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Review
. Jul-Aug 2010;77(4):374-80.
doi: 10.1002/msj.20199.

Role of Antibodies in Developing Drugs That Target G-protein-coupled Receptor Dimers

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Free PMC article
Review

Role of Antibodies in Developing Drugs That Target G-protein-coupled Receptor Dimers

Chris Hipser et al. Mt Sinai J Med. .
Free PMC article

Abstract

G-protein-coupled receptors are important molecular targets in drug discovery. These receptors play a pivotal role in physiological signaling pathways and are targeted by nearly 50% of currently available drugs. Mounting evidence suggests that G-protein-coupled receptors form dimers, and various studies have shown that dimerization is necessary for receptor maturation, signaling, and trafficking. However, the physiological implications of dimerization in vivo have not been well explored because detection of GPCR dimers in endogenous systems has been a challenging task. One exciting new approach to this challenge is the generation of antibodies against specific G-protein-coupled receptor dimers. Such antibodies could be used as tools for characterization of heteromer-specific function; as reagents for their purification, tissue localization, and regulation in vivo; and as probes for mapping their functional domains. In addition, such antibodies could serve as alternative ligands for G-protein-coupled receptor heteromers. Thus, heteromer-specific antibodies represent novel tools for the exploration and manipulation of G-protein-coupled receptor-dimer pharmacology.

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Figure 1
Figure 1
A monoclonal antibody can be generated that specifically recognizes receptor heteromers, but not homomers. It can be used as a tool to detect receptor heteromers in vivo and to characterize heteromer-specific signaling.

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