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...
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...
Background 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 brain and is thought to be neuroprotective. Here, we hypothesize that dysfunction of central TGR5 may contribute to the ...
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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 anhedonia in depression. Anhedonia is a psychological condition...
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 anh...
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,中国科学院上海药...
We disclose GPR26 G-protein coupled receptor (GPCR) polypeptides comprising the amino acid sequence shown in SEQ ID NO. 3 or SEQ ID NO: 5, and homologues, variants and derivatives thereof. Nucleic acids capable of encoding GPR26 polypeptide are also disclosed. The GPR26 receptor is useful in...
PI3Kα, PI3Kβ, and PI3Kδ associate with a regulatory subunit, p85, and are activated by growth factors and cytokines through a tyrosine kinase-dependent mechanism; PI3Kγ associates with two regulatory subunits, p101 and p84, and is activated by G-protein-coupled receptors. See C. Jimenez, ...
takeda G protein-coupled receptor 5OBJECTIVE 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 ...