ArticleJournal of medicinal chemistry2013
Pyranoflavones: a group of small-molecule probes for exploring the active site cavities of cytochrome P450 enzymes 1A1, 1A2, and 1B1.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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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.
The trial behind it
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
16 citing papers in PubMed, 42 citations in OpenAlex.
- 16R-HETE and 16S-HETE alter human cytochrome P450 1B1 enzyme activity probably through an allosteric mechanism.Molecular and cellular biochemistry · 2024Article
- Design, Synthesis, and Biological Studies of Flavone-Based Esters and Acids as Potential P450 2A6 Inhibitors.Chemical research in toxicology · 2023Article
- Discovery of Flavone Derivatives Containing Carboxamide Fragments as Novel Antiviral Agents.Molecules (Basel, Switzerland) · 2023Article
- Novel Synthetic Analogues of 19(S/R)-Hydroxyeicosatetraenoic Acid Exhibit Noncompetitive Inhibitory Effect on the Activity of Cytochrome P450 1A1 and 1B1.European journal of drug metabolism and pharmacokinetics · 2021Article
- Identification of CYP 2A6 inhibitors in an effort to mitigate the harmful effects of the phytochemical nicotine.Journal of cancer metastasis and treatment · 2021Article
- Human Cytochrome P450 1A1 Adapts Active Site for Atypical Nonplanar Substrate.Drug metabolism and disposition: the biological fate of chemicals · 2020Article
- Interspecies Variation in NCMNMolecules (Basel, Switzerland) · 2019Article
- Coumarins and P450s, Studies Reported to-Date.Molecules (Basel, Switzerland) · 2019Review
- Structure-Based Drug Design for Cytochrome P450 Family 1 Inhibitors.Bioinorganic chemistry and applications · 2018Review
- Potential role of CYP1B1 in the development and treatment of metabolic diseases.Pharmacology & therapeutics · 2017Review
- Review of Ligand Specificity Factors for CYP1A Subfamily Enzymes from Molecular Modeling Studies Reported to-Date.Molecules (Basel, Switzerland) · 2017Review
- Ortho-Methylarylamines as Time-Dependent Inhibitors of Cytochrome P450 1A1 Enzyme.Drug metabolism letters · 2017Article
- Combinatorial Synthesis of Structurally Diverse Triazole-Bridged Flavonoid Dimers and Trimers.Molecules (Basel, Switzerland) · 2016Article
- A Ligand-Based Drug Design. Discovery of 4-Trifluoromethyl-7,8-pyranocoumarin as a Selective Inhibitor of Human Cytochrome P450 1A2.Journal of medicinal chemistry · 2015Article
- Ethynylflavones, highly potent, and selective inhibitors of cytochrome P450 1A1.Chemical research in toxicology · 2014Article
- Cytochrome P450 family 1 inhibitors and structure-activity relationships.Molecules (Basel, Switzerland) · 2013Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
Abstract
Selective inhibition of P450 enzymes is the key to block the conversion of environmental procarcinogens to their carcinogenic metabolites in both animals and humans. To discover highly potent and selective inhibitors of P450s 1A1, 1A2, and 1B1, as well as to investigate active site cavities of these enzymes, 14 novel flavone derivatives were prepared as chemical probes. Fluorimetric enzyme inhibition assays were used to determine the inhibitory activities of these probes toward P450s 1A1, 1A2, 1B1, 2A6, and 2B1. A highly selective P450 1B1 inhibitor 5-hydroxy-4'-propargyloxyflavone (5H4'FPE) was discovered. Some tested compounds also showed selectivity between P450s 1A1 and 1A2. α-Naphthoflavone-like and 5-hydroxyflavone derivatives preferentially inhibited P450 1A2, while β-naphthoflavone-like flavone derivatives showed selective inhibition of P450 1A1. On the basis of structural analysis, the active site cavity models of P450 enzymes 1A1 and 1A2 were generated, demonstrating a planar long strip cavity and a planar triangular cavity, respectively.
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What OpenQuestion holds
Registered trials
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.