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CNS & Neurological Disorders - Drug Targets (Formerly Current Drug Targets - CNS & Neurological Disorders)

Volume 9 Issue 5
ISSN: 1871-5273
eISSN: 1996-3181

 

   All Titles

  Prime Time for G-Protein-Coupled Receptor Heteromers as Therapeutic Targets for CNS disorders: The Dopamine D1-D3 Receptor Heteromer
  pp.596-600 (5) Authors: Sergi Ferre, Carmen Lluis, Jose Luis Lanciego, Rafael 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 heteromertailored 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 imporove 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.

 
  Keywords: G-protein-coupled receptors, CNS, homo and hetero-oligomers, heteromer-tailored drugs, dopamine D1-D3 receptor heteromer, Parkinson's disease
  Affiliation: National Institute on Drug Abuse, IRP, NIH, DHHS, 251 Bayview Blvd, Baltimore, MD 21224, USA.
 
  Key: New Content Free Content Open Access Plus Subscribed Content

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