CYP2D6
Greater than 95% as determined by SDS-PAGE.
Description
Cytochrome P450 2D6 Human Recombinant (also called liver/kidney microsomal antigen 1) produced in SF9, is a glycosylated, polypeptide chain having a molecular mass of 60 kDa. The LKM1 is purified by proprietary chromatographic techniques.
Product Specs
Product Science Overview
Cytochrome P450 2D6 (CYP2D6) is a crucial enzyme in the cytochrome P450 superfamily, which is involved in the metabolism of a wide range of endogenous and exogenous compounds. The human recombinant form of CYP2D6 is produced using recombinant DNA technology, allowing for the study and application of this enzyme in various research and clinical settings.
The CYP2D6 gene is located on chromosome 22q13.2 and consists of nine exons spanning 4,408 base pairs of DNA . The enzyme encoded by this gene is primarily expressed in the liver and, to a lesser extent, in the central nervous system . The human recombinant form of CYP2D6 is typically produced in insect cells (Sf9) and is a glycosylated polypeptide with a molecular mass of approximately 55,801 Daltons .
CYP2D6 plays a significant role in the metabolism of about 20-25% of commonly prescribed medications, including antidepressants, antipsychotics, analgesics, and anticancer drugs . It is involved in both the activation of prodrugs (e.g., codeine) and the deactivation of active drugs (e.g., amitriptyline) . Unlike many other CYP enzymes, CYP2D6 is non-inducible, meaning its activity is not increased by other drugs .
CYP2D6 is highly polymorphic, with over 170 haplotypes characterized for their impact on metabolism . This genetic variability leads to significant interindividual differences in enzyme activity, which can affect drug efficacy and the risk of adverse effects . The enzyme’s activity can be predicted by genomic tests for functionally important variants, such as single nucleotide variants, splicing variants, and copy number variants . These variants are categorized using star () allele nomenclature, with CYP2D61 being the reference allele .
The polymorphic nature of CYP2D6 has important clinical implications. Individuals can be classified into different metabolizer phenotypes based on their CYP2D6 genotype: poor metabolizers, intermediate metabolizers, extensive metabolizers, and ultra-rapid metabolizers . These phenotypes influence how patients respond to medications metabolized by CYP2D6, impacting both therapeutic outcomes and the risk of adverse drug reactions .
Human recombinant CYP2D6 is used in various research and clinical applications. It is employed in drug metabolism studies to understand the pharmacokinetics of CYP2D6 substrates and to predict drug-drug interactions . Additionally, it is used in the development of pharmacogenomic tests to guide personalized medicine approaches, ensuring that patients receive the most effective and safe medications based on their CYP2D6 genotype .
