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.

Dr EJ Dell Dr EJ Dell (10)

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 (fig. 1), there are consequently many diseases where GPCRs have gone awry. Over half of the drugs on the market work via GPCRs. Some compounds, such as synthetic cannabinoid receptor agonists are also associated to severe drug misuse. This makes GPCRs one of the most studied families of proteins in research labs throughout the world. Therefore many microplates-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.

Fig. 1: Example of GPCR: Human k-opioid receptor with opioids as ligands.

 

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