Journal
CHEMMEDCHEM
Volume 6, Issue 6, Pages 1074-1080Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201100100
Keywords
Eu-GTP; GPCR; guanosine; nucleosides; receptors
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Funding
- Italian Ministry for University and Research
- 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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