ArticleThe Journal of biological chemistry2012
Crystal structure of human cytochrome P450 2D6 with prinomastat bound.
Article in The Journal of biological chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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Who cites it
45 citing papers in PubMed.
- Nicotiana glauca leaf extract exhibits synergistic antioxidant and anticancer activities revealed by phytochemical profiling and molecular docking.Scientific reports · 2026Article
- Metabolic Stability of Fluorinated Small Molecules: A Physical Organic Chemistry Perspective.Journal of medicinal chemistry · 2026Review
- Allosteric modulation of cytochrome P450 enzymes by the NADPH cytochrome P450 reductase FMN-containing domain.The Journal of biological chemistry · 2023Article
- Generation of new inhibitors of selected cytochrome P450 subtypes-Computational and structural biotechnology journal · 2022Article
- Differential Interactions of Selected Phytocannabinoids with Human CYP2D6 Polymorphisms.Biochemistry · 2021Article
- Beyond generative models: superfast traversal, optimization, novelty, exploration and discovery (STONED) algorithm for molecules using SELFIES.Chemical science · 2021Article
- Tryptophan-75 Is a Low-Energy Channel-Gating Residue that Facilitates Substrate Egress/Access in Cytochrome P450 2D6.Drug metabolism and disposition: the biological fate of chemicals · 2021Article
- Domain-Swap Dimerization ofMolecular pharmacology · 2020Article
- CYP2J2 Molecular Recognition: A New Axis for Therapeutic Design.Pharmacology & therapeutics · 2020Review
- A Review of the Important Role ofGenes · 2020Review
- A Modified Arrhenius Approach to Thermodynamically Study Regioselectivity in Cytochrome P450-Catalyzed Substrate Conversion.Chembiochem : a European journal of chemical biology · 2020Article
- Analysis of the Deleterious Single-Nucleotide Polymorphisms Associated With Antidepressant Efficacy in Major Depressive Disorder.Frontiers in psychiatry · 2020Article
- Pharmacokinetics, excretion and metabolites analysis of DL0410, a dual‑acting cholinesterase inhibitor and histamine‑3 receptor antagonist.Molecular medicine reports · 2019Article
- Functional and structural characterisation of common cytochrome P450 2D6 allelic variants-roles of Pro34 and Thr107 in catalysis and inhibition.Naunyn-Schmiedeberg's archives of pharmacology · 2019Article
- Conformational selection dominates binding of steroids to human cytochrome P450 17A1.The Journal of biological chemistry · 2019Article
- Rolapitant Is a Reversible Inhibitor of CYP2D6.Drug metabolism and disposition: the biological fate of chemicals · 2019Article
- Coumarins and P450s, Studies Reported to-Date.Molecules (Basel, Switzerland) · 2019Review
- Dynamic Effects of CYP2D6 Genetic Variants in a Set of Poor Metaboliser Patients with Infiltrating Ductal Cancer Under Treatment with Tamoxifen.Scientific reports · 2019Article
- Kinetic mechanism of time-dependent inhibition of CYP2D6 by 3,4-methylenedioxymethamphetamine (MDMA): Functional heterogeneity of the enzyme and the reversibility of its inactivation.Biochemical pharmacology · 2018Article
- Biotransformation, Using Recombinant CYP450-Expressing Baker's Yeast Cells, Identifies a Novel CYP2D6.10ACS omega · 2018Article
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5 authors.
Funding
Abstract
Human cytochrome P450 2D6 contributes to the metabolism of >15% of drugs used in clinical practice. This study determined the structure of P450 2D6 complexed with a substrate and potent inhibitor, prinomastat, to 2.85 Å resolution by x-ray crystallography. Prinomastat binding is well defined by electron density maps with its pyridyl nitrogen bound to the heme iron. The structure of ligand-bound P450 2D6 differs significantly from the ligand-free structure reported for the P450 2D6 Met-374 variant (Protein Data Bank code 2F9Q). Superposition of the structures reveals significant differences for β sheet 1, helices A, F, F', G", G, and H as well as the helix B-C loop. The structure of the ligand complex exhibits a closed active site cavity that conforms closely to the shape of prinomastat. The closure of the open cavity seen for the 2F9Q structure reflects a change in the direction and pitch of helix F and introduction of a turn at Gly-218, which is followed by a well defined helix F' that was not observed in the 2F9Q structure. These differences reflect considerable structural flexibility that is likely to contribute to the catalytic versatility of P450 2D6, and this new structure provides an alternative model for in silico studies of substrate interactions with P450 2D6.
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