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Title: 14α-demethylase  
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Subject: Fluconazole, Azole
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cytochrome P450, family 51, subfamily A, polypeptide 1
Symbol CYP51A1
Alt. symbols CYP51, P45014DM
Entrez HUGO OMIM RefSeq UniProt EC number Locus q21.2-21.3

Lanosterol 14 α-demethylase (or CYP51A1, P45014DM) is a cytochrome P450 (family 51, subfamily A, polypeptide 1) enzyme that converts lanosterol to cholesterol.

It is a target for antifungal drugs, inhibiting the production of ergosterol. Over-expression of CYP51A1 can lead to resistance to these antifungals.[1]

Azole fungicides are demethylase inhibitors that inhibit CYP51 activity.[2] CYP51 is a cytochrome P450 that catalyses the oxidative removal of the 14α-methyl group of lanosterol or eburicol in yeasts and fungi - an essential step in the production of sterols.[2] Azoles bind as the sixth ligand to the haem in CYP51 via the unprotonated N atom thus occupying the active site and acting as non-competitive inhibitors.[2]

See also

  • Antifungal drug


This article incorporates CC-BY-2.5 text from the reference[2]

External links

  • Medical Subject Headings (MeSH)
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