Journal ArticleDOI
Amphipathic, α‐helical antimicrobial peptides
TLDR
This review considers alpha-helical, antimicrobial peptides from the point of view of six interrelated structural and physicochemical parameters that modulate their activity and specificity: sequence, size, structuring, charge, amphipathicity, and hydrophobicity.Abstract:
Gene-encoded antimicrobial peptides are an important component of host defense in animals ranging from insects to mammals. They do not target specific molecular receptors on the microbial surface, but rather assume amphipathic structures that allow them to interact directly with microbial membranes, which they can rapidly permeabilize. They are thus perceived to be one promising solution to the growing problem of microbial resistance to conventional antibiotics. A particularly abundant and widespread class of antimicrobial peptides are those with amphipathic, alpha-helical domains. Due to their relatively small size and synthetic accessibility, these peptides have been extensively studied and have generated a substantial amount of structure-activity relationship (SAR) data. In this review, alpha-helical antimicrobial peptides are considered from the point of view of six interrelated structural and physicochemical parameters that modulate their activity and specificity: sequence, size, structuring, charge, amphipathicity, and hydrophobicity. It begins by providing an overview of how these vary in peptides from different natural sources. It then analyzes how they relate to the currently accepted model for the mode of action of alpha-helical peptides, and discusses what the numerous SAR studies that have been carried out on these compounds and their analogues can tell us. A comparative analysis of the many alpha-helical, antimicrobial peptide sequences that are now available then provides further information on how these parameters are distributed and interrelated. Finally, the systematic variation of parameters in short model peptides is used to throw light on their role in antimicrobial potency and specificity. The review concludes with some considerations on the potentials and limitations for the development of alpha-helical, antimicrobial peptides as antiinfective agents.read more
Citations
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Antimicrobial peptides: pore formers or metabolic inhibitors in bacteria?
TL;DR: In this review the different models of antimicrobial-peptide-induced pore formation and cell killing are presented and several observations suggest that translocated peptides can alter cytoplasmic membrane septum formation, inhibit cell-wall synthesis, inhibit nucleic-acid synthesis, inhibits protein synthesis or inhibit enzymatic activity.
Journal ArticleDOI
beta-Peptides: from structure to function.
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Mode of action of membrane active antimicrobial peptides.
TL;DR: Although many studies support that bacterial membrane damage is a lethal event for bacteria, other studies point to a multihit mechanism in which the peptide binds to several targets in the cytoplasmic region of the bacteria.
Journal ArticleDOI
QSAR Modeling: Where have you been? Where are you going to?
Artem Cherkasov,Eugene N. Muratov,Eugene N. Muratov,Denis Fourches,Alexandre Varnek,Igor I. Baskin,Mark T. D. Cronin,John C. Dearden,Paola Gramatica,Yvonne C. Martin,Roberto Todeschini,Viviana Consonni,Victor E. Kuz’min,Richard D. Cramer,Romualdo Benigni,Chihae Yang,James F. Rathman,Lothar Terfloth,Johann Gasteiger,Ann M. Richard,Alexander Tropsha +20 more
TL;DR: In this paper, the authors provide guidelines for QSAR development, validation, and application, which are summarized in best practices for building rigorously validated and externally predictive quantitative structure-activity relationship models.
Journal ArticleDOI
Polymeric materials with antimicrobial activity
TL;DR: The state of the art in the field of antimicrobial polymeric systems during the last decade is described in this paper, where a classification of the different materials is carried out dividing basically those synthetic polymers that exhibit antimicrobial activity by themselves; those whose biocidal activity is conferred through their chemical modification; those that incorporate antimicrobial organic compounds with either low or high molecular weight; and those that involve the addition of active inorganic systems.
References
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