Molecular Function

G Protein-Coupled Receptor (GPCR) Function

G protein-coupled receptors (GPCRs), also known as seven transmembrane receptors, 7TM receptors, heptahelical receptors, and G protein-linked receptors (GPLR), are a protein family of transmembrane receptors that transduce an extracellular signal (ligand binding) into an intracellular signal (G protein activation). GPCRs are the largest protein family known, with somewhere between 600 and 1,000 members, and are involved in many types of stimulus-response pathways.

The function of GPCRs is highly diverse and GPCRs recognize a wide range of ligands, including photons, small molecules, and proteins. Not surprisingly, GPCRs have been linked to many normal biological as well as pathological conditions. In fact, about 45% of modern medicinal drugs affect this target class.

Some key challenges facing researchers interested in the function of GPCRs include understanding novel modes of regulation of GPCRs in an effort to better understand both normal and abnormal cellular processes, particularly processes that might underlie specific disease conditions. Researchers are focused on everything from GPCR structure/function to RNA editing and alternate mRNA splicing to signaling via G proteins and downstream messenger systems to interaction of receptors with accessory proteins.

Molecular Devices offers a variety of GPCR assays as well as a wide range of analytical systems to support studies of GPCR function, including microplate readers, washers, and handlers as well as cellular screening, imaging, and label-free systems. Learn more by selecting among the links below.

GPCR Assay Kits

SpectraMax® Microplate Readers

FlexStation® 3 Benchtop Multi-Mode Microplate Reader 

ImageXpress® High Content Imaging Systems

CellKey® Label-Free Gi/Gs Analysis System

FLIPR® Tetra High Throughput Cellular Screening System