ArticleMolecules (Basel, Switzerland)2019
Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties.
Claudia Finamore, Giuliana Baronissi, Silvia Marchianò, Francesco Saverio Di Leva, Adriana Carino, Maria Chiara Monti, Vittorio Limongelli, Angela Zampella, Stefano Fiorucci, Valentina Sepe
Abstract read
In one paragraphArticle in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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5 · Who and what moneyAuthors and funding
10 authors.
Claudia FinamoreDepartment of Pharmacy, University of Naples "Federico II", via D. Montesano 49, 80131 Naples, Italy. claudia.finamore@unina.it.
Giuliana BaronissiDepartment of Pharmacy, University of Naples "Federico II", via D. Montesano 49, 80131 Naples, Italy. giuliana.baronissi@unina.it.
Silvia MarchianòDepartment of Surgery and Biomedical Sciences, Nuova Facoltà di Medicina, Piazza Lucio Severi, 1 - 06132 Perugia, Italy. silvia4as@hotmail.it.
Francesco Saverio Di LevaDepartment of Pharmacy, University of Naples "Federico II", via D. Montesano 49, 80131 Naples, Italy. francesco.dileva@unina.it.ORCID 0000-0002-2294-0656 Adriana CarinoDepartment of Surgery and Biomedical Sciences, Nuova Facoltà di Medicina, Piazza Lucio Severi, 1 - 06132 Perugia, Italy. adriana.carino@hotmail.it.ORCID 0000-0003-2341-9528 Maria Chiara MontiDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, Salerno, Italy. mcmonti@unisa.it.ORCID 0000-0002-1337-2909 Vittorio LimongelliDepartment of Pharmacy, University of Naples "Federico II", via D. Montesano 49, 80131 Naples, Italy. vittoriolimongelli@gmail.com.
Angela ZampellaDepartment of Pharmacy, University of Naples "Federico II", via D. Montesano 49, 80131 Naples, Italy. azampell@unina.it.
Stefano FiorucciDepartment of Surgery and Biomedical Sciences, Nuova Facoltà di Medicina, Piazza Lucio Severi, 1 - 06132 Perugia, Italy. stefano.fiorucci@unipg.it.ORCID 0000-0003-3816-4222 Valentina SepeDepartment of Pharmacy, University of Naples "Federico II", via D. Montesano 49, 80131 Naples, Italy. valentina.sepe@unina.it.ORCID 0000-0002-0169-4441 Funding
MIUR-ITALY 2015MSCKCE_003Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung 200021_163281University of Naples Federico II "Finanziamento della Ricerca in Ateneo" DR/2016/341, February 2016
6 · The paper itselfAbstract
As a cellular bile acid sensor, farnesoid X receptor (FXR) and the membrane G-coupled receptor (GPBAR1) participate in maintaining bile acid, lipid, and glucose homeostasis. To date, several selective and dual agonists have been developed as promising pharmacological approach to metabolic disorders, with most of them possessing an acidic conjugable function that might compromise their pharmacokinetic distribution. Here, guided by docking calculations, nonacidic 6-ethyl cholane derivatives have been prepared. In vitro pharmacological characterization resulted in the identification of bile acid receptor modulators with improved pharmacokinetic properties.
Indexed as
Bile Acids and SaltsCholanesGlucoseHEK293 CellsHep G2 CellsHumansLipid MetabolismMetabolic DiseasesMolecular Docking SimulationMolecular StructureProtein ConformationReceptor, Farnesoid X-ActivatedReceptors, Cytoplasmic and NuclearReceptors, G-Protein-CoupledStructure-Activity RelationshipBile Acids and SaltsCholanesGlucoseGPBAR1 protein, humanReceptor, Farnesoid X-ActivatedReceptors, Cytoplasmic and NuclearReceptors, G-Protein-Coupledbile acid receptorsFXR agonistsmedicinal chemistrysteroidal scaffolds
Identifiers
PMID30884797
PMCPMC6470523
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