An Effective Strategy to Develop Potent and Selective Antifungal Agents from Cell Penetrating Peptides in Tackling Drug-Resistant Invasive Fungal Infections

Autor: Yueming Wu, Weinan Jiang, Zihao Cong, Kang Chen, Yunrui She, Chao Zhong, Wenjing Zhang, Minzhang Chen, Min Zhou, Ning Shao, Guohui Xiao, Xiaoyan Shao, Yidong Dai, Jian Fei, Gonghua Song, Runhui Liu
Rok vydání: 2022
Předmět:
Zdroj: Journal of Medicinal Chemistry. 65:7296-7311
ISSN: 1520-4804
0022-2623
Popis: The high mortality rate of invasive fungal infections and quick emergence of drug-resistant fungal pathogens urgently call for potent antifungal agents. Inspired by the cell penetrating peptide (CPP) octaarginine (R8), we elongated to 28 residues poly(d,l-homoarginine) to obtain potent toxicity against both fungi and mammalian cells. Further incorporation of glutamic acid residues shields positive charge density and introduces partial zwitterions in the obtained optimal peptide polymer that displays potent antifungal activity against drug-resistant fungi superior to antifungal drugs, excellent stability upon heating and UV exposure, negligible
Databáze: OpenAIRE