New Small-Size Antifungal Peptides: Design, Synthesis and Antifungal Activity

Author(s): Adriana D. Garro, Francisco M. Garibotto, Ana M. Rodriguez, Marcela Raimondi, Susana A. Zacchino, Andras Perczel, Csaba Somlai, Botond Penke, Ricardo D. Enriz.

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 6 , 2011

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The synthesis, in vitro evaluation and conformational study of small-size peptides acting as antifungal agents are reported. These peptides displayed antifungal activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans. Among the peptides reported here, RQWRRWWQR-NH2 exhibited the strongest activity against Cryptococcus neoformans. Our results allowed us to reduce in size these bioactive peptides from 16 to 11 and to 9 amino acid residues in total. Despite their reduction, they still maintained and even enhanced the antifungal activity detected for penetratin. A conformational and electronic structure analysis on these peptides was also performed by using molecular mechanics calculations in conjunction with Molecular Electrostatic Potentials (MEP) maps.

Keywords: Antifungals, Conformational and Electronic Study, Molecular Electrostatic Potentials, Peptides, Antifungal Peptides:, Cryptococcus neoformans, Molecular Electrostatic Potentials (MEP), nature's antibiotics, Cell-penetrating peptides (CPPs), LKB Bromma apparatus, Penetratin, Antennapedia, Candida albicans

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Article Details

Year: 2011
Page: [562 - 567]
Pages: 6
DOI: 10.2174/157018011795906785
Price: $58

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