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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Opioid Receptor Interacting Proteins and the Control of Opioid Signaling

Author(s): Jennifer T. Lamberts and John R. Traynor

Volume 19, Issue 42, 2013

Page: [7333 - 7347] Pages: 15

DOI: 10.2174/138161281942140105160625

Price: $65


Opioid receptors are seven-transmembrane domain receptors that couple to intracellular signaling molecules by activating heterotrimeric G proteins. However, the receptor and G protein do not function in isolation but their activities are modulated by several accessory and scaffolding proteins. Examples include arrestins, kinases, and regulators of G protein signaling proteins. Accessory proteins contribute to the observed potency and efficacy of agonists, but also to the direction of signaling and the phenomenon of biased agonism. This review will present current knowledge of such proteins and how they may provide targets for future drug design.

Keywords: Opioid receptors, regulator of G protein signaling proteins, arrestins, G protein-coupled receptor kinases, protein kinase C, biased agonism, drug discovery.

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