基于人防御素的仿生肽抗生素的发现。

Department of Anesthesiology and Intensive Care, The First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310003, China.

National Clinical Research Center for Child Health, Children's Hospital, School of Medicine, Zhejiang University, Hangzhou 310052, China.

Proc Natl Acad Sci U S A. 2022 Mar 8;119(10):e2117283119. doi: 10.1073/pnas.2117283119. Epub 2022 Mar 1.

SignificanceWe report the development of peptidomimetic antibiotics derived from a natural antimicrobial peptide, human α-defensin 5. By engaging multiple bacterial targets, the lead compound is efficacious in vitro and in vivo against bacteria with highly inducible antibiotic resistance, promising a useful therapeutic agent for the treatment of infections caused by antibiotic-resistant bacteria.

意义我们报告了源自天然抗菌肽人α-防御素 5 的肽模拟抗生素的开发。通过与多个细菌靶标结合，先导化合物在体外和体内对具有高度诱导性抗生素耐药性的细菌有效，有望成为治疗抗生素耐药菌引起的感染的有用治疗剂。