Acta Chimica Sinica ›› 2020, Vol. 78 ›› Issue (12): 1383-1398.DOI: 10.6023/A20070299 Previous Articles     Next Articles



周甲申, 张琳, 张良   

  1. 上海交通大学医学院 药理与化学生物学系 上海 200025
  • 投稿日期:2020-07-08 发布日期:2020-09-22
  • 通讯作者: 张良
  • 作者简介:周甲申,男,上海交通大学基础医学院药理与化学生物学系2018级硕博连读生,主要研究方向为幽门螺旋杆菌脂肪酸合成途径关键酶的动态调控分子机制研究和药物发现.
    张良,男,1980年11月出生,2008年博士毕业于中国科学院上海药物研究所,随后在美国芝加哥大学化学系从事博士后研究,2014年10月至今在上海交通大学基础医学院药理与化学生物学系担任课题组长和博士生导师,国家自然科学基金委优秀青年基金获得者,上海市东方学者特聘教授.研究方向:以化学生物学、结构生物学和细胞生物学交叉技术手段,阐明核酸和脂肪酸合成与动态修饰在肿瘤和病原菌中的独特调控机制,发现新的抗肿瘤/病原菌药物靶标,并通过建立全新的化学生物学技术筛选新的特异性先导药物.研究内容包括:(1) DNA/RNA去甲基化表观修饰在肿瘤中的动态分子调控机制研究和药物发现;(2)核苷酸合成途径在肿瘤中的动态分子调控机制研究和药物发现;(3)脂肪酸合成途径在病原菌中的分子调控机制研究和药物发现.
  • 基金资助:

Advances on Mechanism and Drug Discovery of Type-II Fatty Acid Biosynthesis Pathway

Zhou Jiashen, Zhang Lin, Zhang Liang   

  1. Department of Pharmacology and Chemical Biology, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China
  • Received:2020-07-08 Published:2020-09-22
  • Supported by:
    Project supported by the Major Research Plan of the National Natural Science Foundation of China (Training Program) (No. 91853118) and Youth Program of National Natural Science Foundation of China (No. 21722802).

Type-Ⅱ fatty acid biosynthesis pathway (FAS-Ⅱ) is the only essential biosynthesis pathway that producing saturated and unsaturated fatty acids for bacteria and plant cell assembly and cellular metabolism. It utilizes a series of individual enzymes encoded by discrete genes to stepwisely catalyze lipid chain growing carried by the substrate carrier protein-acyl carrier protein (ACP). Due to its indispensable biological role in bacteria growth, as well as the distinct biological regulation mechanisms from mammalian fatty acid biosynthesis (FAS-I), the enzymes involved in FAS-Ⅱ have been considered as important anti-pathogenic drug targets for a long time. Hence, investigating the catalysis and dynamic regulation mechanisms of FAS-Ⅱ, developing novel anti-pathogenic drugs against the enzymes involved in FAS-Ⅱ is critical to the field. We here summarize the catalytic mechanism studies and inhibitor discovery work involved in FAS-Ⅱ so far, which may potentially facilitate further understanding of FAS-Ⅱ biological functions as well as antibacterial drug discovery for infectious diseases.

Key words: type-II fatty acid biosynthesis pathway (FAS-II), acyl carrier protein (ACP), substrate recognition, catalysis regulation, inhibitor discovery