Open AccessRole of Antibodies in Developing Drugs That Target G‐Protein‐Coupled Receptor Dimers
Author(s) -
Hipser Chris,
Bushlin Ittai,
Gupta Achla,
Gomes Ivone,
Devi Lakshmi A.
Publication year - 2010
Publication title -
mount sinai journal of medicine: a journal of translational and personalized medicine
Language(s) - English
Resource type - Journals
eISSN - 1931-7581
pISSN - 0027-2507
DOI - 10.1002/msj.20199
Subject(s) - receptor , g protein coupled receptor , drug discovery , antibody , signal transduction , in vivo , chemistry , computational biology , microbiology and biotechnology , biology , biochemistry , immunology , genetics
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. Mt Sinai J Med 77:374–380, 2010. © 2010 Mount Sinai School of Medicine