ReviewCurrent drug metabolism2008
Molecular characterization of CYP2B6 substrates.
Review in Current drug metabolism, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 46 citations in OpenAlex.
- Applicability domain-expansion studies for machine learning models reveal new inhibitors of CYP2B6.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Analysis of six CYP450 genetic variants regarding the response to cannabidiol combined with anticonvulsant medication in mexican patients with drug-resistant epilepsy.Frontiers in pharmacology · 2025Article
- Natural Products Inhibition of Cytochrome P450 2B6 Activity and Methadone Metabolism.Drug metabolism and disposition: the biological fate of chemicals · 2024Article
- Flavonoids from Pterogyne nitens as Zika virus NS2B-NS3 protease inhibitors.Bioorganic chemistry · 2021Article
- Period 2 Regulates CYP2B10 Expression and Activity in Mouse Liver.Frontiers in pharmacology · 2021Article
- CYP2B6 Functional Variability in Drug Metabolism and Exposure Across Populations-Implication for Drug Safety, Dosing, and Individualized Therapy.Frontiers in genetics · 2021Review
- Efavirenz Metabolism: Influence of Polymorphic CYP2B6 Variants and Stereochemistry.Drug metabolism and disposition: the biological fate of chemicals · 2019Review
- Halogen Substitution Influences Ketamine Metabolism by Cytochrome P450 2B6: In Vitro and Computational Approaches.Molecular pharmaceutics · 2019Article
- Use of Ca-alginate immobilized Pseudomonas aeruginosa for repeated batch and continuous degradation of Endosulfan.3 Biotech · 2016Article
- Article
- Effect of Brain CYP2B Inhibition on Brain Nicotine Levels and Nicotine Self-Administration.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2015Article
- Monocrotophos induces the expression and activity of xenobiotic metabolizing enzymes in pre-sensitized cultured human brain cells.PloS one · 2014Article
- Impact of nicotine metabolism on nicotine's pharmacological effects and behavioral responses: insights from a Cyp2a(4/5)bgs-null mouse.The Journal of pharmacology and experimental therapeutics · 2013Article
- Structural and thermodynamic basis of (+)-α-pinene binding to human cytochrome P450 2B6.Journal of the American Chemical Society · 2013Article
- Analysis of clinically relevant substrates of CYP2B6 enzyme by computational methods.Journal of molecular modeling · 2011Article
- Drug metabolism within the brain changes drug response: selective manipulation of brain CYP2B alters propofol effects.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2011Article
- Crystal structure of a cytochrome P450 2B6 genetic variant in complex with the inhibitor 4-(4-chlorophenyl)imidazole at 2.0-A resolution.Molecular pharmacology · 2010Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
CYP2B6 has not been as fully characterized at the molecular level as other members of the human cytochrome P450 family. As more widely used in vitro probes for characterizing the involvement of this enzyme in the metabolism of xenobiotics have become available, the number of molecules identified as CYP2B6 substrates has increased. In this study we have analyzed the available kinetic data generated by multiple laboratories with human recombinant expressed CYP2B6 and along with calculated molecular properties derived from the ChemSpider database, we have determined the molecular features that appear to be important for CYP2B6 substrates. In addition we have applied 2D and 3D QSAR methods to generate predictive pharmacophore and 2D models. For 28 molecules with K(m) data, the molecular weight (mean +/- SD) is 253.78+/-74.03, ACD/logP is 2.68+/-1.51, LogD(pH 5.5) is 1.51+/-1.43, LogD(pH 7.4) is 2.02+/-1.25, hydrogen bond donor (HBD) count is 0.57 +/-0.57, hydrogen bond acceptor (HBA) count is 2.57+/-1.37, rotatable bonds is 3.50+/-2.71 and total polar surface area (TPSA) is 27.63+/-19.42. A second set of 15 molecules without K(m) data possessed similar mean molecular property values. These properties are comparable to those of a set of 21 molecules used in a previous pharmacophore modeling study (Ekins et al., J Pharmacol Exp Ther 288 (1), 21-29, 1999). Only the LogD and HBD values were statistically significantly different between these different datasets. We have shown that CYP2B6 substrates are generally small hydrophobic molecules that are frequently central nervous system active, which may be important for drug discovery research.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.