Esculentins-1 are a family of frog skin antimicrobial peptides (AMPs), characterized by a 46 amino acids primary structure and a broad range of antimicrobial activity. Studies on the mode of action of amphibian AMPs evidenced that bacterial membranes are their major target. Esculentins possess the basic features common to most linear AMPs, that is an overall positive charge at neutral pH and a considerable proportion of hydrophobic residues. These properties allow the peptides to bind to the negatively-charged microbial membranes by folding into an amphiphilic structure, thus perturbing membrane permeability. Esculentin 1-21 [Esc(1-21)], consists of the first 20 aminoacids of the naturally occurring Esculentin 1a, with a glycinamide residue at the C-terminus: H-Gly-Ile-Phe-Ser-Lys-Leu-Ala-Gly-Lys-Gly-Leu-Lys-Asn-Leu-Leu-Ile-Ser-Gly-Leu-Lys-Gly-NH2. It was previously demonstrated that Esc(1-21) is highly potent against the most common mastitis-causing microbes in dairy cattle (e.g. Stre
Synthesis and preliminary studies on an esculentin analog carrying Aib residues / Biondi, B.; Crisma, M.; Formaggio, F.; Casciaro, Bruno; Di Grazia, A.; Mangoni, Maria Luisa. - ELETTRONICO. - (2013). (Intervento presentato al convegno Convegno della Divisione di Chimica dei Sistemi Biologici della Società Chimica Italiana tenutosi a Bertinoro (FC) nel 19-20 settembre).
Synthesis and preliminary studies on an esculentin analog carrying Aib residues
CASCIARO, BRUNO;MANGONI, Maria Luisa
2013
Abstract
Esculentins-1 are a family of frog skin antimicrobial peptides (AMPs), characterized by a 46 amino acids primary structure and a broad range of antimicrobial activity. Studies on the mode of action of amphibian AMPs evidenced that bacterial membranes are their major target. Esculentins possess the basic features common to most linear AMPs, that is an overall positive charge at neutral pH and a considerable proportion of hydrophobic residues. These properties allow the peptides to bind to the negatively-charged microbial membranes by folding into an amphiphilic structure, thus perturbing membrane permeability. Esculentin 1-21 [Esc(1-21)], consists of the first 20 aminoacids of the naturally occurring Esculentin 1a, with a glycinamide residue at the C-terminus: H-Gly-Ile-Phe-Ser-Lys-Leu-Ala-Gly-Lys-Gly-Leu-Lys-Asn-Leu-Leu-Ile-Ser-Gly-Leu-Lys-Gly-NH2. It was previously demonstrated that Esc(1-21) is highly potent against the most common mastitis-causing microbes in dairy cattle (e.g. StreI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
