Literature summary for 1.14.14.154 extracted from

Kudo, M.; Ohi, M.; Aoyama, Y.; Nitahara, Y.; Chung, S.K.; Yoshida, Y.
Effects of Y132H and F145L substitutions on the activity, azole resistance and spectral properties of Candida albicans sterol 14-demethylase P450 (CYP51): a live example showing the selection of altered P450 through interaction with environmental compounds (2005), J. Biochem., 137, 625-632.

Search for more literature for 1.14.14.154

Application

Application	Comment	Organism
medicine	fluconazole-resistant strain isolated from patients receiving long-term azole treatment shows Y132H and F145L substitutions	Candida albicans

Protein Variants

Protein Variants	Comment	Organism
F145L	significant modification of heme environment as judged from spectral properties, about 45% of wild-type activity, resistant to azoles	Candida albicans
Y132H	significant modification of heme environment as judged from spectral properties, about 50% of wild-type activity, resistant to azoles	Candida albicans

Inhibitors

Inhibitors	Comment	Organism	Structure
4-[5-(2,4-difluoro-phenyl)-5-imidazol-1-ylmethyl-tetrahydro-furan-3-yl]-1-isopropyl-butylamine	0.0001 mM, wild-type, 10% residual activity, mutant F145L, 35% residual activity, mutant Y132H, 60% residual activity	Candida albicans
4-[5-(2,4-difluoro-phenyl)-5-[1,2,4]triazol-1-ylmethyl-tetrahydro-furan-3-yl]-1-isopropyl-butylamine	0.0001 mM, wild-type, 25% residual activity, mutant F145L, 75% residual activity, mutant Y132H, 75% residual activity	Candida albicans
6-[5-(2,4-difluoro-phenyl)-5-imidazol-1-ylmethyl-tetrahydro-furan-3-yl]-2-methyl-hexan-3-one	0.0001 mM, wild-type, no residual activity, mutant F145L, 5% residual activity, mutant Y132H, 25% residual activity	Candida albicans
6-[5-(2,4-difluoro-phenyl)-5-[1,2,4]triazol-1-ylmethyl-tetrahydro-furan-3-yl]-2-methyl-hexan-3-one	0.0001 mM, wild-type, no residual activity, mutant F145L, 15% residual activity, mutant Y132H, 55% residual activity	Candida albicans

Organism

Organism	UniProt	Comment	Textmining
Candida albicans	P10613	-	-

Cofactor

Cofactor	Comment	Organism	Structure
cytochrome P450	-	Candida albicans

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)