Design, synthesis, and antibacterial evaluation of vancomycin-LPS binding peptide conjugates

doi:10.1016/j.bmcl.2021.128122

	Design, synthesis, and antibacterial evaluation of vancomycin-LPS binding peptide conjugates
	Shi, Weiwei 1,2; Chen, Feifei 1,2; Zou, Xiangman 1,3; Jiao, Shang 1,2; Wang, Siqi 1,2; Hu, Yu 1,4; Lan, Lefu 1,2; Tang, Feng 1,2; Huang, Wei 1,2,5
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2021-08-01
卷号	45 页码:8
关键词	Vancomycin analogues LPS binding peptides Vancomycin-Peptide Conjugates Antibacterial activity
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2021.128122
通讯作者	Lan, Lefu(llan@simm.ac.cn) ; Tang, Feng(tangfeng2013@simm.ac.cn) ; Huang, Wei(haungwei@simm.ac.cn)
英文摘要	Developing novel antibiotics is urgently needed with emergency of drug resistance. Vancomycin, the last resort for intractable Gram-positive bacterial infections, is ineffective against Gram-negative bacteria and vancomycin resistant bacteria. Herein, we report a series of novel vancomycin derivatives carrying LPS binding peptides, vancomycin-LPS binding peptide conjugates (VPCs). The LPS binding peptides were conjugated onto 4 sites of vancomycin via CuAAC or maleimide- sulfydryl addition, and the formed VPCs were screened against VISA/VRE and Gram-negative strains. VPCs exhibited enhanced activity against vancomycin resistant bacteria and obtained the activity against Gram-negative bacteria in vitro, providing a novel strategy for vancomycin modification and glycopeptide antibiotics synthesis.
资助项目	National Natural Science Foundation of China (NNSFC)[21877116] ; SIMM institute fund[CASIMM0120202009] ; Shanghai Action Plan of Technological Innovation[18431900700] ; National Megaproject for Innovative Drugs[2019ZX09721001004009]
WOS关键词	ANTIBIOTICS ; DETOXIFICATION ; MECHANISMS ; ANALOGS ; SITE
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000661400500013
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297178]
专题	中国科学院上海药物研究所
通讯作者	Lan, Lefu; Tang, Feng; Huang, Wei
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Biotherapeut Discovery Res, CAS Ctr Excellence Mol Cell Sci,CAS key Lab Recep, 555 Zuchongzhi Rd,Pudong, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Univ South China, Hunan Prov Key Lab Tumor Microenvironm Response, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China 4.Jinzhou Med Univ, Sch Pharm, Jinzhou 121001, Peoples R China 5.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
推荐引用方式 GB/T 7714	Shi, Weiwei,Chen, Feifei,Zou, Xiangman,et al. Design, synthesis, and antibacterial evaluation of vancomycin-LPS binding peptide conjugates[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2021,45:8.
APA	Shi, Weiwei.,Chen, Feifei.,Zou, Xiangman.,Jiao, Shang.,Wang, Siqi.,...&Huang, Wei.(2021).Design, synthesis, and antibacterial evaluation of vancomycin-LPS binding peptide conjugates.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,45,8.
MLA	Shi, Weiwei,et al."Design, synthesis, and antibacterial evaluation of vancomycin-LPS binding peptide conjugates".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 45(2021):8.