Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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.


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