ArticleEuropean journal of drug metabolism and pharmacokinetics2016
Effect of 22 Novel Cytochrome P450 2D6 (CYP2D6) Variants Found in the Chinese Population on Hemangeol Metabolism In Vitro.
Article in European journal of drug metabolism and pharmacokinetics, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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2 citing papers in PubMed, 7 citations in OpenAlex.
- Functional characterization of wild-type and 24 CYP2D6 allelic variants on gefitinib metabolism in vitro.Drug design, development and therapy · 2017Article
- Metabolic enzyme gene polymorphisms predict the effects of antioxidant treatment on idiopathic male infertility.Asian journal of andrologyArticle
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
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Abstract
BACKGROUND AND
objectivesHemangeol, approved for the treatment of proliferative infantile hemangiomas requiring systemic therapy, is metabolized by cytochrome P450 2D6 (CYP2D6), which is a highly polymorphic enzyme that metabolizes a large number of drugs. More than 100 CYP2D6 allelic variants have been reported so far, including 22 novel variants that discovered in our lab in the Chinese population. Our study aimed to probe the enzymatic activity of these variants toward hemangeol in vitro with recombinant microsomes that expressed in sf21 insect cells using a baculovirus-mediated expression system.
methodsThe wild-type CYP2D6.1 and other variants (CYP2D6.2, CYP2D6.10 and 22 novel CYP2D6 variants) were incubated with 1-200 μM hemangeol for 50 min at 37 °C. Then the products were extracted, and signal detection was performed by high-performance liquid chromatography with fluorescence detector.
resultsAll of the variants exhibited changed apparent Michaelis-Menten constant (Km) or maximum velocity of the reaction (V
conclusionsThe comprehensive in vitro assessment of CYP2D6 variants provides significant insights into allele-specific activity towards hemangeol in vivo.
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