4.5 Article

Evidence for the Existence of a Specific G Protein-Coupled Receptor Activated by Guanosine

Journal

CHEMMEDCHEM
Volume 6, Issue 6, Pages 1074-1080

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201100100

Keywords

Eu-GTP; GPCR; guanosine; nucleosides; receptors

Funding

  1. Italian Ministry for University and Research
  2. Ministry for Health [RF-CNM-2007-662855]

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Guanosine, released extracellularly from neurons and glial cells, plays important roles in the central nervous system, including neuroprotection. The innovative DELFIA Eu-GTP binding assay was optimized for characterization of the putative guanosine receptor binding site at rat brain membranes by using a series of novel and known guanosine derivatives. These nucleosides were prepared by modifying the purine and sugar moieties of guanosine at the 6- and 5'-positions, respectively. Results of these experiments prove that guanosine, 6-thioguanosine, and their derivatives activate a G protein-coupled receptor that is different from the well-characterized adenosine receptors.

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