GPCR activation

Another popular assay for GPCR activation is to measure the increase in intracellular Ca2+ that occurs upon activation. GPCRs on the cell surface produce inositol triphosphate (IP3) via the action of Phospholipase C (PLC). IP3 stimulates calcium channels called IP3 receptors on the endoplasmic reticulum, which raise... 

Additional methods for measuring GPCR activation are reviewed in Sect. 6.3.3 on High Content Screening. 

G Protein Coupling Molecular Mechanism of GPCR Activation... 

The identification and characterization of the processes of GPCR activation and inactivation have defined the genomics of the accessory proteins necessary to these processes. This has accelerated progress in understanding the fundamental mechanisms involved in GPCR synthesis, transport to the membrane, ligand binding, and activation and inactivation by GRK-mediated (and other) phosphorylation (192). 

Diversity parameters for this reference database are shown in Table 12.2. As evident from the number of screens, the number of core heterocyclic fragments, and the diversity coefficients (all these parameters are calculated using the Diversity module [25] of the ChemoSoft software tool), the studied compound database has high structural diversity and can be considered to be a good representation of known GPCR-active compounds. 

For GPCR gene sequences predicted to be the G j binding type, we choose them as candidates for experimental analysis, because this type controls intracellular calcium content, enabling us to monitor GPCR activity more easily. 

SOME MECHANISTIC INSIGHTS INTO GPCR ACTIVATION FROM DETERGENT-SOLUBILIZED TERNARY COMPLEXES ON BEADS... 

SOME MECHANISTIC INSIGHTS INTO GPCR ACTIVATION... 

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