Evaluation of peptoid mimics of short, lipophilic peptide antimicrobials.

International Journal of Antimicrobial Agents
R Madison Green, Kevin L Bicker

Abstract

Antimicrobial peptides are proving to be promising lead compounds for therapeutics. The major disadvantage of antimicrobial peptides is their proteolytic instability in the body, with half-lives averaging less than an hour. Peptoids, or N-substituted glycines, have emerged as a promising field of peptidomimetics by retaining the beneficial properties of antimicrobial peptides while improving their stability. This study evaluated peptoid derivatives of ultra-short lipophilic antimicrobial peptides, comparing their potency side-by-side with the most prevalent multidrug-resistant bacteria (ESKAPE) and yeast pathogens (Candida albicans and Cryptococcus neoformans). Both peptide and peptoid counterparts were most effective against Gram-positive bacteria with minimum inhibitory concentration (MIC) values as low as 1.6 and 6.3 µg/mL, respectively. In general, peptides retained better antimicrobial activity than their peptoid counterparts; however, certain peptoids proved to be more effective than peptides against Gram-negative bacteria. For example, peptoid MG10 displayed an MIC of 6.3 µg/mL against Pseudomonas aeruginosa compared with the peptide counterpart with an MIC of 100 µg/mL. All tested compounds were more potent against Cryp...Continue Reading

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Citations

Sep 2, 2020·Chemical Communications : Chem Comm·Kevin L Bicker, Steven L Cobb
Jul 28, 2020·The Biochemical Journal·Sarah A MannBryan Knuckley
May 16, 2021·Bioorganic & Medicinal Chemistry·Luana AlvesCarlos A Montanari
Sep 18, 2021·ACS Medicinal Chemistry Letters·R Madison Green, Kevin L Bicker
Oct 7, 2021·Chemical Communications : Chem Comm·Claudine Nicole HerlanStefan Bräse
Nov 13, 2021·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·Kang DingXiangli Dang

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