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Department of Pharmacology, Emory University School of Medicine, Atlanta Georgia
Abstract
Abstract I. Introduction A. GABAB Receptors B. Taste Receptors C. Adrenergic Receptors D. Opioid Receptors E. Somatostatin Receptors F. Purinergic Receptors G. Olfactory Receptors H. Vasopressin, Oxytocin, and Other Receptors II. Clinical Significance of GPCR Heterodimerization III. Conclusions
G protein-coupled receptors (GPCRs) are cell surface receptors that mediate physiological responses to a diverse array of stimuli. GPCRs have traditionally been thought to act as monomers, but recent evidence suggests that GPCRs may form dimers (or higher-order oligomers) as part of their normal trafficking and function. In fact, certain GPCRs seem to have a strict requirement for heterodimerization to attain proper surface expression and functional activity. Even those GPCRs that do not absolutely require heterodimerization may still specifically associate with other GPCR subtypes, sometimes resulting in dramatic effects on receptor pharmacology, signaling, and/or internalization. Understanding the specificity and functional significance of GPCR heterodimerization is of tremendous clinical importance since GPCRs are the molecular targets for numerous therapeutic drugs.
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