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G Protein-Coupled Receptors: A New Target for Monoclonal Antibodies.

G protein-coupled receptors (GPCRs) are a large family of proteins that play important roles in human health and disease. Roughly one third of all approved medicines work by targeting a GPCR however, historically none of these medicines have been monoclonal antibodies.

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Figure 1: Activation of the G alpha subunit of a G-protein-coupled receptor In unstimulated cells, the state of G alpha (orange circles) is defined by its interaction with GDP, G beta-gamma (purple circles), and a G-protein-coupled receptor (GPCR; light green loops). Upon receptor stimulation by a ligand called an agonist, the state of the receptor changes. G alpha dissociates from the receptor and G beta-gamma, and GTP is exchanged for the bound GDP, which leads to G alpha activation. G alpha then goes on to activate other molecules in the cell. © 2002 Nature Publishing Group Li, J. et al. The Molecule Pages database. Nature 420, 716-717 (2002). All rights reserved.

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