Oxygenated derivatives of cholesterol (oxysterols) present a remarkably diverse profile of biological activities, including effects on sphingolipid metabolism, platelet aggregation, apoptosis, and ...

Oxysterols: modulators of cholesterol metabolism and other processes.

The OLE1 gene of Saccharomyces cerevisiae encodes the delta 9 fatty acid desaturase and can be functionally replaced by the rat stearoyl-CoA desaturase gene.

Sterol 14α-Demethylase Cytochrome P450 (CYP51), a P450 in all Biological Kingdoms

Cytochrome P450s (P450s) are subject to inhibition/inactivation by various chemically diverse agents, which may interact directly or indirectly with either the P450 prosthetic heme or the protein moiety or with both moieties. This inhibition is clinically relevant, as it can block physiological pathways as well as result in therapeutically significant beneficial or adverse effects and clinically relevant drug–drug interactions. Herein, we discuss the various chemical agents and their chemical mechanisms that lead to such reversible, quasi-irreversible, or irreversible inhibition of these enzymes. We note that such inhibition targeted at P450-dependent physiological and/or pathological processes has been ingeniously and effectively harnessed not only in the design and development of clinically relevant therapeutic agents but also of fungicides, insecticides, and herbicides.

Inhibition of Cytochrome P450 Enzymes

Material dealing with the chemistry, biochemistry, and biological activities of oxysterols is reviewed for the period 1987-1995. Particular attention is paid to the presence of oxysterols in tissues and foods and to their physiological relevance.

Review of progress in sterol oxidations: 1987–1995

7-Oxo-24,25-dihydrolanosterol: a novel lanosterol 14α-demethylase (P-45014DM) inhibitor which blocks electron transfer to the oxyferro intermediate

Mutant and immunochemical studies on the involvement of cytochrome b5 in fatty acid desaturation by yeast microsomes

Inhibition by a novel azole antifungal agent with a geranyl group on lanosterol 14α-demethylase of yeast

Selectivity of isoprenoid-containing imidazole antifungal compounds for sterol 14-demethylase P450 (P45014dm) and 7-ethoxycoumarin O-deethylase P450 of rat liver microsomes

Yoshida Yuzo

Papers

7-Oxo-24,25-dihydrolanosterol: a novel lanosterol 14α-demethylase (P-45014DM) inhibitor which blocks electron transfer to the oxyferro intermediate

Mutant and immunochemical studies on the involvement of cytochrome b5 in fatty acid desaturation by yeast microsomes

Inhibition by a novel azole antifungal agent with a geranyl group on lanosterol 14α-demethylase of yeast

Selectivity of isoprenoid-containing imidazole antifungal compounds for sterol 14-demethylase P450 (P45014dm) and 7-ethoxycoumarin O-deethylase P450 of rat liver microsomes