兰州大学机构库
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies
Ouyang, Xu1,2; Li, Beibei1,2; Yang, Yinyin1,2; Ba, Zufang1,2; Zhang, Jingying1,2; Zhang, Tianyue1,2; Chang, Linlin1,2; Zhang, Fangyan1,2; Zhang, Yun1,2; Liu, Hui1,2; Gou, Sanhu1,2; Ni, Jingman1,2
2022-09-01
Online publication date2022-09
Source PublicationJOURNAL OF MEDICINAL CHEMISTRY   Impact Factor & Quartile
ISSN0022-2623
EISSN1520-4804
Volume65Issue:20Pages:13833-13851
page numbers19
AbstractNonselective toxicity of antimicrobial peptides (AMPs) needs to be solved urgently for their application. Temporin-PE (T-PE, FLPIVAKLLSGLL-NH2), an AMP extracted from skin secretions of frogs, has high toxicity and specific antimicrobial activity against Gram-positive bacteria. To improve the antimicrobial performance of T-PE, a series of T-PE analogues were designed and synthesized by glutamic acid full-scan, and then their key positions were replaced with lysine. Finally, E11K4K10, the highest therapeutic indicial AMP, was screened out. E11K4K10 was not easy to induce and produce drug-resistant bacteria when used alone, as well as it could also inhibit the development of the drug resistance of traditional antibiotics when it was used in combination with the traditional antibiotics. In addition, E11K4K10 had an excellent therapeutic effect on a mouse model of pulmonary bacterial infection. Taken together, this study provides a new approach for the further improvement of new antimicrobial peptides against the antimicrobial-resistance crisis.
PublisherAMER CHEMICAL SOC
DOI10.1021/acs.jmedchem.2c01076
Indexed BySCIE ; IC
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000861195300001
Original Document TypeArticle ; Early Access
PMID 3614851
Citation statistics
Cited Times:8[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttps://ir.lzu.edu.cn/handle/262010/488465
Collection兰州大学
Corresponding AuthorGou, Sanhu; Ni, Jingman
Affiliation
1.Lanzhou Univ, Inst Pharmaceut, Chinese Acad Med Sci, Sch Basic Med Sci, 2019RU066, Lanzhou 730000, Peoples R China;
2.Chinese Acad Med Sci, Peking Union Med Coll, Inst Mat Med, Beijing 100050, Peoples R China
Recommended Citation
GB/T 7714
Ouyang, Xu,Li, Beibei,Yang, Yinyin,et al. Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies[J]. JOURNAL OF MEDICINAL CHEMISTRY,2022,65(20):13833-13851.
APA Ouyang, Xu.,Li, Beibei.,Yang, Yinyin.,Ba, Zufang.,Zhang, Jingying.,...&Ni, Jingman.(2022).Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.JOURNAL OF MEDICINAL CHEMISTRY,65(20),13833-13851.
MLA Ouyang, Xu,et al."Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies".JOURNAL OF MEDICINAL CHEMISTRY 65.20(2022):13833-13851.
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