G-protein coupled receptors (GPCRs) have long been a hotspot for drug discovery against various diseases. With extensive experience and leading technologies, Creative Biolabs has established a unique Magic™ GPCR biosensor cell lines for in-depth characterize/evaluate functionalities of GPCR-targeting drug compound. In particular, we now provide a full series of GPCR stable cell lines engineered with calcium-activated biosensors (e.g. BB2, CCK2, M5, NK1, NK3). Here, our scientists are proud to introduce our Magic™ CCK1 stable cell line for our global customers.
Introduction to CCK1
Cholecystokinin is a peptide hormone responsible for stimulating the digestion of fat and protein. Cholecystokinin (CCK) exerts its physiological actions through the activation of two class A G protein-coupled receptors (GPCRs) referred to as type 1 CCK receptor (CCK1) and type 2 CCK receptor (CCK2).
The CCK1 has typical sequences of this family including NPxxY at the intracellular side of transmembrane segment 7 and E/DRY at the intracellular side of transmembrane segment 3. Agonist stimulation of CCK1 causes a conformational change in the receptor that results in receptor coupling with Gq, which subsequently induces PLC activation and an increase in intracellular calcium levels. An increase in calcium drives gene expression, initiates proliferation, controls muscle contraction, triggers fertilization and initiates apoptosis, mediates neurotransmitter release, stimulates fluid and electrolyte secretion.
Fig. 1 Schematic description of the signaling pathways known to be activated by CCK1R and CCK2R.1
CCK1 is widely expressed in different parts of the gastrointestinal tract, such as neurons controlling pancreatic secretion, gallbladder muscularis, muscularis propria of gastric antrum, fundus and pylorus, and vagal afferent neurons. CCK elicits a variety of physiological responses through the CCK1, such as stimulation of gallbladder contraction, inhibition of gastric acid secretion, delay of gastric emptying, induction of post-cibal satiety, and relaxation of the sphincter.
Magic™ CCK1 Stable Cell Line
Generally speaking, GPCRs consist of a single polypeptide that is folded into a globular shape and embedded in a cell's plasma membrane. These cell surface receptors, or so-called second messengers, act as message transducers in the form of peptides, proteins, sugars, and lipids. Activation of a single G protein will alter the activities of second messenger molecules (e.g. Ca2+, cAMP, DAG), which can then translate the signals to diverse downstream cellular events.
Magic™ CCK1 stable cell line has been designed by co-transfecting calcium-responsive biosensor and human cholecystokinin A receptor (CCK1) into U2OS cell line. Based on the special biosensor that can quickly react to calcium changes (via translocating from membrane to cytosol), GPCR activities can be simply monitored and quantified through fluorescent signal changes in living cells. Therefore, it makes an efficient tool to analyze compound function potentials against CCK1.
Featured Advantages of Magic™ CCK1 Stable Cell Lines
Based on the unique Magic™ platform, Creative Biolabs now provides a variety of engineered GPCR stable cell lines for receptor function studies. We are professional in tailoring high-quality, custom-oriented service package to address every specific demand of our clients. If you cannot find your desired target in our catalog, we are always happy to construct a custom cell line for you. Please contact us for more information and a detailed quote.
Reference
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