Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (9): 2348-2362.DOI: 10.6023/cjoc201805062 Previous Articles     Next Articles

Special Issue: 合成科学



田凯a, 邓友超a, 李玉玲a, 段燕文a,b,c, 黄勇a,c   

  1. a 中南大学湘雅国际转化医学联合研究院 长沙 410013;
    b 组合生物合成与天然产物药物湖南省工程研究中心 长沙 410205;
    c 新药组合生物合成国家地方联合工程研究中心 长沙 410205
  • 收稿日期:2018-05-31 修回日期:2018-06-28 发布日期:2018-07-16
  • 通讯作者: 黄勇
  • 基金资助:


Biosynthesis, Total Synthesis and Semisynthesis of Platensimycin, Platencin and their Analogues

Tian Kaia, Deng Youchaoa, Li Yulinga, Duan Yanwena,b,c, Huang Yonga,c   

  1. a Xiangya International Academy of Translational Medicine, Central South University, Changsha 410013;
    b Hunan Engineering Research Center of Combinatorial Biosynthesis and Natural Product Drug Discovery, Changsha 410205;
    c National Engineering Research Center of Combinatorial Biosynthesis for Drug Discovery, Changsha 410205
  • Received:2018-05-31 Revised:2018-06-28 Published:2018-07-16
  • Contact: 10.6023/cjoc201805062
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81473123) and the Chinese Ministry of Education 111 Project (No. B0803420).

The emergence of multi-drug resistant bacteria is one of the major public heath crises. Platensimycin (PTM) and platencin (PTN) are potent antibacterial drug leads against many gram-postive pathogens, such as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus. The past decade has witnessed the systematic study of biosynthesis, total synthesis and semisynthesis of these facinating molecules, due to their novel structures and excellent biological activities in vitro and in vivo. These studies have shed new lights on the disovery of microbial drug leads through novel high throughput strategies. Dedicated enzymes for the formation of PTM and PTN and other metabolites in their biosynthetic pathways, including new-characterized bacterial diterpenoid synthases and thiocarboxylate biosynthetic enzymes, have been revealed. The generation of many analogues of PTM and PTN though organic synthesis and precursor-directed biosynthesis has helped to establish the structure-activity relationships of PTM, PTN and their analgues. This review summarizes the progress in the disovery and development of these outstanding natural product drug leads, which supports the notion to integrate biosynthesis and organic synthesis for rapid microbial drug discovery and development.

Key words: platensimycin, platencin, antibiotic, biosynthesis, total synthesis, semisynthesis