Synthesis of new antifungal peptides selective against Cryptococcus neoformans

Brunella Posteraro, Maurizio Sanguinetti, Giovanni Fadda, Manuela Grimaldi, Margherita De Rosa, Sara Di Marino, Mario Scrima, Annunziata Soriente, Anna Maria D'Ursi

Risultato della ricerca: Contributo in rivistaArticolo in rivistapeer review

20 Citazioni (Scopus)

Abstract

Many drugs are available for the treatment of systemic or superficial mycoses, but only a limited number of them are effective antifungal drugs, devoid of toxic and undesirable side effects. Furthermore, resistance development and fungistatic rather than fungicidal activities represent limitations of current antifungal therapy. Therefore there remains an urgent need for a new generation of antifungal agents. According to a polypharmacological approach, the present work concerns the synthesis and antifungal activity of a set of peptides designed to simultaneously target the fungal cell surface and lanosterol demethylase, a key enzyme involved in ergosterol synthesis. Our peptides include amino acid sequences characteristic of membrane-active antimicrobial peptides (AMP), and due to the presence of His residues, they carry the imidazole ring characteristic of azole compounds. The peptides synthesized by us, were tested against different yeast species, and displayed general antifungal activity, with a therapeutically promising antifungal specificity against Cryptococcus neoformans.
Lingua originaleEnglish
pagine (da-a)7985-7990
Numero di pagine6
RivistaBIOORGANIC & MEDICINAL CHEMISTRY
Volume18
DOI
Stato di pubblicazionePubblicato - 2010

Keywords

  • Amino Acid Sequence
  • Antifungal Agents
  • Antimicrobial Cationic Peptides
  • Circular Dichroism
  • Cryptococcus neoformans
  • Enzyme Inhibitors
  • Fungal Proteins
  • Microbial Sensitivity Tests
  • Protein Structure, Secondary

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