http://jcps.bjmu.edu.cn

中国药学(英文版) ›› 2017, Vol. 26 ›› Issue (7): 467-478.DOI: 10.5246/jcps.2017.07.052

• 【综述】 •    下一篇

β-内酯类蛋白酶体抑制剂乳胞素及其衍生物的合成研究进展

王玉平, 朱晓伟, 辛健, 郭妍妍, 徐向楠, 马宇衡*   

  1. 内蒙古医科大学 药学院 药物化学教研室, 内蒙古 呼和浩特 010110
  • 收稿日期:2017-03-27 修回日期:2017-03-29 出版日期:2017-07-28 发布日期:2017-05-29
  • 通讯作者: Tel.: +86-471-6653149, E-mail: myhstar@126.com
  • 作者简介:马宇衡博士, 2009年毕业于北京大学药学院, 获药物化学专业博士学位; 2009–2012年在于北京大学工学院、化学院从事博士后研究; 2012年10月任内蒙古医科大学药学院药物化学专业副教授。研究方向: 抗肿瘤药物的研究与开发。
  • 基金资助:

    National Natural Science Foundation of China (Grant No. 21362021). Inner Mongolia Natural Science Foundation (Grant No. 2015MS0206).

Research progress of synthetic lactacystin and its analogs as β-lactone proteasome inhibitors

Yuping Wang, Xiaowei Zhu, Jian Xin, Yanyan Guo, Xiangnan Xu, Yuheng Ma*   

  1. School of Pharmacy, Inner Mongolia Medical University, Hohhot 010110, China
  • Received:2017-03-27 Revised:2017-03-29 Online:2017-07-28 Published:2017-05-29
  • Contact: Tel.: +86-471-6653149, E-mail: myhstar@126.com
  • About author:In 2009, Dr. Ma obtained his Ph.D. degree in medicinal chemistry from School of Pharmaceutical Sciences, Peking University. During 2009–2012, he did postdoctoral research at college of engineering and college of chemistry and molecular engineering, Peking University. In October 2012, he joined the School of Pharmacy at Inner Mongolia Medicinal University as an Associate Professor. His research interest is discovery de novo antitumor drug.
  • Supported by:

    National Natural Science Foundation of China (Grant No. 21362021). Inner Mongolia Natural Science Foundation (Grant No. 2015MS0206).

摘要:

硼替佐米和卡非佐米被FDA批准用于治疗多发性骨髓瘤后, 20S蛋白酶体已经作为靶点引起了关注, 但这两种药物存在耐药性作为第二代候选药物, 从天然产物中提取得到的β-内酯类蛋白酶抑制剂被用于癌症关节炎哮喘阿尔茨海默病治疗, 代表药物为Salinosporamide A (1)。本文综述了具有β-内酯结构的乳胞素及其衍生物的合成方法

关键词: 乳胞素, β-内酯, 蛋白酶体, 抑制剂

Abstract:

As Bortezomib and Carfilzomib are approved to treat refractory multiple myeloma, 20S proteasome has become a highly interested tumor therapeutic target. Because of drug resistance of Bortezomib and Carfilzomib, β-lactone natural products are used to treat cancer, arthritis, asthma, and Alzheimer’s diseases. Now the second generation drug candidates are developed, eg. Salinosporamide A (1). This review is aiming to encapsulate the synthetic methods of β-lactone proteasome inhibitors, lactacystin (3) and its analogs.

Key words: Lactacystin, β-Lactone, Proteasome, Inhibitors

中图分类号: 

Supporting: