Inhibitors of CYP51 As Antifungal Agents and Resistance to Azole Antifungals
作者： Steven L. Kelly , David C. Lamb , Diane E. Kelly
DOI: 10.1007/978-1-4615-4855-3_11
关键词: Sterol 、 Azole 、 Candida albicans 、 Cytochrome 、 Cytochrome P450 、 Fungicide 、 Metabolic pathway 、 Biochemistry 、 Ergosterol 、 Chemistry
摘要: Sterol biosynthesis is an essential metabolic pathway in animals (cholesterol), fungi (ergosterol) and plants (sitosterol) (Figure 1) requires the removal of C32-methyl group at position 14α- from precursor sterols. This reaction catalysed by a microsomal cytochrome P450, sterol 14α-demethylase (cytochrome P45051, CYP51) only P450 family found so far plants, animals. Fungal CYP51 target commercially important azole drugs fungicides, which are central to therapy (>$2bn pa) represent about one-third agrochemical fungicides used ($lbn pa). The importance compounds clinic stems emergency fungal infections, but many have also developed resistance cross-resistance agents available.
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