CYP27A1: A Potential Drug Target and Metabolism Enzyme (G1593)

Target Name: CYP27A1

NCBI ID: G1593

CYP27A1: A Potential Drug Target and Metabolism Enzyme

CYP27A1, a member of the cytochrome P450 (CYP) gene family, is a widely expressed enzyme that is involved in the metabolism of various drugs and endogenous compounds. One of its primary functions is the conversion of the metabolite of the drug alfuzosin, which is an anti-diabetic drug, to its active metabolite, irinotecan, which is excreted in the urine and feces.

CYP27A1 is a member of the subfamily A of the CYP27 gene family, which consists of six subfamilies, including subfamily A. These subfamilies are characterized by the presence of a specific amino acid residue, which is important for the stability and activity of the enzyme. CYP27A1 is characterized by the presence of the amino acid residue Asp-27, which is located at position 27 on the R-subunit of the enzyme.

CYP27A1 is a cytoplasmic protein that is expressed in various cell types of the body, including the liver, heart, kidney, and intestine. It is primarily localized to the mitochondria, where it is involved in the metabolism of a wide variety of compounds, including drugs, toxins, and other exogenous substances. CYP27A1 is also expressed in the endoplasmic reticulum (ER), where it can be internalized and processed by endoplasmic reticulum-resident proteins (ERPs).

CYP27A1 has been identified as a potential drug target due to its involvement in the metabolism of a wide variety of drugs, including anti-diabetic drugs, which are often metabolized by CYP27A1 to their active metabolites. The metabolism of these drugs can be affected by genetic variations in the CYP27A1 gene, which can result in altered levels of metabolites and potential drug interactions. For example, studies have shown that individuals with certain genetic variations in the CYP27A1 gene are at increased risk of developing drug-induced lactic acidosis, a potentially life-threatening condition that can occur as a complication of certain medications.

In addition to its role in drug metabolism, CYP27A1 is also involved in the metabolism of other compounds, including toxins and other exogenous substances. For example, CYP27A1 is involved in the metabolism of the neurotransmitter serotonin, which is involved in mood regulation and other physiological processes. CYP27A1 has also been shown to be involved in the metabolism of other drugs, including chemotherapy drugs, angiotensin-converting enzyme (ACE) inhibitors, and diuretics.

CYP27A1 is also a potential biomarker for a variety of diseases, including cancer, cardiovascular disease, and neurodegenerative diseases. For example, studies have shown that individuals with certain genetic variations in the CYP27A1 gene are at increased risk of developing pancreatic cancer, a particularly aggressive and deadly form of cancer. In addition, CYP27A1 has been shown to be involved in the metabolism of a variety of neurodegenerative diseases, including Alzheimer's disease and Parkinson's disease.

The CYP27A1 gene has also been the subject of extensive research in the field of pharmacology, with a focus on the identification and characterization of drug targets and inhibitors. Several studies have shown that CYP27A1 can be targeted by small molecules, including inhibitors of its catalytic activity and modulators of its expression. In addition, several studies have shown that modulation of CYP27A1 activity can be a useful strategy for the development of new anti-drug

Protein Name: Cytochrome P450 Family 27 Subfamily A Member 1

Functions: Cytochrome P450 monooxygenase that catalyzes regio- and stereospecific hydroxylation of cholesterol and its derivatives. Hydroxylates (with R stereochemistry) the terminal methyl group of cholesterol side-chain in a three step reaction to yield at first a C26 alcohol, then a C26 aldehyde and finally a C26 acid (PubMed:9660774, PubMed:12077124, PubMed:21411718, PubMed:28190002). Regulates cholesterol homeostasis by catalyzing the conversion of excess cholesterol to bile acids via both the 'neutral' (classic) and the 'acid' (alternative) pathways (PubMed:9660774, PubMed:1708392, PubMed:11412116, PubMed:2019602, PubMed:7915755, PubMed:9186905, PubMed:9790667). May also regulate cholesterol homeostasis via generation of active oxysterols, which act as ligands for NR1H2 and NR1H3 nuclear receptors, modulating the transcription of genes involved in lipid metabolism (PubMed:9660774, PubMed:12077124). Plays a role in cholestanol metabolism in the cerebellum. Similarly to cholesterol, hydroxylates cholestanol and may facilitate sterol diffusion through the blood-brain barrier to the systemic circulation for further degradation (PubMed:28190002). Also hydroxylates retinal 7-ketocholesterol, a noxious oxysterol with pro-inflammatory and pro-apoptotic effects, and may play a role in its elimination from the retinal pigment epithelium (PubMed:21411718). May play a redundant role in vitamin D biosynthesis. Catalyzes 25-hydroxylation of vitamin D3 that is required for its conversion to a functionally active form (PubMed:15465040)

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