Page last updated: 2024-10-24

cholesterol 24-hydroxylase activity

Definition

Target type: molecularfunction

Catalysis of the reaction: cholesterol + H+ + NADPH + O2 = (24S)-24-hydroxycholesterol + H2O + NADP+. [EC:1.14.14.25, RHEA:22716]

Cholesterol 24-hydroxylase activity is a crucial enzymatic function involved in the metabolism and detoxification of cholesterol. It catalyzes the hydroxylation of cholesterol at the C24 position, converting it into 24S-hydroxycholesterol. This reaction is a critical step in the bile acid synthesis pathway, which plays a vital role in the elimination of excess cholesterol from the body. 24S-hydroxycholesterol serves as a precursor to bile acids, which are synthesized in the liver and secreted into the bile. Bile acids aid in the digestion and absorption of fats in the small intestine. In addition to its role in bile acid synthesis, cholesterol 24-hydroxylase activity is also involved in cholesterol homeostasis. It helps regulate the levels of cholesterol in the body by removing excess cholesterol from circulation. Furthermore, cholesterol 24-hydroxylase activity has been implicated in the regulation of immune responses and the development of certain types of cancers. The enzyme is expressed in various tissues, including the liver, brain, and immune cells. Its activity is tightly regulated by a complex interplay of factors, including hormones, dietary cholesterol levels, and other signaling molecules.'
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Proteins (2)

ProteinDefinitionTaxonomy
Cholesterol 24-hydroxylaseA cytochrome P450 46A1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y6A2]Homo sapiens (human)
Cholesterol 24-hydroxylaseA cytochrome P450 46A1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y6A2]Homo sapiens (human)

Compounds (6)

CompoundDefinitionClassesRoles
efavirenzefavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.

efavirenz: HIV-1 reverse transcriptase inhibitor
acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound
antiviral drug;
HIV-1 reverse transcriptase inhibitor
cholesteryl sulfatecholesterol sulfate : A steroid sulfate that is cholesterol substituted by a sulfoxy group at position 3.

cholesteryl sulfate: component of human seminal plasma & spermatozoa; RN given refers to (3beta)-isomer
steroid sulfatehuman metabolite
voriconazolevoriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.

Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.
conazole antifungal drug;
difluorobenzene;
pyrimidines;
tertiary alcohol;
triazole antifungal drug
P450 inhibitor
pregnenolone sulfatepregnenolone sulfate: RN given refers to (3 beta)-isomersteroid sulfateEC 2.7.1.33 (pantothenate kinase) inhibitor;
human metabolite
8-hydroxyefavirenz
thioperamidethioperamide: structure given in first source; histamine H3 receptor antagonistprimary aliphatic amine