中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Deciphering the Regioselective Acylation Modification in Bipentaromycin

文献类型:期刊论文

作者Chen, Mengsong3,4; Shang, Guohui2,3; Chen, Xingyu1,3; Xie, Yunchang1; Li, Chunhuan4; Huang, Chunshuai2,3
刊名CHINESE JOURNAL OF CHEMISTRY
出版日期2025-05-27
页码6
关键词Direct cloning REGAIN Bipentaromycin Biosynthesis Acyltransferase Computational modeling Inactivation Active sites
ISSN号1001-604X
DOI10.1002/cjoc.70086
通讯作者Li, Chunhuan(chunhuanli@nwsuaf.edu.cn) ; Huang, Chunshuai(huangchunshuai@simm.ac.cn)
英文摘要Aromatic polyketides (APKs) are renowned for their structural diversity and potent biological activities, making them valuable resources for drug discovery in antibiotics, anticancer agents, and antiparasitic therapies. Bipentaromycins, a unique class of dimeric APKs with a cyclic head-to-tail linkage, exhibit broad-spectrum antibacterial activities. Acylation modifications in bipentaromycins C-F enhance their pharmacological properties, yet the responsible acyltransferase remains enigmatic. Herein, we present REGAIN, an innovative strategy combining restriction enzyme digestion, Gibson assembly, and in vivo Cre-lox recombinatio n, enabling rapid and efficient cloning of biosynthetic gene clusters (BGCs). Using REGAIN, we successfully cloned a 40 kb bipentaromycin BGC (bpm). By integrating genetic experiments and computational modeling, we speculated BpmP as the acyltransferase responsible for regioselective acylation. This study establishes a robust platform for exploring novel bioactive molecules and advances the understanding of bipentaromycin biosynthesis.
WOS关键词GCN5-RELATED N-ACETYLTRANSFERASES ; BIOSYNTHETIC GENE-CLUSTER ; CRYSTAL-STRUCTURE ; DIRECT CLONING
资助项目Key R&D Program of Shandong Province, China[2024CXPT029] ; National Natural Science Foundation of China[22407132] ; The 100 Talents Program of the Chinese Academy of Sciences ; Shanghai Pujiang Program[23PJ1415100] ; Shandong Provincial Excellent Youth Science Fund Project (Overseas)[2025HWYQ-069] ; TaiShan Scholars Program[tsqn202408316] ; Shandong Provincial Natural Science Foundation[ZR2024QC204]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:001495473300001
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/317989]  
专题中国科学院上海药物研究所
通讯作者Li, Chunhuan; Huang, Chunshuai
作者单位1.Jiangxi Normal Univ, Coll Life Sci, Nanchang 330022, Jiangxi, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
3.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China
4.Northwest A&F Univ, Coll Chem & Pharm, Shaanxi Key Lab Nat Prod & Chem Biol, Yangling 712100, Shaanxi, Peoples R China
推荐引用方式
GB/T 7714
Chen, Mengsong,Shang, Guohui,Chen, Xingyu,et al. Deciphering the Regioselective Acylation Modification in Bipentaromycin[J]. CHINESE JOURNAL OF CHEMISTRY,2025:6.
APA Chen, Mengsong,Shang, Guohui,Chen, Xingyu,Xie, Yunchang,Li, Chunhuan,&Huang, Chunshuai.(2025).Deciphering the Regioselective Acylation Modification in Bipentaromycin.CHINESE JOURNAL OF CHEMISTRY,6.
MLA Chen, Mengsong,et al."Deciphering the Regioselective Acylation Modification in Bipentaromycin".CHINESE JOURNAL OF CHEMISTRY (2025):6.

入库方式: OAI收割

来源:上海药物研究所

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