| 吴贯召,何雄,董雪洋,等.Mcl-1小分子抑制剂研究进展[J].中国海洋药物,2018,37(4):80-86. |
| Mcl-1小分子抑制剂研究进展 |
| Research progress of small-molecule Mcl-1 inhibitors |
| 投稿时间：2018-03-02 修订日期：2018-03-21 |
| DOI： |
| 中文关键词: Bcl-2 Mcl-1 凋亡 小分子抑制剂 |
| English Keywords:Bcl-2 Mcl-1 Apoptosis Inhibitors |
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| 中文摘要: |
| MCL-1(myeloid cell leukemia-1)蛋白是BCL-2(B-cell lymphoma-2)蛋白家族中重要的抗凋亡蛋白成员之一,在多种肿瘤细胞中过表达。Mcl-1蛋白的过表达不仅与肿瘤的发生发展密切相关,还会导致肿瘤细胞对化疗药物产生耐药性,因此以Mcl-1为靶点的小分子抑制剂是未来抗肿瘤药物研发的重点。本文对2012-2017年间发表的Mcl-1小分子抑制剂进行了综述,主要介绍小分子抑制剂的化学结构和生物活性,旨在为Mcl-1小分子抑制剂的深入研究以及更多海洋来源的新型Mcl-1小分子抑制剂的开发提供参考。 |
| English Summary: |
| Myeloid cell leukemia-1 (MCL-1) protein is one of the key anti-apoptotic protein members of the B-cell lymphoma-2 protein family. Overexpression of Mcl-1 is not only closely related to the tumor survival, but also leads to the resistance to chemotherapeutic drug. Therefore, developing small-molecule inhibitors targeting Mcl-1 is promising for cancer therapy. This review summarized the Mcl-1 small molecule inhibitors published from 2012 to 2017, including their chemical structures and biological activities, and thus attracted the interest of chemists and biologists. |
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