TGR5也被称为G蛋白胆汁酸偶联受体1(G protein-coupled bile acid receptor 1,GPBAR1),与Gαs相偶联,广泛表达于多种的细胞类型。 TGR5的激活不仅可以直接刺激胰岛β细胞分泌胰岛素,也可作用于肠内分泌细胞,通过促进GLP-1(glucagon-like peptide 1)的分泌,以间接的方式作用于胰岛素的分泌,因而成为备受关注糖尿病药物...
胆汁酸受体TGR5(Takeda G protein-coupled receptor 5)在血糖稳态、能量消耗和肝脏保护等方面起重要作用,是一个极具潜力的治疗代谢综合征及炎症性疾病的药物靶点。然而,多种已报道的TGR5激动剂在人和小鼠体内存在较大的活性差异,利用现有的啮齿类动物模型开展化合物药效学和毒理学研究会产生偏差。近日,中国科学院上海...
Takeda G Protein–Coupled Receptor 5 Modulates Depression-like Behaviors via Hippocampal CA3 Pyramidal Neurons Afferent to Dorsolateral Septum Author links open overlay panelHao Wang a 1, Yuan-Zhi Tan a 1, Rong-Hao Mu a, Su-Su Tang a, Xiao Liu a, Shu-Yu...
This phase II trial compares the effects of immunoglobulin replacement therapy with a placebo for preventing infectious complications in patients receiving CD19 chimeric antigen receptor (CAR)-T cell therapy. Hypogammaglobulinemia is a common complication in patients who receive CD19 CAR-T cell therapy...
OBJECTIVE Takeda G protein-coupled receptor 5(TGR5)is recognized as a promising target for type 2 diabetes and metabolic syndrome;its expression has been demonstrated in the brain and is thought to be neuroprotective.Here,we hypothesize that dysfunction of central TGR5 may contribute to the pathogene...
Takeda G protein-coupled receptor 5(TGR5)Serotonin(5-HT)High fat,high fructose,and high sucrose(HFS)Background and aims:Diet-induced obesity and metabolic syndrome can trigger the progression of fatty liver disease to non-alcoholic steatohepatitis and fibrosis,which is a major public health concern...
Bile acids play a critical role in the regulation of glucose, lipid and energy metabolisms by activating the nuclear bile acid receptor farnesoid X receptor (FXR) and membrane G protein-coupled bile acid receptor-1 (aka takeda G protein couple receptor 5, TGR5) signaling. Paradoxical roles of...
TAK-041 is a potential first-in-class G Protein-Coupled Receptor 139 (GPR139) agonist. TAK-041 has completed multiple Phase I studies and is a Phase II study-ready compound with the potential to be developed for the treatment of anhed...
A novel G-protein coupled receptor protein, a partial peptide and their salts are disclosed. DNA encoding the receptor protein, production of the receptor protein, determination of a ligand to the rec
Molecular Cloning and Chromosomal Localization of the Mouse Gpr37 Gene Encoding an Orphan G-Protein-Coupled Peptide Receptor Expressed in brain and Testis, Daniela Marazziti, et al., Genomics 53, 315-324 (1998) Article No. GE985433. Dorland's Illustrated Medical Dictionary, 28th ed. (1994)...