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Curr Med Chem. 2001 Jul;8(8):941-8.

Candida proteases and their inhibition: prospects for antifungal therapy.

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Department of Structural Biology, Abbott Laboratories, Abbott Park, IL 60064, USA. STEWARTK@RAND.PPRD.Abbott.Com


The rationale for inhibition of the secreted acid proteases (SAP) of Candida fungal species as a novel antifungal strategy is outlined. Enzyme structure-activity relationship data regarding the inhibitor A-70450 are described along with results from in vivo antifungal assays. Developments from protein X-ray crystallographic studies, SAP knock-out genetic studies, and the importance of these new results for drug discovery are reviewed. Finally, inhibition of the Candida SAP enzymes with HIV protease inhibitors and a proposed role in candidiasis of AIDS patients is discussed.

[Indexed for MEDLINE]

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