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Journal of Chinese Pharmaceutical Sciences ›› 2017, Vol. 26 ›› Issue (7): 467-478.DOI: 10.5246/jcps.2017.07.052

• Reviews •     Next Articles

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).

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

CLC Number: 

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