Friday, July 13, 2012

Focus On G-protein Coupled Receptors (GPCRs)

Image by: S. Jähnichen

G-protein Coupled Receptors or GPCRs are a class of over 1000 different receptors found throughout the human body that have a distinct seven transmembrane domain region. GPCRs are involved in almost every biological process in the body including vision, taste, smell, touch, cardiovascular, respiratory, growth, differentiation, etc. These receptors are associated with a family of intracellular proteins known as heterotrimeric G-proteins. When a specific GPCR is activated, a specific heterotrimeric G-protein is subsequently activated and this leads to a series of specific downstream effects, which can include PIP2 and IP3 production, calcium release, cAMP or cGMP production or inhibition, MAP kinase activation, and beta-arrestin activation, to name a few.

Since GPCRs are involved with many biological processes, there are consequently many diseases where GPCRs have gone awry. This makes GPCRs one of the most studied family of proteins in research labs throughout the world. Therefore many microplate based GPCR and heterotrimeric G-protein assays have been developed to study these systems on microplate readers. Here is a brief list of GPCR related assays that can be performed on a BMG LABTECH microplate reader:

227 - Quantifying Fluorescent Ligand Binding to GPCRs in Live Cells using the PHERAstar FS
225 - Methyltransferase, Acetyltransferase, Kinases, and GTPases Can All Be Measured with Transcreener® Assays
222 - HTS Instrument Discovers Low Affinity Inhibitors of the IP Signaling Pathway
221 - Monitoring Intracellular cAMP with hMSC cAMP biosensor using the LUMIstar Omega
216 - Monitoring Intracellular Ca2+ Fluxes with Clonetics™ primary sensors
210 - An AlphaScreen® SureFire® Phospho-ERK1/2 assay performed on POLARstar Omega
209 - GPCR Activation is Measured with Cisbio’s cAMP and IP-One HTRF® HTplex™ Cell-based Assay
206 - Cellular Dopamine and Intracellular Calcium Signaling Using the Next Generation Microplate Reader
196 - Using Intrinsic Tryptophan Fluorescence to Measure Heterotrimeric G-Protein Activation
194 - FRET-based screening for potential modulators of the Gαi1 protein/GoLoco interaction
193 - Functional Screening of recombinant CHO-M1 cells using the PHERAstar from BMG LABTECH
177 - HTRF®IP-One Terbium-based assay performed on BMG LABTECH´s PHERAstar Plus
157 - Calcium Detection Upon GPCR Stimulation Using the NOVOstar and Screen Quest
143 - Study of GPCR pharmacology using the DiscoveRx HitHunter
142 - HitHunter™ IP3 Assay for GCPR Screening using the PHERAstar
134 - New HitHunter cAMP XS+ Assay for GPCR Screening Using the PHERAstar
107 - Rapid functional screening at dopamine receptors by measuring intracellular calcium with the NOVOstar fluorescence reader
104 - Intracellular Calcium Assay performed on NOVOstar Microplate Reader

For more gpcr and other applications, visit our applications center at:

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