GPCR antibodies

G protein-coupled receptors (GPCRs) are one of the major classes of drug targets and an estimated 30-50% of all marketed drugs act on them. They are integral membrane receptors that transmit signals from various small molecules, peptides and lipids via G proteins where they affect many physiological functions in almost all organs.

Understanding the tissue distribution of a particular GPCR, and thus its potential physiological function and therapeutic potential, is an important part of pharmacological target validation in the drug discovery process. To aid in this endeavour, Biomol International has produced an extensive line of 53 antibodies against many GPCRs, which can be used in tissue distribution studies.

The antibodies have been produced using peptide antigens of specific and unique epitopes in each GPCR. All can be used in immunoblots, most can be used in immunohistochemistry and some are validated for flow cytometry.

Some examples from the Biomol range are: Anti-Calcium Sensing Receptor (extracellular) — CaSR regulates cellular processes such as proliferation, apoptosis and differentiation; Anti-Melanocortin Receptor 1, 2, 3 and 4 — MCR expression in melanoma cells is up-regulated up to 20 fold compared to normal melanocytes; Anti-Bombesin Receptor 1, 2 and 3 — BB is coupled to a Gq/11 protein that activates phospholipase C and leads to the production of inositol 1, 4, 5 triphosphate, intracellular Ca2+ mobilisation and cell growth; and Anti-B1 and B2 Bradykinin Receptor — Expression of BKRB1 is inducible in various types of tissue injury and BKRB2 is widely expressed throughout the central and peripheral nervous systems.