Lanosterol 14 alpha-demethylase
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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]
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[edit] References
This article incorporates CC-BY-2.5 text from the reference[2]
- ^ Vanden Bossche H, Dromer F, Improvisi I, Lozano-Chiu M, Rex JH, Sanglard D (1998). "Antifungal drug resistance in pathogenic fungi". Med. Mycol. 36 Suppl 1: 119–28. PMID 9988500.
- ^ a b c d Mullins J. G. L., Parker J. E., Cools H. J., Togawa R. C., Lucas J. A., et al. (2011). "Molecular Modelling of the Emergence of Azole Resistance in Mycosphaerella graminicola. PLoS ONE 6(6): e20973. doi:10.1371/journal.pone.0020973.
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| CYP1 |
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| CYP2 |
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| CYP3 (CYP3A) |
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| CYP4 |
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| CYP5-20 |
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| CYP21-51 |
CYP21 ( A2) · CYP24 ( A1) · CYP26 ( A1, B1, C1) · CYP27 ( A1, B1, C1) · CYP39 ( A1) · CYP46 ( A1) · CYP51 ( A1)
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