GLP1R/CRE/LUCI HEK293熒光穩(wěn)轉(zhuǎn)細(xì)胞株GPCR靶點(diǎn)藥物篩選細(xì)胞 BioVector NTCC質(zhì)粒載體菌種細(xì)胞基因保藏中心

G蛋白偶聯(lián)受體（G Protein-Coupled Receptors，GPCRs）是一大類膜蛋白受體的統(tǒng)稱。這類受體的共同點(diǎn)是其立體結(jié)構(gòu)中都有7個(gè)跨膜α螺旋，且其肽鏈的C端和連接第5和第6個(gè)跨膜螺旋的胞內(nèi)環(huán)上都有G蛋白（鳥苷酸結(jié)合蛋白）的結(jié)合位點(diǎn)。研究顯示G蛋白偶聯(lián)受體只見于真核生物之中，而且參與了很多細(xì)胞信號(hào)轉(zhuǎn)導(dǎo)過(guò)程。在這些過(guò)程中，G蛋白偶聯(lián)受體能結(jié)合細(xì)胞周圍環(huán)境中的化學(xué)物質(zhì)并激活細(xì)胞內(nèi)的一系列信號(hào)通路，最終引起細(xì)胞狀態(tài)的改變。已知的與G蛋白偶聯(lián)受體結(jié)合的配體包括氣味，費(fèi)洛蒙，激素，神經(jīng)遞質(zhì)，趨化因子等等。這些配體可以是小分子的糖類，脂質(zhì)，多肽，也可以是蛋白質(zhì)等生物大分子。一些特殊的G蛋白偶聯(lián)受體也可以被非化學(xué)性的刺激源激活，例如在感光細(xì)胞中的視紫紅質(zhì)可以被光所激活。與G蛋白偶聯(lián)受體相關(guān)的疾病為數(shù)眾多，并且大約40%的現(xiàn)代藥物都以G蛋白偶聯(lián)受體作為靶點(diǎn)。
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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