ArticleMolecular pharmaceutics2018
Molecular Docking-Based Design and Development of a Highly Selective Probe Substrate for UDP-glucuronosyltransferase 1A10.
Article in Molecular pharmaceutics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 21 citations in OpenAlex.
- Production of Anti-melanogenic Glucosides via Molecular Docking-guided Biotransformation of p-hydroxyphenethyl anisate.Applied biochemistry and biotechnology · 2026Article
- Rational design of a novel specific fluorescent substrate for monitoring hUGT1A4 activity and its application in identification of selective inhibitors.Journal of pharmaceutical analysis · 2026Article
- Umbelliferon: a review of its pharmacology, toxicity and pharmacokinetics.Inflammopharmacology · 2023Review
- Western Diet Decreases Hepatic Drug Metabolism in Male LDLrJournal of nutrition and metabolism · 2023Article
- Article
- Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives.Acta pharmaceutica Sinica. B · 2022Review
- Predicting reactivity to drug metabolism: beyond P450s-modelling FMOs and UGTs.Journal of computer-aided molecular design · 2021Article
- Article
- Coumarin-Based Profluorescent and Fluorescent Substrates for Determining Xenobiotic-Metabolizing Enzyme Activities In Vitro.International journal of molecular sciences · 2020Review
- A Practical Perspective: The Effect of Ligand Conformers on the Negative Image-Based Screening.International journal of molecular sciences · 2019Article
- Recent progress and challenges in screening and characterization of UGT1A1 inhibitors.Acta pharmaceutica Sinica. B · 2019Review
- Discovery of Retinoic Acid-Related Orphan Receptor γt Inverse Agonists via Docking and Negative Image-Based Screening.ACS omega · 2018Article
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Intestinal and hepatic glucuronidation by the UDP-glucuronosyltransferases (UGTs) greatly affect the bioavailability of phenolic compounds. UGT1A10 catalyzes glucuronidation reactions in the intestine, but not in the liver. Here, our aim was to develop selective, fluorescent substrates to easily elucidate UGT1A10 function. To this end, homology models were constructed and used to design new substrates, and subsequently, six novel C3-substituted (4-fluorophenyl, 4-hydroxyphenyl, 4-methoxyphenyl, 4-(dimethylamino)phenyl, 4-methylphenyl, or triazole) 7-hydroxycoumarin derivatives were synthesized from inexpensive starting materials. All tested compounds could be glucuronidated to nonfluorescent glucuronides by UGT1A10, four of them highly selectively by this enzyme. A new UGT1A10 mutant, 1A10-H210M, was prepared on the basis of the newly constructed model. Glucuronidation kinetics of the new compounds, in both wild-type and mutant UGT1A10 enzymes, revealed variable effects of the mutation. All six new C3-substituted 7-hydroxycoumarins were glucuronidated faster by human intestine than by liver microsomes, supporting the results obtained with recombinant UGTs. The most selective 4-(dimethylamino)phenyl and triazole C3-substituted 7-hydroxycoumarins could be very useful substrates in studying the function and expression of the human UGT1A10.
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