Recombinant Human CYP2D6 protein (His tag) is a Human Fragment protein, in the 236 to 472 aa range, expressed in Escherichia coli, with >90% purity, < 1 EU/µg endotoxin level and suitable for SDS-PAGE.
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A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:19965576, PubMed:20972997). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:18698000, PubMed:21289075). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid (PubMed:10681376). Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
CYP2DL1, CYP2D6, Cytochrome P450 2D6, CYPIID6, Cholesterol 25-hydroxylase, Cytochrome P450-DB1, Debrisoquine 4-hydroxylase
Recombinant Human CYP2D6 protein (His tag) is a Human Fragment protein, in the 236 to 472 aa range, expressed in Escherichia coli, with >90% purity, < 1 EU/µg endotoxin level and suitable for SDS-PAGE.
pH: 8
Constituents: 82.8% Trehalose, 16.38% PBS, 0.17% Sodium-N-Lauroylsarcosinate
nan
A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:19965576, PubMed:20972997). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:18698000, PubMed:21289075). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid (PubMed:10681376). Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Belongs to the cytochrome P450 family.
CYP2D6 also known as cytochrome P450 2D6 is a critical enzyme in the cytochrome P450 superfamily. It possesses a molecular mass of approximately 55 kDa. CYP2D6 is primarily expressed in the liver and to a lesser extent in the brain. As a monooxygenase it catalyzes the oxidation of organic substances including the metabolism of many xenobiotics and drugs. Its activity varies greatly among individuals due to genetic polymorphisms making it an important target for pharmacogenomic studies.
Enzymes related to drug metabolism perform essential roles in the detoxification of foreign chemicals. CYP2D6 is notably part of the microsomal enzyme complex in the liver. It facilitates the transformation of lipophilic compounds into more water-soluble metabolites rendering them easier for the body to excrete. This enzyme affects the bioavailability and efficacy of many medications such as antidepressants antipsychotics and beta-blockers. Its role is integral in the activation of certain prodrugs converting them into their active pharmacological forms.
CYP2D6 functions significantly in drug metabolism and clearance pathways. It takes part in the Phase I metabolism pathway where it initiates the oxidation of drugs setting the stage for further modifications. It interacts closely with other CYP enzymes like CYP3A4 which sometimes share substrates and inhibitors affecting their metabolic activities. CYP2D6's interaction with these pathways emphasizes its involvement in the intricate network of enzyme-mediated drug handling in the body.
Alterations in CYP2D6 activity relate to variations in drug metabolism leading to treatment challenges. For instance poor metabolizers may have increased risks of side effects or therapeutic failures in drugs like codeine which relies on CYP2D6 for activation. Additionally abnormal CYP2D6 activity associates with certain psychiatric disorders where specific drugs require precise metabolic conversion. The interaction between CYP2D6 and other proteins such as CYP3A4 further complicates its role in pharmacotherapy and its impact on individual responses to drugs.
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