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...
胆汁酸在体内可激活核受体FXR(farnesoid X receptor)及膜受体TGR5(Takeda G protein-coupled receptor 5)。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...
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 ...
2016 年 5 月,Agios 随后与 Celgene 达成了一项价值 2 亿美元的交易,以开发影响细胞代谢的疗法并探索免疫肿瘤药物的前景。Celgene 此前与 Juno 达成了一项价值 10 亿美元的交易,涉及 CAR-T 和 T 细胞受体技术,现在正在这些领域内支持 Agios。Alaunos Therapeutics(前身为Ziopharm) 2022 年 1 月,Ziopharm 更名...
TC-G 1005TC G 1005,G protein-coupled Bile Acid Receptor 1,levels,coupled,glucose,TCG 1005,Takeda,inh TargetMol®所有产品仅用作科学研究,不为任何个人提供产品和服务产品名称:TC-G 1005CAS:1415407-60-1产品介绍:TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). ...
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-041TAK-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 th...
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...
WO1998049295A1 1998-11-05 LIGAND POLYPEPTIDE FOR THE G PROTEIN-COUPLED RECEPTOR FROM HUMAN PITUITARY GLANDSOther References: Stongin., 1993. “Sensitivity, Specificity, and Predictive Value of Diagnostic Tests: Definitions and Clinical Applications”, in Laboratory Diagnosis of Viral Infections, Lennette...
41. The compound according to claim 1, which is selected from the following compounds: (S)-2-Amino-4-methyl-6-(1-(1-methyl-6-(piperazin-1-yl)-1H-pyrrolo[3,2-b]pyridin-5-yl)ethylamino)pyrimidine-5-carbonitrile; (S)-4-(1-(6-(1,4-Diazepan-1-yl)-1-methyl-1H-pyrrolo[3,2-b...