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
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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 |
DOI | 10.1002/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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