文献类型：期刊文献

英文题名：Short Guanidinium-Functionalized Poly(2-oxazoline)s Displaying Potent Therapeutic Efficacy on Drug-Resistant Fungal Infections

作者：Jiang, Weinan[1];Zhou, Min[1];Cong, Zihao[2,3];Xie, Jiayang[2,3];Zhang, Wenjing[2,3];Chen, Sheng[2,3];Zou, Jingcheng[2,3];Ji, Zhemin[2,3];Shao, Ning[2,3];Chen, Xin[3];Li, Maoquan[4];Liu, Runhui[1,2,3]

机构：[1]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Minist Educ, Res Ctr Biomed Mat,Frontiers Sci Ctr Materiobiol, Shanghai Frontier Sci Res Base Optogenet Tech Cel, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, Sch Mat Sci & Engn, Minist Educ, Key Lab Ultrafine Mat, Shanghai 200237, Peoples R China;[4]Tongji Univ, Sch Med, Shanghai Peoples Hosp 10, Dept Intervent & Vasc Surg, Shanghai 200072, Peoples R China

年份：2022

卷号：61

期号：17

外文期刊名：ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

收录：;EI(收录号：20220911732496);WOS:【SCI-EXPANDED(收录号:WOS:000762127600001)】；

基金：This research was supported by the National Natural Science Foundation of China for Innovative Research Groups (No. 51621002), the National Natural Science Foundation of China (No. 22075078, 21861162010), Program of Shanghai Academic/Technology Research Leader (20XD1421400), Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism (Shanghai Municipal Education Commission, grant 2021 Sci & Tech 03-28), Research program of State Key Laboratory of Bioreactor Engineering, the Fundamental Research Funds for the Central Universities (JKD01211520). The authors also thank Research Center of Analysis and Test of East China University of Science and Technology for the help on the characterization. We also thank the staff members of the Mass Spectrometry System at the National Facility for Protein Science in Shanghai (NFPS), Zhangjiang Lab, China for providing technical support and assistance in data collection and analysis.

语种：英文

外文关键词：Antifungal Polymers; Drug-Resistant Fungi; Guanidinium-Pendent; Peptidomimetics; Poly(2-oxazoline)s

摘要：New antifungals are urgently needed to combat invasive fungal infections, due to limited types of available antifungal drugs and frequently encountered side effects, as well as the quick emergence of drug-resistance. We previously developed amine-pendent poly(2-oxazoline)s (POXs) as synthetic mimics of host defense peptides (HDPs) to have antibacterial properties, but with poor antifungal activity. Hereby, we report the finding of short guanidinium-pendent POXs, inspired by cell-penetrating peptides, as synthetic mimics of HDPs to display potent antifungal activity, superior mammalian cells versus fungi selectivity, and strong therapeutic efficacy in treating local and systemic fungal infections. Moreover, the unique antifungal mechanism of fungal cell membrane penetration and organelle disruption explains the insusceptibility of POXs to antifungal resistance. The easy synthesis and structural diversity of POXs imply their potential as a class of promising antifungal agents.