IMIBIO-SL   20937
INSTITUTO MULTIDISCIPLINARIO DE INVESTIGACIONES BIOLOGICAS DE SAN LUIS
Unidad Ejecutora - UE
artículos
Título:
Penetratin analogues acting as antifungal agents
Autor/es:
FRANCISCO M. GARIBOTTO, ADRIANA D. GARRO, ANA M. RODRÍGUEZ, MARCELA RAIMONDI, SUSANA A. ZACCHINO, CSABA SOMLAI, BOTOND PENKE Y RICARDO D. ENRIZ.
Revista:
EUROPEAN JOURNAL OF MEDICAL CHEMISTRY
Editorial:
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Referencias:
Año: 2010
ISSN:
0223-5234
Resumen:
The synthesis, in vitro evaluation, and conformational study of penetratin analogues acting as antifungal
agents are reported. Different peptides structurally related with penetratin were evaluated. Analogues of
penetratin rich in Arg, Lys and Trp amino acids were tested. In addition, HFRWRQIKIWFQNRRM[O]KWKKNH2,
a synthetic 20 amino acid peptide was also evaluated. These penetratin analogues displayed antifungal
activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans.
In contrast, Tat peptide, a well-known cell penetrating peptide, did not show a significant antifungal
activity against fungus tested here. We also performed a conformational study by means experimental
and theoretical approaches (CD spectroscopic measurements and MD simulations). The electronic
structure analysis was carried out fromMolecular Electrostatic Potentials (MEP) obtained by using RHF/6-
31G ab initio calculations. Our experimental and theoretical results permitted us to identify a topographical
template which may provide a guide for the design of new peptides with antifungal effects.in vitro evaluation, and conformational study of penetratin analogues acting as antifungal
agents are reported. Different peptides structurally related with penetratin were evaluated. Analogues of
penetratin rich in Arg, Lys and Trp amino acids were tested. In addition, HFRWRQIKIWFQNRRM[O]KWKKNH2,
a synthetic 20 amino acid peptide was also evaluated. These penetratin analogues displayed antifungal
activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans.
In contrast, Tat peptide, a well-known cell penetrating peptide, did not show a significant antifungal
activity against fungus tested here. We also performed a conformational study by means experimental
and theoretical approaches (CD spectroscopic measurements and MD simulations). The electronic
structure analysis was carried out fromMolecular Electrostatic Potentials (MEP) obtained by using RHF/6-
31G ab initio calculations. Our experimental and theoretical results permitted us to identify a topographical
template which may provide a guide for the design of new peptides with antifungal effects.2,
a synthetic 20 amino acid peptide was also evaluated. These penetratin analogues displayed antifungal
activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans.
In contrast, Tat peptide, a well-known cell penetrating peptide, did not show a significant antifungal
activity against fungus tested here. We also performed a conformational study by means experimental
and theoretical approaches (CD spectroscopic measurements and MD simulations). The electronic
structure analysis was carried out fromMolecular Electrostatic Potentials (MEP) obtained by using RHF/6-
31G ab initio calculations. Our experimental and theoretical results permitted us to identify a topographical
template which may provide a guide for the design of new peptides with antifungal effects.Candida albicans and Cryptococcus neoformans.
In contrast, Tat peptide, a well-known cell penetrating peptide, did not show a significant antifungal
activity against fungus tested here. We also performed a conformational study by means experimental
and theoretical approaches (CD spectroscopic measurements and MD simulations). The electronic
structure analysis was carried out fromMolecular Electrostatic Potentials (MEP) obtained by using RHF/6-
31G ab initio calculations. Our experimental and theoretical results permitted us to identify a topographical
template which may provide a guide for the design of new peptides with antifungal effects.ficant antifungal
activity against fungus tested here. We also performed a conformational study by means experimental
and theoretical approaches (CD spectroscopic measurements and MD simulations). The electronic
structure analysis was carried out fromMolecular Electrostatic Potentials (MEP) obtained by using RHF/6-
31G ab initio calculations. Our experimental and theoretical results permitted us to identify a topographical
template which may provide a guide for the design of new peptides with antifungal effects.ab initio calculations. Our experimental and theoretical results permitted us to identify a topographical
template which may provide a guide for the design of new peptides with antifungal effects.