PMID: 20632968Jul 17, 2010Paper

Prime time for G-protein-coupled receptor heteromers as therapeutic targets for CNS disorders: the dopamine D₁-D₃ receptor heteromer

CNS & Neurological Disorders Drug Targets
Sergi FerréRafael Franco

Abstract

A number of G-protein-coupled receptors (GPCRs) are currently under consideration as potential therapeutic targets for drugs acting in the central nervous system (CNS). Attempts to discover new medications have operated under the assumption that GPCRs are monomers and that a specific drug activates one single receptor coupled to one single signal transduction mechanism. In the neuronal membrane, GPCRs are now known to be arranged into homo- and hetero-oligomers; drugs acting on a single receptor within a specific heteromer context are thought to induce a particular downstream signaling. However, there is recent evidence showing that heteromer-tailored drugs can be designed that display different affinities for a given receptor depending on the receptor partners contained within the heteromer. It can therefore be predicted that customized drugs targeting a specific receptor heteromer in the CNS might improve safety and efficacy for their therapeutic targets. Finally, it will be important to identify receptor heteromers that are involved in the pathogenesis of diseases, such as the recently discovered dopamine D₁-D₃ receptor heteromer, which might play a key role in L-DOPA-induced dyskinesia in Parkinson's disease.

Citations

Jun 19, 2013·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Melissa L PerreaultSusan R George
Feb 12, 2014·Pharmacological Reviews·Sergi FerréXavier Guitart
Jun 22, 2012·Expert Opinion on Drug Discovery·Linjie ChenNaiming Zhou
Dec 3, 2014·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Roberto MaggioMark J Millan
Mar 10, 2016·Journal of Neurochemistry·Paul CastellanoEliseo A Eugenin
May 3, 2016·Expert Opinion on Drug Discovery·Antoni CortésVicent Casadó
Jun 28, 2016·Pharmacology & Therapeutics·Gian Marco LeggioFilippo Drago
Feb 9, 2018·Journal of Neural Transmission·Oscar Solís, Rosario Moratalla
Jun 5, 2017·Journal of Neuroimmune Pharmacology : the Official Journal of the Society on NeuroImmune Pharmacology·Monica PinoliMarco Cosentino
Apr 10, 2021·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Desye Misganaw

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