Azoles - Fluconazole - (Digital) Tree Post Series - Continuation to "Cytochromes - Cytochomes P450 - ERG11 gene - Non-Elaborate Posts - Post 5 (Continuation to Post 4)" - Post 3

 

 

ERG11 mutations are not randomly distributed. They often occur in "hotspot" regions of the gene that encode critical parts of the enzyme’s active site.

Mutations in these hotspots have a disproportionately high effect on drug resistance.

One of the best-characterized mutations is Y132H.

This substitution changes the polarity and structure near the fluconazole-binding site, dramatically lowering drug affinity and conferring resistance.


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