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3 results on '"Steroidal scaffolds"'

1. Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties

Author

Claudia Finamore, Giuliana Baronissi, Silvia Marchianò, Francesco Saverio Di Leva, Adriana Carino, Maria Chiara Monti, Vittorio Limongelli, Angela Zampella, Stefano Fiorucci, and Valentina Sepe

Subjects
FXR agonists, bile acid receptors, steroidal scaffolds, medicinal chemistry, Organic chemistry, QD241-441
Abstract

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.

Published
2019
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2. Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties

Author

Giuliana Baronissi, Adriana Carino, Valentina Sepe, Francesco Saverio Di Leva, Silvia Marchianò, Vittorio Limongelli, Claudia Finamore, Maria Chiara Monti, Stefano Fiorucci, Angela Zampella, Finamore, Claudia, Baronissi, Giuliana, Marchianò, Silvia, Di Leva, Francesco Saverio, Carino, Adriana, Chiara Monti, Maria, Limongelli, Vittorio, Zampella, Angela, Fiorucci, Stefano, and Sepe, Valentina

Subjects
FXR agonist, Protein Conformation, Pharmaceutical Science, Receptors, Cytoplasmic and Nuclear, Analytical Chemistry, Receptors, G-Protein-Coupled, Cholane, chemistry.chemical_compound, 0302 clinical medicine, Drug Discovery, Glucose homeostasis, Receptor, 0303 health sciences, Bile acid, Molecular Structure, FXR agonists, steroidal scaffold, Hep G2 Cells, G protein-coupled bile acid receptor, bile acid receptor, Molecular Docking Simulation, Biochemistry, Chemistry (miscellaneous), 030220 oncology & carcinogenesis, Molecular Medicine, Bile acid receptors, Medicinal chemistry, Steroidal scaffolds, bile acid receptors, medicinal chemistry, steroidal scaffolds, medicine.drug_class, Article, lcsh:QD241-441, Bile Acids and Salts, 03 medical and health sciences, Structure-Activity Relationship, lcsh:Organic chemistry, Metabolic Diseases, medicine, Humans, Physical and Theoretical Chemistry, 030304 developmental biology, Organic Chemistry, Lipid Metabolism, In vitro, Glucose, HEK293 Cells, chemistry, Docking (molecular), Cholanes, Farnesoid X receptor
Abstract

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.

Published
2019
Full Text
View/download PDF

3. Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties.

Author

Finamore, Claudia, Baronissi, Giuliana, Marchianò, Silvia, Di Leva, Francesco Saverio, Carino, Adriana, Monti, Maria Chiara, Limongelli, Vittorio, Zampella, Angela, Fiorucci, Stefano, Sepe, Valentina, Oliviero, Giorgia, and Borbone, Nicola

Subjects
*NUCLEAR receptors (Biochemistry), *BILE acids, *APOPTOSIS, *PHARMACOKINETICS, *CRYSTAL structure, *METABOLIC disorders
Abstract

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. [ABSTRACT FROM AUTHOR]

Published
2019
Full Text
View/download PDF

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