Novel beta-Hairpin Antimicrobial Peptides Containing the beta-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance br | |
Li, Beibei1,2,3; Ouyang, Xu1,2,3; Ba, Zufang1,2; Yang, Yinyin1,2; Zhang, Jingying1,2,3; Liu, Hui1,2,3; Zhang, Tianyue1,2; Zhang, Fangyan1,2; Zhang, Yun1,2,3; Gou, Sanhu1,2,3; Ni, Jingman1,2,3 | |
2022-04-14 | |
Source Publication | JOURNAL OF MEDICINAL CHEMISTRY Impact Factor & Quartile |
ISSN | 0022-2623 |
EISSN | 1520-4804 |
Volume | 65Issue:7Pages:5625-5641 |
page numbers | 17 |
Abstract | The emergence of multidrug-resistant bacteria has dramatically increased the lethality, level of resistance, and difficulty of treatment. In this study, a series of new antimicrobialpeptides (AMPs) based on the beta-hairpin structure with thetemplate (XY)2RRRF(YX)2-NH2(X: hydrophobic amino acids; Y:cationic amino acids) were synthesized; surprisingly, almost all ofthe new peptides have strong antibacterial activity and negligiblehemolytic toxicity. Particularly, the therapeutic index (TI) values ofF(RI)2R and F(KW)2K reached up to 115.9 and 70.7, respectively.In addition, they did not show induced drug resistance andinhibited the development of antibiotic resistance when combinedand used with traditional antibiotics. In addition, their antibacterial mechanism was preliminarily studied. Moreover, the newpeptides F(RI)2R and F(KW)2K showed excellent performance in the pulmonary bacterial infection model and low toxicity in mice.In conclusion, F(RI)2R and F(KW)2K are considered new antimicrobial alternatives to address the antimicrobial-resistance crisis |
Publisher | AMER CHEMICAL SOC |
DOI | 10.1021/acs.jmedchem.1c02140 |
Indexed By | SCIE |
Language | 英语 |
WOS Research Area | Pharmacology & Pharmacy |
WOS Subject | Chemistry, Medicinal |
WOS ID | WOS:000792282200025 |
Original Document Type | Article |
PMID | 35311294 |
Citation statistics | |
Document Type | 期刊论文 |
Identifier | https://ir.lzu.edu.cn/handle/262010/479969 |
Collection | 兰州大学 |
Corresponding Author | Gou, Sanhu; Ni, Jingman |
Affiliation | 1.Lanzhou Univ, Chinese Acad Med Sci, Inst Pharmaceut, Sch Pharm, 2019RU066, Lanzhou 730000, Peoples R China; 2.Lanzhou Univ, Chinese Acad Med Sci, Res Unit Peptide Sci, 2019RU066, Lanzhou 730000, Peoples R China; 3.Lanzhou Univ, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, Lanzhou 730000, Peoples R China |
Recommended Citation GB/T 7714 | Li, Beibei,Ouyang, Xu,Ba, Zufang,et al. Novel beta-Hairpin Antimicrobial Peptides Containing the beta-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance br[J]. JOURNAL OF MEDICINAL CHEMISTRY,2022,65(7):5625-5641. |
APA | Li, Beibei.,Ouyang, Xu.,Ba, Zufang.,Yang, Yinyin.,Zhang, Jingying.,...&Ni, Jingman.(2022).Novel beta-Hairpin Antimicrobial Peptides Containing the beta-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance br.JOURNAL OF MEDICINAL CHEMISTRY,65(7),5625-5641. |
MLA | Li, Beibei,et al."Novel beta-Hairpin Antimicrobial Peptides Containing the beta-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance br".JOURNAL OF MEDICINAL CHEMISTRY 65.7(2022):5625-5641. |
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