Abstract
Antimicrobial peptides are promising candidates for anti-infective pharmaceuticals. Unfortunately, because of their low proteolytic and chemical stability, their usage is generally narrowed down to topical formulations. Until now, numerous approaches to increase peptide stability have been proposed. One of them, peptide hydrocarbon stapling, a modification based on stabilizing peptide secondary structure with a side-chain covalent hydrocarbon bridge, have been successfully applied to many peptides. Moreover, constraining secondary structure of peptides have also been proven to increase their biological activity. This review article describes studies on hydrocarbon stapled antimicrobial peptides with respect to improved drug-like properties.
Highlights
Increasing resistance to antibiotics among microorganisms is a serious threat for human health
This review focuses on the latest achievements in the development of hydrocarbon stapled antimicrobial peptides
Antibiotic-resistant bacterial infections are becoming a serious threat for mankind
Summary
Increasing resistance to antibiotics among microorganisms is a serious threat for human health. Current unsatisfactory situation is a result of complex processes It is associated with a worldwide overuse of antibiotics in humans and animals resulting in selection of drug-resistant strains [2]. Process inhibition, with no membrane disruption have been observed Those AMPs with cell penetrating peptide (CPP) properties may provide a new delivery systems for known drugs [7, 8]. Many approaches have been proposed to improve serum stability and to increase antimicrobial activity [15,16,17], inter alia, d-amino acid substitution [18] or other non-ribosomal amino acid substitution [19], PEGylation [20], lipidization [21], and dimerization [22] Another AMP design approach is peptide stapling. The article presents some aspects of design and synthesis of the peptides as well as their effects on overall biological activity, stability, and structure
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