Screen Quest™ HEK-CNGC-Cannabinoid Receptor 1 Cells

G protein coupled receptors (GPCRs) are one of the largest receptor classes targeted by drug discovery programs. Calcium flux (coupled via Gq pathway) assay is a preferred method in drug discovery for screening GPCR targets. However, over 60% of the known GPCRs signal through adenylyl cyclase activity coupled to cAMP. Most of the existing cAMP assays not only require cell lysis but also lack both temporal and spatial resolution. Screen Quest™ cell lines enable to investigate GPCR that do not conventionally couple through intracellular calcium. Screen Quest™ cell lines are based on a series of G-protein chimeras, including the promiscuous G-protein, Gα16, and an exogenous cyclic nucleotide-gated channel (CNGC). The chimeras consist of the alpha subunit of a Gq-protein complex whose 5 carboxy-terminal amino acids have been replaced with those from one of the other G-proteins (either Gαs, Gαi, Gαo, or Gαz). These amino acids are responsible for the coupling of the receptor to its G-protein. Co-expression of these chimeras or CNGC with specific non-Gq-coupled receptors may result in the generation of an intracellular calcium signal upon receptor stimulation. Screen Quest™ HEK-CNGC-Cannabinoid Receptor 1 (CB1) cell line is HEK-293 cells stably transfected with both the CNGC and human Cannabinoid Receptor. The constitutively expressed CNGC in the cells responds in real-time to increases or decreases in intracellular cAMP levels by coordinately altering cation flux (e.g., calcium, potassium or sodium). Activation of the CB1 in these cells by specific ligands can be detected with either a calcium-sensitive fluorescent indicator (such as Calbryte 520 AM, Cal-520 AM, Fluo-8 AM, or Fluo-4 AM and corresponding no wash calcium kit) or an AAT’s optimized membrane-potential assay kit. This cell line has been successfully used in drug discovery and screening environments for studying GPCRs that do not conventionally couple through intracellular calcium. It has been effectively used with FLIPR and FDSS systems.

<p>Screen Quest™ Live Cell cAMP Assay Principle</p>

Protocol

SDS

COA

Catalog	Size	Price	Quantity
38001	Each	Price

Citations

View all 2 citations: Citation Explorer

Activation of P2X7 and P2Y11 purinergic receptors inhibits migration and normalizes tumor-derived endothelial cells via cAMP signaling

Authors:

Avanzato, D and Genova, T and Pla, A Fiorio and Bernardini, M and Bianco, S and Bussolati, B and Mancardi, D and Giraudo, E and Maione, F and Cassoni, P and others, undefined

Journal:

Scientific Reports (2016)

The M2 muscarinic receptors are essential for signaling in the heart left ventricle during restraint stress in mice

Authors:

Tomankova, Hana and Valuskova, Paulina and Varejkova, Eva and Rotkova, Jana and Benes, Jan and Myslivecek, Jaromir

Journal:

Stress (2015)

References

View all 132 references: Citation Explorer

cAMP-Induced Histones H3 Dephosphorylation Is Independent of PKA and MAP Kinase Activations and Correlates With mTOR Inactivation

Authors:

Rodriguez P, Rojas J.

Journal:

J Cell Biochem (2016): 741

Changes in the Arabidopsis thaliana Proteome Implicate cAMP in Biotic and Abiotic Stress Responses and Changes in Energy Metabolism

Authors:

Alqurashi M, Gehring C, Marondedze C.

Journal:

Int J Mol Sci (2016): 852

Role of the cAMP Pathway in Glucose and Lipid Metabolism

Authors:

Ravnskjaer K, Madiraju A, Montminy M.

Journal:

Handb Exp Pharmacol (2016): 29

Odor-induced cAMP production in Drosophila melanogaster olfactory sensory neurons

Authors:

Miazzi F, Hansson BS, Wicher D.

Journal:

J Exp Biol (2016): 1798

A cardiac mitochondrial cAMP signaling pathway regulates calcium accumulation, permeability transition and cell death

Authors:

Wang Z, Liu D, Varin A, Nicolas V, Courilleau D, Mateo P, Caubere C, Rouet P, Gomez AM, V and ecasteele G, Fischmeister R, Brenner C.

Journal:

Cell Death Dis (2016): e2198

Storage, safety and handling

H-phrase	H303, H313, H333
Hazard symbol	XN
Intended use	Research Use Only (RUO)
R-phrase	R20, R21, R22
Storage	Liquid nitrogen
UNSPSC	12352200

Telephone
Fax
Email	sales@aatbio.com
International	See distributors
Bulk request	Inquire
Custom size	Inquire
Technical Support	Contact us
Request quotation	Request
Purchase order	Send to sales@aatbio.com
Shipping	Standard overnight for United States, inquire for international

Page updated on July 12, 2023