Biological Information

Background Information:

Cholecystokinin receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Cholecystokinin CCK1 receptors are found in high concentrations in the gastrointestinal tract and a few discrete brain regions.

PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.

Family:

GPCR

Sub Family:

Cholecystokinin

Class:

Class A

Protein Name:

CCK1 (CCKA)

Uniprot Number:

P32238

Protein Aliases:

CCK-AR|Cholecystokinin-1 receptor|CCK1-R

Gene Name:

CCKAR

Gene ID:

886

Accession Number:

AY322549

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

PAM

Testing Information

Control Activator:

Sincalide

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

CCK1 receptor agonism may enhance pancreatic exocrine secretion and gall bladder contraction while reducing gastric emptying and food intake. CCK1 receptor antagonism may decrease symptoms of constipation predominant IBS and functional dyspepsia.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA