Journal
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 56
Volume 56, Issue -, Pages 403-+Publisher
ANNUAL REVIEWS
DOI: 10.1146/annurev-pharmtox-011613-135952
Keywords
allosterism; dimerization; oligomers; proximity-based assays; biochemical fingerprint; heterodimerization; bivalent ligands
Categories
Funding
- NIDA NIH HHS [R01 DA008863, R37 DA008863, R56 DA008863, DA008863] Funding Source: Medline
- NINDS NIH HHS [R01 NS026880, NS026880] Funding Source: Medline
- NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE [R01NS026880, R29NS026880] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE ON DRUG ABUSE [R01DA008863, R37DA008863, R56DA008863] Funding Source: NIH RePORTER
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Gprotein-coupled receptors (GPCRs) compose one of the largest families of membrane proteins involved in intracellular signaling. They are involved in numerous physiological and pathological processes and are prime candidates for drug development. Over the past decade, an increasing number of studies have reported heteromerization between GPCRs. Many investigations in heterologous systems have provided important indications of potential novel pharmacology; however, the physiological relevance of these findings has yet to be established with endogenous receptors in native tissues. In this review, we focus on family A GPCRs and describe the techniques and criteria to assess their heteromerization. We conclude that advances in approaches to study receptor complex functionality in heterologous systems, coupled with techniques that enable specific examination of native receptor heteromers in vivo, are likely to establish GPCR heteromers as novel therapeutic targets.
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