Friday, October 12, 2012

Focus On G-protein Coupled Receptors (GPCRs)

With Robert Lefkowitz and Brian Kobilka winning the 2012 Nobel Prize in Chemistry for their work on G-protein Coupled Receptors or GPCRs, here is a repost of part of an older blog that discusses this class of proteins. Congratulations to Drs. Lefkowitz and Kobilka for their achievement.

Beta2Receptor-with-GsG-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. Over half of the drugs on the market work via GPCRs. 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

Here is a list of BMG LABTECH application notes  were these can be found.
For more GPCR and other applications, visit our applications center at: