What is CYP2D6 pathway?
Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the CYP2D6 gene. This enzyme also metabolizes several endogenous substances, such as hydroxytryptamines, neurosteroids, and both m-tyramine and p-tyramine which CYP2D6 metabolizes into dopamine in the brain and liver.
What is the importance of CYP2D6?
CYP2D6 is responsible for the metabolism of the second highest number of drugs metabolized by P450 enzymes. Substrates for CYP2D6 can be found in Table 3.1. CYP2D6 is a particularly challenging enzyme to understand and study because of its genetic polymorphism.
What is cytochrome P450 pathway?
Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compounds, as well as for hormone synthesis and breakdown.
What metabolizes CYP2D6?
Cytochrome P450 CYP2D6 is the most extensively characterized polymorphic drug-metabolizing enzyme. The CYP2D6 enzyme catalyses the metabolism of a large number of clinically important drugs including antidepressants, neuroleptics, some antiarrhythmics, lipophilic β-adrenoceptor blockers and opioids.
Why is CYP1A2 important?
CYP1A2 has been shown to be important for dosing of several antipsychotics and for assessing both drug efficacy and adverse drug reactions. CYP1A2 is the main CYP isoform involved in clozapine metabolism [16]. This is likely by induction of CYP1A2, causing it to play a larger role in the generation of active drugs.
What is the CYP2D6 enzyme?
The CYP2D6 enzyme catalyses the metabolism of a large number of clinically important drugs including antidepressants, neuroleptics, some antiarrhythmics, lipophilic β-adrenoceptor blockers and opioids.
What is the clinical importance of cytochrome P450?
Both of these characteristics account for their central importance in medicine. Cytochrome P450 enzymes are present in most tissues of the body, and play important roles in hormone synthesis and breakdown (including estrogen and testosterone synthesis and metabolism), cholesterol synthesis, and vitamin D metabolism .
What are Isoenzymes in cytochrome P-450?
The cytochrome P450 isoenzymes are a superfamily of haemoprotein enzymes that catalyse the metabolism of a large number of endogenous and exogenous compounds. Recently, the cytochrome isoenzymes have been shown to be important in the synthesis of steroid hormones and bile acids, the arachidonic acid cascade and in central nervous function.
What does cytochrome P-450 CYP27A1 mean?
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency owing to genetic mutations is detrimental to human health, whereas 50% of activity retention is not and does not affect the whole body cholesterol levels. CYP27A1 is considered a potential therapeutic target in breast cancer and age-related neurodegenerative diseases; however, CYP27A1 inhibition should be ≤50%.