: 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

Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties / Finamore, Claudia; Baronissi, Giuliana; Marchianò, Silvia; Di Leva, Francesco Saverio; Carino, Adriana; Chiara Monti, Maria; Limongelli, Vittorio; Zampella, Angela; Fiorucci, Stefano; Sepe, Valentina. - In: MOLECULES. - ISSN 1420-3049. - 24:6(2019), p. 1043. [10.3390/molecules24061043]

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

Claudia Finamore
Primo
;
Giuliana Baronissi;Francesco Saverio Di Leva;Maria Chiara Monti;Vittorio Limongelli;Angela Zampella;Valentina Sepe
2019

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
2019
Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties / Finamore, Claudia; Baronissi, Giuliana; Marchianò, Silvia; Di Leva, Francesco Saverio; Carino, Adriana; Chiara Monti, Maria; Limongelli, Vittorio; Zampella, Angela; Fiorucci, Stefano; Sepe, Valentina. - In: MOLECULES. - ISSN 1420-3049. - 24:6(2019), p. 1043. [10.3390/molecules24061043]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/749615
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