Target intelligence / Profile preview

14α-lanosterol demethylase

Molecular classification
Enzyme, Cytochrome P450
01

Overview

14α-lanosterol demethylase (CYP51A1) is a cytochrome P450 enzyme that catalyzes the oxidative removal of the 14α-methyl group from lanosterol, an essential step in the conversion of lanosterol to cholesterol in animals and ergosterol in fungi. It is a key target for azole antifungal drugs, which inhibit ergosterol synthesis in fungi.

Other names
Lanosterol 14α-demethylaseCYP51A1CYP51P45014DM
02

Mechanism of action

Inhibition of ergosterol synthesis by binding to the heme iron in the active site.

03

Biological functions

Cholesterol/ergosterol biosynthetic processOxidation-reduction processCellular response to drugSteroid/sterols bindingHeme bindingIron ion bindingSteroid/sterols monooxygenase activity
04

Disease associations

InfectionCancer
05

Safety considerations

Potential for off-target effects due to structural similarity with other cytochrome P450 enzymes.Drug resistance in fungi due to mutations in CYP51A1.Lack of potency/selectivity against human forms compared with microbial ones.
06

Interacting drugs

Imidazoles

2 more in the full profile.

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