Cytochromes - Cytochomes P450 - ERG11 gene - Non-Elaborate Posts - Post 9

 

 Mechanistically, ERG11 mutations lower azole binding affinity. Structural analyses and mutagenesis studies have shown that many resistance mutations cluster near the heme and substrate channel.

By changing side chains in the binding pocket, these mutations prevent the triazole ring from coordinating the iron, so the drug can no longer inhibit Erg11p effectively. In other words, the fungus has traded some enzymatic efficiency for drug resistance: the mutant Erg11p still processes sterols (often somewhat slower) but no longer binds azoles tightly.

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