Recombinant Human Uracil nucleotide/cysteinyl leukotriene receptor (GPR17)

1. In silico and ex vivo validation experiments provided the deep understanding of ligand binding with GPR17 and the present findings reported here may lead to use these two compounds as a potential activator of GPR17 for therapeutic intervention. PMID:28827203
2. Results show a crucial role of SNX27 in modulating GPR17 levels by means of a post-translational mechanism and highlights the relationship between the trafficking of the receptor through the endomembrane system and oligodendrocyte differentiation; and provide novel evidence of impairment of GPR17 expression and oligodendrocyte maturation in a mouse model of Down syndrome that is characterized by SNX27 down-regulation. PMID:27270750
3. uracil nucleotides and cysteinyl leukotrienes do not activate human, mouse, or rat GPR17 in various cellular backgrounds. PMID:28254957
4. GPR17 gene disruption does not alter food intake or glucose homeostasis in mice. PMID:25624481
5. This review summarizes knowledge about role of GPR17 receptors in physiology and pathology of nervous system, with special attention to remyelination processes. PMID:25807830
6. Low levels of GRK2/GRK5 causes a slow and not complete desensitization/down-regulation of GPR17. PMID:24613411
7. Data indicate that small molecule MDL29,951 activates human, mouse and rat orphan G protein-coupled receptor GPR17. PMID:24150254
8. Data validate GPR17 as a target for neurorepair PMID:23801362
9. Nucleotides, nucleotide sugars, and cysteinyl leukotrienes do not promote activation of GPR17 in five different cell lines, nor does GPR17 have signaling properties. PMID:23908386
10. analysis of agonist-induced trafficking of native GPR17 in oligodendroglial cells PMID:23288840
11. A functional cross-talk exists between cysteinyl-leukotriene and purinergic sites at GPR17; the latter have a hierarchy in producing desensitizing signals. PMID:21531793
12. REVIEW: functional properties and in vivo biology PMID:21261596
13. We present the first isoform-specific characterization of GPR17 and show that differences exist between the isoforms in expression pattern and pharmacological profile; the two human isoforms might serve tissue-specific functions PMID:20148890
14. GPR17, a Gi-coupled orphan receptor at intermediate phylogenetic position between P2Y and CysLT receptors, is specifically activated by both families of endogenous ligands. PMID:16990797
15. Molecular dynamics simulations suggest that GPR17 nucleotide binding pocket is similar to that described for the other P2Y receptors, although only one of the 3 basic residues that have been typically involved in ligand recognition is conserved (Arg255). PMID:18533035
16. long-GPR17 isoform is a functional receptor that is stimulated by both uracil nucleotides and cysteinyl leukotrienes PMID:19625605

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HGNC: 4471

UNIGENE: Hs.46453

KEGG: hsa:2840

STRING: 9606.ENSP00000272644

OMIM: 603071