Results 251 to 260 of about 43,333,653 (285)

Investigation on bile acid receptor regulators. Discovery of cholanoic acid derivatives with dual G-protein coupled bile acid receptor 1 (GPBAR1) antagonistic and farnesoid X receptor (FXR) modulatory activity

Steroids, 2016
Bile acids, the end products of cholesterol metabolism, activate multiple mechanisms through the interaction with membrane G-protein coupled receptors including the bile acid receptor GPBAR1 and nuclear receptors such as the bile acid sensor, farnesoid X receptor (FXR).
Carmen Festa, Valentina Sepe, Angela Zampella   +2 more
exaly   +4 more sources

Stereoselective synthesis, biological evaluation, and modeling of novel bile acid-derived G-protein coupled Bile acid receptor 1 (GP-BAR1, TGR5) agonists

Bioorganic and Medicinal Chemistry, 2015
GP-BAR1 (also known as TGR5), a novel G-protein coupled receptor regulating various non-genomic functions via bile acid signaling, has emerged as a promising target for metabolic disorders, including obesity and type II diabetes. However, given that many bile acids (BAs) are poorly tolerated for systemic therapeutic use, there is significant need to ...
Nagarajan Vaidehi, Xianghui Fu, Wendong Huang   +2 more
exaly   +3 more sources

Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5)

Journal of Medicinal Chemistry, 2018
Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated influence on metabolic, inflammatory, and proliferative processes.
Tao Chen, Nicholas William Reich, Noah Bell, Patricia D. Finn, David Rodriguez, Jill Kohler, Kenji Kozuka, Limin He, Andrew G. Spencer, Dominique Charmot, Marc Navre, Christopher W. Carreras, Samantha Koo-McCoy, Jocelyn Tabora, Jeremy S. Caldwell, Jeffrey W. Jacobs, Jason Gustaf Lewis   +16 more
core   +4 more sources

Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects

European Journal of Medicinal Chemistry, 2020
The G-protein-coupled bile acid receptor TGR5 agonists were widely developed in type 2 diabetes and gastrointestinal disorders, but were also full of challenges, due to the systemic on-targeted side effects, especially the gallbladder-filling effects.
Fanghui, Han, Mengmeng, Ning, Hua, Cao, Yangliang, Ye, Ying, Feng, Ying, Leng, Jianhua, Shen   +6 more
openaire   +2 more sources

Modification on Ursodeoxycholic Acid (UDCA) Scaffold. Discovery of Bile Acid Derivatives As Selective Agonists of Cell-Surface G-Protein Coupled Bile Acid Receptor 1 (GP-BAR1)

Journal of Medicinal Chemistry, 2014
Bile acids are signaling molecules interacting with the nuclear receptor FXR and the G-protein coupled receptor 1 (GP-BAR1/TGR5). GP-BAR1 is a promising pharmacological target for the treatment of steatohepatitis, type 2 diabetes, and obesity. Endogenous bile acids and currently available semisynthetic bile acids are poorly selective toward GP-BAR1 and
SEPE, VALENTINA, Barbara Renga, FESTA, CARMEN, Claudio D’Amore, MASULLO, DARIO, Sabrina Cipriani, Di Leva, Francesco Saverio, Maria Chiara Monti, NOVELLINO, ETTORE, LIMONGELLI, VITTORIO, ZAMPELLA, ANGELA, Stefano Fiorucci   +11 more
openaire   +5 more sources

Exploitation of Cholane Scaffold for the Discovery of Potent and Selective Farnesoid X Receptor (FXR) and G-Protein Coupled Bile Acid Receptor 1 (GP-BAR1) Ligands

Journal of Medicinal Chemistry, 2014
Nuclear and G-protein coupled receptors are considered major targets for drug discovery. FXR and GP-BAR1, two bile acid-activated receptors, have gained increasing consideration as druggable receptors. Because endogenous bile acids often target both receptor families, the development of selective ligands has been proven difficult, exposing patients to ...
Carmen Festa, Barbara Renga, Claudio D’Amore, Valentina Sepe, Claudia Finamore, Simona De Marino, Adriana Carino, Sabrina Cipriani, MONTI, Maria Chiara, Angela Zampella, Stefano Fiorucci   +10 more
openaire   +6 more sources

Deoxyschizandrin ameliorates obesity and non‐alcoholic fatty liver disease: Involvement of dual Farnesyl X receptor/G protein‐coupled bile acid receptor 1 activation and leptin sensitization

Phytotherapy Research, 2023
AbstractNatural dual farnesyl X receptor (FXR)/G protein‐coupled bile acid receptor 1 (TGR5) activators have received little attention in the management of metabolic diseases. Deoxyschizandrin (DS), a natural lignan, occurs in S. chinensis fruit and has potent hepatoprotective effects, whereas its protective roles and mechanisms against obesity and non‐
Ming Gu, Yaru Feng, Yujun Chen, Shengjie Fan, Cheng Huang   +4 more
openaire   +2 more sources

G Protein–Coupled Bile Acid Receptor 1 Stimulation Mediates Arterial Vasodilation through a KCa1.1 (BKCa)–Dependent Mechanism

The Journal of Pharmacology and Experimental Therapeutics, 2014
Bile acids (BAs) and BA receptors, including G protein-coupled bile acid receptor 1 (GPBAR1), represent novel targets for the treatment of metabolic and inflammatory disorders. However, BAs elicit myriad effects on cardiovascular function, although this has not been specifically ascribed to GPBAR1. This study was designed to test whether stimulation of
Ryan M, Fryer, Khing Jow, Ng, Suzanne G, Nodop Mazurek, Lori, Patnaude, Donna J, Skow, Akalushi, Muthukumarana, Kyle E, Gilpin, Roger M, Dinallo, Daniel, Kuzmich, John, Lord, Sulagna, Sanyal, Hui, Yu, Christian, Harcken, Matthew A, Cerny, Matthew C, Cerny, Eugene R, Hickey, Louise K, Modis   +16 more
openaire   +2 more sources

G-Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5) Agonists Reduce the Production of Proinflammatory Cytokines and Stabilize the Alternative Macrophage Phenotype

Journal of Medicinal Chemistry, 2014
GPBAR1 (also known as TGR5) is a G-protein-coupled receptor (GPCR) that triggers intracellular signals upon ligation by various bile acids. The receptor has been studied mainly for its function in energy expenditure and glucose homeostasis, and there is little information on the role of GPBAR1 in the context of inflammation.
Klemens, Högenauer, Luca, Arista, Niko, Schmiedeberg, Gudrun, Werner, Herbert, Jaksche, Rochdi, Bouhelal, Deborah G, Nguyen, B Ganesh, Bhat, Layla, Raad, Celine, Rauld, José M, Carballido   +10 more
openaire   +2 more sources

Discovery of amine bile acid derivatives as selective agonists of cell-surface G-protein coupled bile acid receptor 1

2015
Nuclear and G-protein coupled receptors are considered major targets for drug discovery. FXR and GP-BAR1, two bile acid-activated receptors, have gained increasing consideration as druggable receptors, providing new opportunities for the treatment of enterohepatic and metabolic disorders.
Di Leva, Francesco Saverio, Renga, Barbara, SEPE, VALENTINA, NOVELLINO, ETTORE, Fiorucci, Stefano, ZAMPELLA, ANGELA, LIMONGELLI, VITTORIO, FESTA, CARMEN   +7 more
openaire   +1 more source