Signal transduction cascades initiated by G﹑roteinヽoupled receptors (GPCRs) integrate a number of components including seven﹑ass transmembrane receptors (7TM), heterotrimeric G﹑roteins, downstream protein kinases and responsive transcription factors. This signalling pathway has evolved to facilitate a...
G protein-coupled receptors (GPCRs) are membrane proteins that play important roles in signal transduction and cellular communication. As such, GPCRs are often targeted by therapeutics, including small molecule drugs and antibody drugs. Small molecule drugs and antibody drugs targeting G protein-couple...
Whenever a G protein is active, both its GTP-bound alpha subunit and its beta-gamma dimer can relay messages in the cell by interacting with other membrane proteins involved in signal transduction. Specific targets for activated G proteins include various enzymes that produce second messengers, as...
Drs. Gilman and Rodbell (who jointly were awarded the Nobel Prize in 1994), established that molecules referred to asguaninenucleotide-binding proteins (G proteins) help send the signal from GPCRs located on the
receptors(GPCRs) are membrane proteins that play important roles in signal transduction and cellular...
GPCR Signal Detection We deploy multiplexed detection for cAMP, calcium flux, IP1/IP3, and β-arrestin recruitment, covering Gi/Gs/Gq-coupled receptors. Customized reporter gene assays validate pathway-specific activation, critical for characterizing biased signaling in cancer immunotherapy and metabolic ...
The dissection of different receptor-mediated signal transduction pathways underpins the scientific and potential therapeutic benefits of biased ligands. Pathway validation links specific signaling pathways to different pharmacological outcomes, establishing both the mechanisms of receptor function and opportunities...
By regulating both the functional status and number of plasma membrane located GPCRs the GRKs play a pivotal role in modulating GPCR-mediated signal transduction. GPCRs are a pharmacologically important protein family with approximately 450 genes identified to date. Pathways involving these receptors ...
Signal transduction via G-protein-coupled receptors (GPCRs) is a fundamental pathway through which the functions of an individual cell can be integrated within the demands of a multicellular organism. Since this family of receptors first discovered, the proteins that constitute this signaling cascade ...
5. Yang, D., et al., G protein-coupled receptors: structure-and function-based drug discovery. Signal transduction and targeted therapy, 2021. 6(1): p. 7. 6. Buck, A.K., et al., CXCR4-targeted theranostics in oncology. Eur J Nucl Med Mol Imaging, 2022. 49(12): p. 4133-4144...