| Mcl-1小分子抑制剂研究进展 |
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| 引用本文： | 吴贯召,何雄,董雪洋,于日磊,江涛.Mcl-1小分子抑制剂研究进展[J].中国海洋药物,2018,37(4):80-86. |
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| 作者姓名： | 吴贯召 何雄 董雪洋 于日磊 江涛 |
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| 作者单位： | 中国海洋大学 海洋药物教育部重点实验室,中国海洋大学 海洋药物教育部重点实验室,中国海洋大学医药学院,中国海洋大学 海洋药物教育部重点实验室,中国海洋大学 海洋药物教育部重点实验室 |
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| 基金项目： | 国家自然科学基金-山东省联合基金 (U1706213, U1406403) ,山东省泰山学者专项资助 |
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| 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。
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| 关 键 词： | Bcl-2 Mcl-1 凋亡 小分子抑制剂 |
| 收稿时间： | 2018/3/2 0:00:00 |
| 修稿时间： | 2018/3/21 0:00:00 |
Research progress of small-molecule Mcl-1 inhibitors |
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| Institution: | Key Laboratory of Marine Drugs,Ministry of Education of China,School of Pharmacy,Ocean University of China,Key Laboratory of Marine Drugs,Ministry of Education of China,School of Pharmacy,Ocean University of China,Key Laboratory of Marine Drugs,Ministry of Education of China,School of Pharmacy,Ocean University of China and Key Laboratory of Marine Drugs,Ministry of Education of China,School of Pharmacy,Ocean University of China |
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| Abstract: | 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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| Keywords: | Bcl-2 Mcl-1 Apoptosis Inhibitors |
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