Cytochromes - Cytochomes P450 - ERG11 gene - Non-Elaborate Posts - Post 4

 

 Mutations in ERG11 are a well-known mechanism of azole resistance. Point substitutions can alter the enzyme’s structure so that azole drugs no longer bind tightly. In effect, the MIC (minimum inhibitory concentration) of the drug rises and the fungus becomes resistant. For example, a classic substitution Y132H (or Y132F) in C. albicans Erg11p severely reduces fluconazole binding by disrupting the azole–heme interaction. Many other “hot-spot” mutations (in clusters around the active site) have been documented. In general, ERG11 variants from resistant isolates show amino acid changes that alter drug–target interactions.

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