HUMAN RECOMBINANT CCK2 RECEPTOR
MULTISCREEN™ DIVISION ARRESTED CELL LINE
1 vial (4 x 106) frozen cells
Cell Banker 2 (Amsbio)
Expression vector containing full-length human CCKBR cDNA (GenBank Accession Number NM_176875.2) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS
Background: Cholecystokinin B receptor (CCKBR/CCK2R) is a 447-amino acid 7 transmembrane protein. The cholecystokinin (CCK) family of peptides and their receptors are widely distributed throughout the central nervous system and gastrointestinal tract. CCKBR is a type B (gastrin) receptor that has high affinity for both sulfated and nonsulfated CCK analogs found principally in the CNS and select areas of the gastrointestinal tract.Type B receptors regulate anxiety, arousal, neuroleptic activity and opiate-induced analgesia. Outside of the CNS they regulate gastric acid secretion and may play a role in gastrointestinal motility and growth of normal and neoplastic gastrointestinal tissue. Northern hybridization shows CCKBR expressed in the stomach, pancreas, brain and gallbladder. The cholecystokinin-2 receptor (CCK-2R) is overexpressed in several human cancers but displays limited expression in normal tissues. For this reason, it is a suitable target for developing specific radiotracers.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MULTISCREEN™Calcium 1.0 No Wash Assay Kit (Multispan MSCA01).
Verona et al. (2021). Preliminary Study of a 1,5-Benzodiazepine-Derivative Labelled with Indium-111 for CCK-2 Receptor Targeting. Molecules. Feb 9;26(4):918.
Beinborn et al. (1993) A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists. Nature 362:348-350.
Pisegna et al. (1992) Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization. Biochem Biophys Res Commun 189:296-303.