Citation: Tian Kai, Deng Youchao, Li Yuling, Duan Yanwen, Huang Yong. Biosynthesis, Total Synthesis and Semisynthesis of Platensimycin, Platencin and their Analogues[J]. Chinese Journal of Organic Chemistry, ;2018, 38(9): 2348-2362. doi: 10.6023/cjoc201805062 shu

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

Tian Kai ^a ,
Deng Youchao ^a ,
Li Yuling ^a ,
Duan Yanwen ^a,b,c ,
Huang Yong ^a,c,,

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

Corresponding author: Huang Yong, jonghuang@csu.edu.cn
Received Date: 31 May 2018
Revised Date: 28 June 2018
Available Online: 16 September 2018
Fund Project: the Chinese Ministry of Education 111 Project B0803420the National Natural Science Foundation of China 81473123Project supported by the National Natural Science Foundation of China (No. 81473123) and the Chinese Ministry of Education 111 Project (No. B0803420)

Figures(11)

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.
- platensimycin,
- platencin,
- antibiotic,
- biosynthesis,
- total synthesis,
- semisynthesis
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沈阳化工大学材料科学与工程学院沈阳 110142