on cancer therapy

目的阐述近年来Mcl-1小分子抑制剂的结构及在肿瘤治疗中的应用。方法归纳国内外的最新研究进展报道,按照分子结构类型,对主要的、具有发展潜力的重要分子抑制剂进行综述。结果采用计算机分子模拟、对接、活性预测,进一步通过毒性和活性测定,各种分子具有大小不等的抑制活性,并在肿瘤治疗中取得了较好的效果。结论 Mcl-1有望作为一种开发前景广阔的肿瘤治疗靶点。

Objective Mcl-1is a promising cancer target.This review highlights the current research progress on the inhibition of this target.Method Base on the inhibitors′structure,this review focuses on the current state of Mcl-1inhibitors,especially some important members.Result Aided by docking models and high-throughput screen,some inhibitors showed rather high bioactivity and low toxicity,further induced Bcl-2dependent apoptosis in some tumor cells.Conclusion The recent efforts will lead to discovery novel Mcl-1inhibitors for the treatment of cancer.