GPCRs/G Protein Interaction Assay Services

Highly automated liquid-dispensing systems along with detection devices that quickly and sensitively identify signals produced in radiometric, fluorometric, or luminous assays have been used for the evaluation of a large number of drugs at GPCRs. But as our understanding of GPCR function deepens-especially when studying it in a cellular setting-it becomes evident that new strategies are required to find the chemicals that affect GPCR activity. GPCR-G-protein coupling is thought to have a stoichiometry of 1:1. They could, nevertheless, also work in assemblies through the creation of dimers or even higher-order assemblies. It does explain how GPCRs display tissue-dependent pharmacologies. Creative Biolabs offers GPCRs/G protein interaction assay services to meet the requirements of our clients.

G Protein Pathways

Heterotrimeric guanine nucleotide-binding proteins (G proteins) are transducers of signals that link receptors to effectors and, in turn, to intracellular signaling pathways. They are affixed to the plasma membrane of cells. The three subunits that make up G proteins are α, β, and γ. They essentially act as dimers while signaling since the Gα subunit or the Gβγ complex transmits the signal. Gβγ subunits often cannot separate in nondenaturing environments. At present, 20 Gα, 6 Gβ, and 11 Gγ subunits are identified.

The Gα subunits are classified into four groups based on sequence similarity. The effector pathways of the Gs and Gq families are phospholipase C-β (PLC-β) and adenylyl cyclase, respectively. The Gα (Gαo, Gαi) and Gβγ complexes have been found to have several additional downstream effector pathways. The transducin pathway, which governs the detection of light in the eye, is arguably the most well-understood of the Gi family pathways.

Some signaling pathways through G protein. (Neves, et al, 2002) Fig.1. Regulation of systemic functions by signaling through G protein pathways.¹

Gβγ

Apart from its supportive function in GPCR-dependent Gα interactions, Gβγ independently regulates downstream signaling. Atrial myocytes' acetylcholine-regulated, inwardly-rectifying K+ channel was the first effector discovered to be triggered by Gβγ. The fact that the acetylcholine-driven channel activation in isolated inside-out patches from atrial myocytes was independent of soluble second messengers was a crucial finding, indicating that the Gi protein's subunits may be able to independently activate the channel. The roles of Gβγ subunits in mediating downstream signaling from GPCRs are now well known, and they may be just as common as those mediated by Gα subunits.

Important players in G protein signaling include scaffolding receptors, G protein α subunits, effectors, and G protein βγ subunits. The significance of this protein in a wide range of physiological processes is becoming clearer as research into it advances. The interaction between GPCRs and G proteins may play a major role in the development of novel pharmacologic approaches to therapies for a number of significant disorders, given the biological potential of these proteins as therapeutic targets. Please contact us for more information about our GPCRs/G protein interaction assay services. Our scientists will effectively design and create the best method for your project.

Reference

Neves, et al.; "G protein pathways." Science 296.5573 (2002): 1636-1639.

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