Role of antibodies in developing drugs that target G-protein-coupled receptor dimers

Chris Hipser, Ittai Bushlin, Achla Gupta, Ivone Gomes, Lakshmi A. Devi

Research output: Contribution to journalReview articlepeer-review

9 Scopus citations


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 receptordimer pharmacology.

Original languageEnglish
Pages (from-to)374-380
Number of pages7
JournalMount Sinai Journal of Medicine
Issue number4
StatePublished - Jul 2010


  • Antibodies
  • Dimers
  • G-protein-coupled receptors
  • GPCRs
  • Heteromers


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