Results 11 to 20 of about 42,926,125 (284)

Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1

Journal of Medicinal Chemistry, 2021
G-protein-coupled receptors (GPCRs) are the molecular target of 40% of marketed drugs and the most investigated structures to develop novel therapeutics. Different members of the GPCRs superfamily can modulate the same cellular process acting on diverse pathways, thus representing an attractive opportunity to achieve multitarget drugs with synergic ...
Fiorillo B., Sepe V., Conflitti P., Roselli R., Biagioli M., Marchiano S., De Luca P., Baronissi G., Rapacciuolo P., Cassiano C., Catalanotti B., Zampella A., Limongelli V., Fiorucci S.   +13 more
openaire   +6 more sources

G protein-coupled bile acid receptor 1 activation attenuates endothelin-1-induced rat cardiomyocyte hypertrophy by inhibiting CaN/NAFT3 pathway

Di-san junyi daxue xuebao, 2019
Objective To investigate the inhibitory effect of G protein-coupled bile acid receptor 1 (TGR5) on endothelin-1 (ET-1)-induced cardiomyocyte hypertrophy and explore the mechanism.
CHEN Dexiu, LI Jiafu, FENG Jian
doaj   +2 more sources

Combinatorial targeting of G‐protein‐coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug‐induced liver injury

Hepatology, 2022
Background and Aim: Drug‐induced liver injury (DILI) is a common disorder that involves both direct liver cell toxicity and immune activation. The bile acid receptor, G‐protein‐coupled bile acid receptor 1 (GPBAR1; Takeda G‐protein‐coupled receptor 5 [TGR5]), and cysteinyl leukotriene receptor (CYSLTR) 1 are G‐protein‐coupled ...
Biagioli M., Marchiano S., di Giorgio C., Roselli R., Bordoni M., Bellini R., Fiorillo B., Sepe Valentina, Catalanotti B., Cassiano C., Monti M. C., Distrutti E., Zampella Angela, Fiorucci S.   +13 more
openaire   +5 more sources

Research Progress on the Mechanism and Targeted Intervention of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1)-Mediated "Inflammation-Apoptosis-Metabolism-Microcirculation" Regulatory Network in Hepatitis B-Associated Liver Failure. [PDF]

Drug Des Devel Ther
Cui C, Sun Y, Zhang K, Shi J, Wang K, Gao S.   +5 more
europepmc   +2 more sources

Bile Acids Trigger GLP-1 Release Predominantly by Accessing Basolaterally Located G Protein–Coupled Bile Acid Receptors [PDF]

Endocrinology, 2015
Bile acids are well-recognized stimuli of glucagon-like peptide-1 (GLP-1) secretion. This action has been attributed to activation of the G protein–coupled bile acid receptor GPBAR1 (TGR5), although other potential bile acid sensors include the nuclear farnesoid receptor and the apical sodium-coupled bile acid transporter ASBT.
Brighton, Cheryl A., Rievaj, Juraj, Kuhre, Rune E., Glass, Leslie L., Schoonjans, Kristina, Holst, Jens J., Gribble, Fiona M., Reimann, Frank   +7 more
openaire   +5 more sources

Bile acids alter male fertility through G-protein-coupled bile acid receptor 1 signaling pathways in mice [PDF]

Hepatology, 2014
Bile acids (BAs) are signaling molecules that are involved in many physiological functions, such as glucose and energy metabolism. These effects are mediated through activation of the nuclear and membrane receptors, farnesoid X receptor (FXR-α) and TGR5 (G-protein-coupled bile acid ...
Baptissart, Marine, Vega, Aurélie, Martinot, Emmanuelle, Pommier, Aurélien J., Houten, Sander M., Marceau, Geoffroy, Haze, Angélique, Baron, Silvère, Schoonjans, Kristina, Lobaccaro, Jean-Marc A., Volle, David H.   +10 more
openaire   +6 more sources

Bile acid activated receptors: Integrating immune and metabolic regulation in non-alcoholic fatty liver disease

Liver Research, 2021
Bile acids are a family of atypical steroids generated at the interface of liver-intestinal microbiota acting on a ubiquitously expressed family of membrane and nuclear receptors known as bile acid activated receptors.
Michele Biagioli, Stefano Fiorucci
doaj   +1 more source

(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells

Frontiers in Pharmacology, 2021
Bile acids (BAs) are key signaling steroidal molecules that regulate glucose, lipid, and energy homeostasis via interactions with the farnesoid X receptor (FXR) and G-protein bile acid receptor 1 (GPBAR1).
Alzbeta Stefela, Miroslav Kaspar, Miroslav Kaspar, Martin Drastik, Thales Kronenberger, Thales Kronenberger, Stanislav Micuda, Martin Dracinsky, Blanka Klepetarova, Eva Kudova, Petr Pavek   +10 more
doaj   +1 more source

Targeted disruption of G protein-coupled bile acid receptor 1 (Gpbar1/M-Bar) in mice [PDF]

Journal of Endocrinology, 2006
G protein-coupled bile acid receptor 1 ( Gpbar1/M-Bar ) is a novel G protein-coupled receptor for bile acid. Tissue distribution and cell-type specificity of Gpbar1 mRNA suggest a potential role for the receptor in the endocrine system; however, the precise physiological role of Gpbar1 still ...
Takaharu, Maruyama, Kenichi, Tanaka, Jun, Suzuki, Hiroyuki, Miyoshi, Naomoto, Harada, Takao, Nakamura, Yasuhisa, Miyamoto, Akio, Kanatani, Yoshitaka, Tamai   +8 more
openaire   +2 more sources

Glycoursodeoxycholic acid regulates bile acids level and alters gut microbiota and glycolipid metabolism to attenuate diabetes

Gut Microbes, 2023
Accumulating evidence suggests that the bile acid regulates type 2 diabetes mellitus (T2DM) through gut microbiota-host interactions. However, the mechanisms underlying such interactions have been unclear.
Bingting Chen, Yu Bai, Fenglian Tong, Junlin Yan, Rui Zhang, Yewei Zhong, Huiwen Tan, Xiaoli Ma   +7 more
doaj   +1 more source