CHIMIA International Journal for Chemistry 2011-01-01

Chitin synthase, a fungal glycosyltransferase that is a valuable antifungal target.

Jean-Bernard Behr

Index: Chimia 65(1-2) , 49-53, (2011)

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Abstract

During the last 30 past years, more life-threatening fungal infections have appeared due to the increasing frequency of patients with weakened immune systems. Inhibition of fungal enzymes involved in the biosynthesis of sterols is considered to be a safe and effective option for antifungal therapy. However, the intensive use of sterol-biosynthesis inhibitors for years has resulted in resistance development. Consequently, the search for alternative therapeutics must be intensified. In this context, the biosynthesis of chitin, an essential component of the fungal cell wall that is absent in mammalian cells, was envisioned as a safe and selective therapeutic target. We present here recent successes in the inhibition of chitin synthase, the enzyme involved in the last step of the biosynthesis of chitin.