G Protein-coupled Receptors (GPCRs)

G protein-coupled receptors (GPCRs) are the largest class of membrane proteins in the human genome and they representing the largest family of validated therapeutic targets with over 800 know human GPCRs. The new member’s list is growing daily with advances in new techniques.

About half of GPCRs have sensory functions, mediating olfaction (~400), taste (33), light perception (10) and pheromone signalling. The remaining ~350 non-sensory GPCRs mediate signalling by ligands that range in size from small molecules to peptides to large proteins; they are the targets for the majority of drugs in clinical usage. Over 1500 drugs were approved by the FDA, where around 40% drugs target mainly GPCRs.

To support researchers drug R&D activity, ScreeNingBio encourages exploring all possible signaling scenarios with a variety of available biologically-relevant cell-based functional and binding assays and stable cell lines.

ScreeNingBio’s stable GPCR panel including the full human, mouse and rat GPCRs which are no promiscus G protein co-transfection. The GPCR products in the ScreeNingBio are sensitive and robust for detecting receptor-mediated second messenger signals (cAMP, IP1 and calcium), β-arrestin recruitment, receptor internalization, and ligand binding. These assays are suitable for the compounds profiling and high throughput screening.

cAMP Assays: Homogeneous TR-FRET cAMP detection cell-based assays to monitor the functional status of GPCRs upon small molecules or biologics binding. Characterize ligand pharmacology and obtain reproducible performance with large assay windows and broad sensitivity ranges.

IP1 Assays: Homogeneous TR-FRET IP1 detection cell-based assays to monitor the functional status of GPCRs upon small molecules or biologics binding. Characterize ligand pharmacology and obtain reproducible performance with large assay windows and broad sensitivity ranges.

Calcium Assays: Fluorescent dye-based assays to measure calcium mobilization in cell lines as a direct indication of GPCR activation or inhibition.

β-Arrestin Assays: Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin. Ideal for ligand bias analysis, antagonist mode screening, and studying virtually any GPCR including orphan receptors.

GPCR Internalization Assays: Secondary, orthogonal screening cell-based assays for measuring GPCR desensitization and recycling as well as uncovering novel classes of compound pharmacologies and identifying safer drugs without imaging or antibodies.

Membrane Preparations: Purified membrane preps for obtaining GPCR ligand binding affinities and evaluating GPCR activity through GTPγS functional studies in response to the addition of a ligand or therapeutic.

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