GLP1R/CRE/LUCI HEK293荧光稳转细胞株GPCR靶点药物筛选细胞 BioVector NTCC质粒载体菌种细胞基因保藏中心

GLP1R/CRE/LUCI HEK293荧光稳转细胞株GPCR靶点药物筛选细胞 BioVector NTCC质粒载体菌种细胞基因保藏中心

G蛋白偶联受体（G Protein-Coupled Receptors，GPCRs）是一大类膜蛋白受体的统称。这类受体的共同点是其立体结构中都有7个跨膜α螺旋，且其肽链的C端和连接第5和第6个跨膜螺旋的胞内环上都有G蛋白（鸟苷酸结合蛋白）的结合位点。研究显示G蛋白偶联受体只见于真核生物之中，而且参与了很多细胞信号转导过程。在这些过程中，G蛋白偶联受体能结合细胞周围环境中的化学物质并激活细胞内的一系列信号通路，最终引起细胞状态的改变。已知的与G蛋白偶联受体结合的配体包括气味，费洛蒙，激素，神经递质，趋化因子等等。这些配体可以是小分子的糖类，脂质，多肽，也可以是蛋白质等生物大分子。一些特殊的G蛋白偶联受体也可以被非化学性的刺激源激活，例如在感光细胞中的视紫红质可以被光所激活。与G蛋白偶联受体相关的疾病为数众多，并且大约40%的现代药物都以G蛋白偶联受体作为靶点。
I. Background
GLP1R binds specifically the glucagon-like peptide-1 (GLP1) and has much lower affinity for related peptides such as the gastric inhibitory polypeptide and glucagon.

GLP1R is known to be expressed in pancreatic beta cells. Activated GLP1R stimulates the adenylyl cyclase pathway which results in increased insulin synthesis and release of insulin. Consequently, GLP1R has been suggested as a potential target for the treatment of diabetes.GLP1R is also expressed in the brain where it is involved in the control of appetite. Furthermore, mice which over express GLP1R display improved memory and learning.


II. Introduction
Host Cell:
HEK293

Expressed gene: Genbank Accession Number NM_002062; no expressed tags
Stability: 16 passages
Synonym(s):
GLP-1

Freeze Medium: 45% culture medium, 45% FBS, 10% DMSO
Culture Medium: DMEM, 10% FBS, 500 μg/ml G418
Mycoplasma Status: Negative
Storage: Liquid nitrogen immediately upon delivery
Application(s):
Functional assay for GLP1 receptor


Ⅲ. Description of Host Cell Line
Organism: Human
Tissue: Embryonic kidney
Disease: Normal
Morphology: Epitheloid cell
Growth Properties: Adherent

Ⅳ.Representative Data

Figure 1. GLP-1 (7-37)-induced concentration-dependent stimulation of intracellular luciferase in HEK293/GLP1R/Luc and HEK293 cells.

After stimulation with GLP1 receptor agonist, GLP-1 (7-37), the cells are checked with BrightGlo™Luciferase Assay System and the relative luminescence units (RLU) of

luciferase were recorded on a FlexStation. The RLU were plotted against the log of the cumulative doses (10 -fold dilution) of GLP-1 (7-37) (Mean ± SD, n = 2). The EC50 of GLP-1 (7-37) co-expressing with Luc

in HEK293 cells was 4.91 nM.


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