A GPBAR1 (TGR5) small molecule agonist shows specific inhibitory effects on myeloid cell activation in vitro and reduces experimental autoimmune encephalitis (EAE) in vivo. [PDF]
PLoS ONE, 2014 GPBAR1 is a G protein-coupled receptor that is activated by certain bile acids and plays an important role in the regulation of bile acid synthesis, lipid metabolism, and energy homeostasis.
Nuruddeen D Lewis +16 more
doaj +2 more sources
Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1. [PDF]
PLoS ONE, 2015 GPBAR1 is a bile acids activated receptor expressed in entero-hepatic tissues. In the liver expression of GPBAR1 is restricted to sinusoidal and Kuppfer cells.
Barbara Renga +5 more
doaj +2 more sources
GPBAR1 is associated with asynchronous bone metastasis and poor prognosis of hepatocellular carcinoma [PDF]
Frontiers in Oncology, 2023 BackgroundHepatocellular carcinoma (HCC) is the second leading cause of cancer-related death in China. Asynchronous metastasis is the main reason for HCC recurrence, but the current assessment of HCC metastasis and prognosis is far from clinically ...
Nan Chen +5 more
doaj +2 more sources
Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling. [PDF]
PLoS ONE, 2015 Background & aimsIn cholestatic syndromes, body accumulation of bile acids is thought to cause itching. However, the mechanisms supporting this effect remain elusive.
Sabrina Cipriani +9 more
doaj +2 more sources
Cellular and Molecular Gastroenterology and Hepatology, 2019 Background & Aims: GPBAR1, also known as TGR5, is a G protein–coupled receptor activated by bile acids. Hepatic innate immune cells are involved in the immunopathogenesis of human liver diseases and in several murine hepatitis models.
Michele Biagioli +11 more
doaj +2 more sources
Liver GPBAR1 Associates With Immune Dysfunction in Primary Sclerosing Cholangitis and Its Activation Attenuates Cholestasis in Abcb4−/− Mice [PDF]
Liver InternationalBackground and Aims: Primary sclerosing cholangitis (PSC) is a chronic cholestatic liver disease characterised by progressive biliary inflammation and fibrosis, leading to liver cirrhosis and cholangiocarcinoma.
Cristina Di Giorgio +2 more
exaly +4 more sources
Sodium butyrate regulates macrophage polarization by TGR5/β-arrestin2 in vitro [PDF]
Molecular MedicineBackground Macrophages play an important role in the pathogenesis of ulcerative colitis (UC). We will explore the effects of sodium butyrate (SB) on macrophage function.
Miao Liu +5 more
doaj +2 more sources
Conjugated Lithocholic Acid Activates Hepatic TGR5 to Promote Lipotoxicity and MASLD‐MASH Transition by Disrupting Carnitine Biosynthesis [PDF]
Advanced ScienceConjugated lithocholic acid (LCA) plays a critical role in the development of metabolic dysfunction‐associated steatotic liver disease (MASLD). In this process, hepatocyte inflammation‐caused upregulation of its receptor, Takeda G protein‐coupled ...
Senlin Lian +10 more
doaj +2 more sources
Therapeutic Opportunities of GPBAR1 in Cholestatic Diseases
Frontiers in Pharmacology, 2022 GPBAR1, a transmembrane G protein-coupled receptor for bile acids, is widely expressed in multiple tissues in humans and rodents. In recent years, GPBAR1 has been thought to play an important role in bile homeostasis, metabolism and inflammation.
Fangling Zhang +9 more
doaj +1 more source
Journal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 2023 Background Patients with nonalcoholic fatty liver disease are at increased risk to develop atherosclerotic cardiovascular diseases. FXR and GPBAR1 are 2 bile acid–activated receptors exploited in the treatment of nonalcoholic fatty liver disease: whether
Silvia Marchianò +20 more
doaj +1 more source