Gramicidin-S-Inspired Cyclopeptidomimetics as Potent Membrane-Active Bactericidal Agents with Therapeutic Potential

作者: Yi Jin , Rémy Campagne , Valérie Alezra , Emeric Miclet , Jinhua Zhu

DOI: 10.1002/CMDC.202000568

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摘要: Antimicrobial peptides (AMPs) are promising antibacterial agents often hindered by their undesired hemolytic activity. Inspired gramicidin S (GS), a well-known cyclodecapeptide, we synthesized panel of cyclopeptidomimetics using β,γ-diamino acids (β,γ-DiAAs). We observed that peptidomimetic CP-2 displays bactericidal activity similar to GS while possessing lower side-effects. Moreover, extensive studies revealed likely kills bacteria through membrane disruption. Altogether, is membrane-active antibiotic with therapeutic potential.

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