G-Protein Coupled Receptors

G protein-coupled receptors (GPCRs) are a large and diverse family of transmembrane receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. They contain seven membrane-spanning helices, an extracellular N-terminus and an intracellular C-terminus.

They are involved in regulating many processes including neurotransmission and neuromodulation. The importance of these receptors is underscored their role in the drug discovery.

 Images: Mouse frontal cortical neuron cultures (p1 pups, day 4 culture stained with 5-HT2AR at 1:100 48 hours. MAP2 Ab: 1:20,000, 24 h. Courtesy of Laura Bohn, Scripp's Insitute. Details in Schmid, Raehal, and Bohn; 2008; PNAS.