G-protein-coupled receptors (GPCRs) are considered as the largest and most diverse group of membrane receptors in eukaryotes. They act as an inbox for extracellular signals (in form of light energy, peptides, lipids, sugars, and proteins, etc.) and participate in many key physiological functions. Dysfunction/abnormal expression of GPCRs can lead to many diseases. Therefore, GPCRs are currently among the most popular therapeutic targets (30%-40% of current marketed drugs). Creative Biolabs has developed an innovative Magic™ GPCR cell line platform engineered with specialty biosensors to accelerate diverse GPCR drug discovery campaigns. Especially, we now provide this well-established Magic™ VIPR1 stable cell line to our global clients for in vitro compound function studies.
Introduction to VIPR1
Vasoactive intestinal polypeptide (VIP) has a wide physiological profile. In the periphery, it induces relaxation in smooth muscle; inhibits secretion in certain tissues, but stimulates secretion in others; and modulates activity of cells in the immune system. In the CNS, it has a range of both excitatory and inhibitory actions. VIP receptors are distributed widely in the periphery and occur throughout the gastrointestinal tract and genitourinary system, other smooth muscles and secretory glands. In the CNS, they are found abundantly in, e.g. the cortex, hippocampus, and thalamus. All VIP receptors activate adenylyl cyclase and induce cAMP production.
There are two structurally distinct receptors that can recognize VIP peptides and pituitary adenylate cyclase activating polypeptide (PACAP) with similar affinities (PACAP/VIPR-1, PACAP/VIPR-2), as well as a specific receptor for the PACAP peptide (PACAP-1).
Magic™ VIPR1 Stable Cell Line
Magic™ VIPR1 stable cell line is constructed through co-transfection of human VIPR1 and cAMP-reactive fluorescent biosensor in U2OS cell surface. Upon receptor activation/inhibition by agonist/antagonist compound, alterations in cellular cAMP will quickly elicit biosensor translocation from plasma membrane to cytosolic vesicles. Therefore, VIPR1 activities will be real-time translated into fluorescence signals, which can be easily monitored and quantified in living cells. This featured cell line has been applied to assay compounds and assess their VIPR1-modulating potentials. It has been proved to be an efficient, simple and flexible strategy for receptor function studies during an early stage.
Featured Advantages of Magic™ VIPR1 Stable Cell Lines
In addition to VIPR1, Creative Biolabs also presents a full catalog of other Magic™ GPCR stable cell lines with cAMP-activated biosensors, including but not limited to:
As alternative, we also provide ready-to-use Magic™ biosensor cell line options to investigate calcium-, DAG-related as well as multiplex pathway events of various GPCRs. Our well-validated cell lines are available in-house, and we are also pleased to tailor custom strains to meet clients' individual requirement. Please contact us for more information and a detailed quote.
For Research Use Only.
