The screening of a library of small molecule peptidomimetics toward secreted aspartic proteinase-2 (SAP2) of Candida albicans allowed us to identify two compounds that showed in vitro inhibitory potency comparable to pepstatin A. In an experimental model of vaginal candidiasis, the two candidate compounds were as active as a therapeutic dose of fluconazole. Importantly, this activity was fully preserved when the challenger was a fluconazole-resistant strain of the fungus. Altogether, our data demonstrate SAP2 as a valid C. albicans target for the development of new drugs against this important human pathogen.
Trabocchi, A., Mannino, C., Machetti, F., De Bernardis, F., Arancia, S., Cauda, R., Cassone, A., Guarna, A., Identification of inhibitors of drug-resistant Candida albicans strains from a library of bicyclic peptidomimetic compounds., <<JOURNAL OF MEDICINAL CHEMISTRY>>, 2010; 53 (6): 2502-2509 [http://hdl.handle.net/10807/6363]
Identification of inhibitors of drug-resistant Candida albicans strains from a library of bicyclic peptidomimetic compounds.
Cauda, Roberto;
2010
Abstract
The screening of a library of small molecule peptidomimetics toward secreted aspartic proteinase-2 (SAP2) of Candida albicans allowed us to identify two compounds that showed in vitro inhibitory potency comparable to pepstatin A. In an experimental model of vaginal candidiasis, the two candidate compounds were as active as a therapeutic dose of fluconazole. Importantly, this activity was fully preserved when the challenger was a fluconazole-resistant strain of the fungus. Altogether, our data demonstrate SAP2 as a valid C. albicans target for the development of new drugs against this important human pathogen.
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