Identification of a novel antifungal nonapeptide generated by combinatorial approach

Synthesis, stability and mechanistic studies of potent anticryptococcal hexapeptides

“…One such identified peptide, His-D-Trp-D-Phe-Phe-D-Phe-Lys-NH 2 exhibited antifungal activity against five pathogenic fungi in the range of 6.2 – 100 μg/mL. Further structural optimization by bio-screening of synthetic combinatorial libraries resulted in the identification of another antifungal peptide Arg-D-Trp-D-Phe-Ile-D-Phe-His-NH 2 that exhibit IC 50 value of 6.8 μM against Candida albicans [43, 44]. A detailed investigation by our group, of the above mentioned peptide resulted in several analogues with far superior antimicrobial activity [45].…”

A novel dodecapeptide from a combinatorial synthetic library exhibits potent antifungal activity and synergy with standard antimycotic agents

“…For this study we selected a novel dodecapeptide derived from our previously published nonapeptide [5]. This dodecapeptide, designated as W, exhibited low IC 50 values against the test fungi C. albicans, C. parapsilosis and C. neoformans (Table 1), which are known to cause human mycoses in a large number of cases.…”

“…Long-term treatment with the commonly used antifungals such as amphotericin B has toxic effects on the patient, flucytosine and echinocandins have a limited spectrum, while azoles may result in strain resistance [2,3]. Therefore, in the search for an alternative form of treatment for fungal infections, the last decade has seen an upsurge in new approaches, such as therapeutic antibodies and peptide molecules [4,5].…”

Combinatorial Synthesis and Directed Evolution Applied to the Production of α-Helix Forming Antimicrobial Peptides Analogues

“…These studies allowed the optimization of a lead molecule (a hexapeptide His-D-Trp-D-Phe-Phe-D-PheLys-NH2 related to the growth hormone releasing hexapeptide, GHRP-6) against pathogenic fungi [40][41][42].…”