Journal
FRONTIERS IN CHEMISTRY
Volume 5, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fchem.2017.00026
Keywords
antimicrobial peptide; frog-skin; antibiotic-resistance; D-amino acids; gold nanoparticles; Pseudomonas aeruginosa
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Funding
- Sapienza University of Rome (Ricerca Universita)
- FILAS Grant [FILAS RU-2014-1020]
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Antimicrobial peptides (AMPs) represent an interesting class ofmolecules with expanding biological properties which make them a viable alternative for the development of future antibiotic drugs. However, for this purpose, some limitations must be overcome: (i) the poor biostability due to enzymatic degradation; (ii) the cytotoxicity at concentrations slightly higher than the therapeutic dosages; and (iii) the inefficient delivery to the target site at effective concentrations. Recently, a derivative of the frog skin AMP esculentin-1a, named esculentin-1a(1-21) NH2, [Esc(1-21): GIFSKLAGKKIKNLLISGLKG-NH2] has been found to have a potent activity against the Gram-negative bacterium Pseudomonas aeruginosa; a slightly weaker activity against Gram-positive bacteria and interesting immunomodulatory properties. With the aim to optimize the antimicrobial features of Esc(1-21) and to circumvent the limitations described above, two different approaches were followed: (i) substitutions by non-coded amino acids, i. e., a -aminoisobutyric acid or D-amino acids; and (ii) peptide conjugation to gold nanoparticles. In this mini-review, we summarized the structural and functional properties of the resulting Esc(1-21)-derived compounds. Overall, our data may assist researchers in the rational design and optimization of AMPs for the development of future drugs to fight the worldwide problem of antibiotic resistance.
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