Brain expression and 3H-Guanosine binding analysis of novel G protein-coupled receptor for guanosine (GPR23/LPA4)

Several studies have shown that guanine-based purines exert biological effects on the central nervous system, possibly through membrane receptor. In a parallel work, we have identified the first guanosine G protein-coupled receptor GPR23, known as LPA4 receptor, involved in the modulation of guanosine-mediated antiproliferative effects in human glioma cell lines. Here, we performed in different brain areas the following studies: by PCR, the expression levels of GPR23; by [3H]-Guanosine radioligand binding assay, the binding properties of GPR23; by [35S] GTPγS binding assay, the receptor activation properties of guanosine. Among the examined areas, the cerebral cortex showed the highest GPR2…

Identification of GPR23/LPA4 as a candidate G protein-coupled receptor for Guanosine

Identification and functional binding analysis of GPR23/! LPA4 as a candidate G protein-coupled receptor for Guanosine.

Several studies have shown that guanine-based purines exert biological effects on the central nervous system (CNS), possibly through membrane receptors, but at the present there are not reports related to the identification of such specific receptor(s). We have identified the first guanosine G protein-coupled receptor GPR23, also known as LPA4 receptor, involved in the modulation of guanosine-mediated antiproliferative effects in human glioma cell line (U87). We report that the silencing of GPR23 reduces significantly the antiproliferative effects of guanosine, while stably transfected cell clones over-expressing GPR23 increase sensitivity to guanosine. [3H] Guanosine radioligand binding as…

ANTIPROLIFERATIVE EFFECTS OF GUANINE-BASED PURINES AND IDENTIFICATION OF A CANDIDATE RECEPTOR