Assay Designs™ is the exclusive worldwide distributor of Proteimax activation-state specific GPCR antibodies.
G protein-coupled receptors (GPCRs) are a ubiquitous family of transmembrane molecules that act as sensors for extracellular stimuli including hormones, neurotransmitters, and sensory stimuli such as light and smell. GPCRs are characterized by their conserved structure of seven transmembrane-spanning helices, as well as extracellular N-terminal and intracellular C-terminal domains which are more diverse in length and function across receptor sub-types.
GPCR-mediated signaling is carried out by coupling of heterotrimeric G proteins to the agonist-bound receptor. Upon receptor activation the GTP-hydrolyzing alpha subunit and beta/gamma dimer dissociate from each other to form two independent signaling units that signal through GPCR-associated effector molecules including adenylyl cyclases, ion channels, and other enzymes. This complex and versatile signaling system regulates cAMP production, intracellular Ca2+ and K+ levels, and controls cellular processes such as sensory perception, synaptic transmission, hormone release, cell growth and differentiation.
These conformation-specific antibodies are sensitive to a conformational shift in the GPCR extracellular N-terminus upon agonist activation, thus distinguishing between inactive and agonist-activated receptor states. Application protocols and sample data are available in our online support section.