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Keywords = dendrimeric γ-AApeptides

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9 pages, 2709 KB  
Communication
Short, Lipidated Dendrimeric γ-AApeptides as New Antimicrobial Peptidomimetics
by Yafeng Wang, Menglin Xue, Ruixuan Gao, Soumyadeep Chakraborty, Shaohui Wang, Xue Zhao, Meng Gu, Chuanhai Cao, Xingmin Sun and Jianfeng Cai
Int. J. Mol. Sci. 2023, 24(7), 6407; https://doi.org/10.3390/ijms24076407 - 29 Mar 2023
Cited by 5 | Viewed by 2152
Abstract
Antibiotic resistance is one of the most significant issues encountered in global health. There is an urgent demand for the development of a new generation of antibiotic agents combating the emergence of drug resistance. In this article, we reported the design of lipidated [...] Read more.
Antibiotic resistance is one of the most significant issues encountered in global health. There is an urgent demand for the development of a new generation of antibiotic agents combating the emergence of drug resistance. In this article, we reported the design of lipidated dendrimeric γ-AApeptides as a new class of antimicrobial agents. These AApeptides showed excellent potency and broad-spectrum activity against both Gram-positive bacteria and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). The mechanistic studies revealed that the dendrimeric AApeptides could kill bacteria rapidly through the permeabilization of bacterial membranes, analogous to host-defense peptides (HDPs). These dendrimers also did not induce antibiotic resistance readily. The easy access to the synthesis, together with their potent and broad-spectrum activity, make these lipidated dendrimeric γ-AApeptides a new generation of antibacterial agents. Full article
(This article belongs to the Special Issue Small Molecule Drug Design and Research 2.0)
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