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Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the CYP2D6 gene. CYP2D6 is primarily expressed in the liver . It is also highly expressed in areas of the central nervous system , including the substantia nigra .
For example, CYP2E1 is the gene that encodes the enzyme CYP2E1—one of the enzymes involved in paracetamol (acetaminophen) metabolism. The CYP nomenclature is the official naming convention, although occasionally CYP450 or CYP 450 is used synonymously. These names should never be used as according to the nomenclature convention (as they denote ...
The fluctuation in the amount of CYP450 enzymes (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4, and CYP3A5) in phase 1 (detoxification) can have varying effects on individuals, as genetic expression varies from person to person. This variation is due to the enzyme's genetic polymorphism, which leads to variability in its function and expression.
The cytochrome P450 enzyme family is responsible for metabolism of 70-80% of all medications used clinically. [11] CYP3A4 , CYP2C9 , CYP2C19 , and CYP2D6 are major CYP enzymes involved in drug metabolism and are all known to be highly polymorphic. [ 11 ]
1576 n/a Ensembl ENSG00000160868 n/a UniProt P08684 n/a RefSeq (mRNA) NM_001202855 NM_001202856 NM_001202857 NM_017460 n/a RefSeq (protein) NP_001189784 NP_059488 n/a Location (UCSC) Chr 7: 99.76 – 99.78 Mb n/a PubMed search n/a Wikidata View/Edit Human Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97) is an important enzyme in the body, mainly found in the liver and in the intestine ...
Prior to the 1960s, the oxidation of xenotoxic materials was thought to be completely accomplished by CYP450.However, in the early 1970s, Dr. Daniel Ziegler from the University of Texas at Austin discovered a hepatic flavoprotein isolated from pig liver that was found to oxidize a vast array of various amines to their corresponding nitro state.
Lumateperone is a substrate for numerous metabolic enzymes, including various glucuronosyltransferase (UGT) isoforms (UGT1A1, 1A4, and 2B15), aldo-keto reductase (AKR) isoforms (AKR1C1, 1B10, and 1C4), and cytochrome P450 (CYP) enzymes (CYP3A4, 2C8, and 1A2). [2] Lumateperone does not cause appreciable inhibition of any common CYP450 enzymes.
These enzymes oxidize N-methyl groups, which occur in histones, in lysine derivatives, and in some forms of DNA. [4] R 2 N-CH 3 + O → R 2 N-H + CH 2 O. One family of such oxidative enzymes is the cytochrome P450. [5] Alpha-ketoglutarate-dependent hydroxylases are also active for demethylation of DNA, operating by a similar stoichiometry. [6]