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Molecules 2017, 22(7), 1217; doi:10.3390/molecules22071217

Cyclic Peptides as Novel Therapeutic Microbicides: Engineering of Human Defensin Mimetics

1
Department of Pharmacy, University of Naples Federico II, via Mezzocannone 16, 80134 Naples, Italy
2
Dipartimento di Scienze e Tecnologie Ambientali Biologiche Farmaceutiche, University of Campania “Luigi Vanvitelli”, Via G. Vivaldi 42, 81100 Caserta, Italy
3
CEINGE-Biotecnologie Avanzate Scarl, Via G. Salvatore 486, 80145 Napoli, Italy
4
Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università degli Studi di Napoli “Federico II”, 80131 Napoli, Italy
These two authors contributed equally.
*
Authors to whom correspondence should be addressed.
Received: 28 June 2017 / Revised: 17 July 2017 / Accepted: 18 July 2017 / Published: 20 July 2017
(This article belongs to the Special Issue Peptide-Based Drugs and Drug Delivery Systems)
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Abstract

Cyclic peptides are receiving significant attention thanks to their antimicrobial activity and high serum stability, which is useful to develop and design novel antimicrobial agents. Antimicrobial peptides appear to be key components of innate defences against bacteria, viruses, and fungi. Among the others, defensins possess a strong microbicidial activity. Defensins are cationic and amphipathic peptides with six cysteine residues connected by three disulfide bonds found in plants, insects, and mammals; they are divided in three families: α-, β-, and θ-defensins. α-Defensins are contained in the primary granules of human neutrophils; β-defensins are expressed in human epithelia; and θ-defensins are pseudo-cyclic defensins not found in humans, but in rhesus macaques. The structural diversities among the three families are reflected in a different antimicrobial action as well as in serum stability. The engineering of these peptides is an exciting opportunity to obtain more functional antimicrobial molecules highlighting their potential as therapeutic agents. The present review reports the most recent advances in the field of cyclic peptides with a specific regard to defensin analogs. View Full-Text
Keywords: defensins; defensin analogs; antimicrobial drugs; cyclic peptides defensins; defensin analogs; antimicrobial drugs; cyclic peptides
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Falanga, A.; Nigro, E.; De Biasi, M.G.; Daniele, A.; Morelli, G.; Galdiero, S.; Scudiero, O. Cyclic Peptides as Novel Therapeutic Microbicides: Engineering of Human Defensin Mimetics. Molecules 2017, 22, 1217.

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