Introduction of GPR17
GPR17 is encoded by the GPR17 gene. It belongs to the G-protein-coupled receptor (GPCR) family which are the most abundant cell surface receptors that can be targeted clinically. And GPRs has become a priority in pharmacogenetic investigations aimed at advancing personalized medicine. GPR17 is phylogenetically associated with the nucleotide (P2Y) and cysteinyl leukotriene receptors. Both cysteinyl leukotriene and uracil nucleotides can activate GPR17 which will inhibit adenylyl cyclase and increase intracellular calcium.
|Basic Information of GPR17|
|Protein Name||Uracil nucleotide/cysteinyl leukotriene receptor|
|Aliases||G-protein coupled receptor 17, P2Y-like receptor, R12|
|Organism||Homo sapiens (Human)|
Function of GPR17 Membrane Protein
It has been proved that GPR17 is the dual specificity receptor for uracil nucleotides and cysteinyl leukotrienes, and once it is speciﬁcally activated by both families of endogenous ligands, it will lead to both adenylyl cyclase inhibition and intracellular calcium increases. At the same time, some ﬁndings suggest that GPR17 is a ligand-independent, constitutive negative regulator for the CysLT1R that suppresses CysLT1R-mediated function at the cell membrane. GPR17 highly expressed in central nervous system (CNS) tissues of animal models undergoing ischemia, experimental autoimmune encephalomyelitis, and focal demyelination as well as in the CNS tissues of humans suffering brain damage made by trauma, multiple sclerosis, and ischemia. Besides, some studies suggested that GPR17 is a sensor of damage in the CNS and participates in the resolution of this damage by clearing and/or promoting the re-myelination of injured neurons due to all kinds of insults maybe including old age.
Fig.1 GPR17 model built by modpipe software (Saravanan, 2017)
Application of GPR17 Membrane Protein in Literature
Authors in the article identify HAMI3379 as an antagonist of the orphan G protein-coupled receptor GPR17. HAMI3379 inhibits signaling of recombinant human, rat, and mouse GPR17 across various cellular backgrounds, and of endogenous GPR17 in primary rodent oligodendrocytes. They propose that HAMI3379 holds promise for pharmacological exploitation of orphan GPR17 to enhance regenerative strategies for the promotion of remyelination in patients.
The study mainly discusses the relationship between GPR17 and Oligodendrocyte differentiation. Being a membrane receptor, GPR17 represents an ideal druggable target to be exploited for innovative regenerative approaches to acute and chronic CNS diseases.
This article reports detailed protein-ligand interactions and the dynamics of GPR17-ligand interaction by molecular docking and molecular dynamics experiments which provided the deep understanding of ligand binding with GPR17.
The article shows that Zhenbao pill increased the level of miR-146a-5p and decreased GPR17 expression in vivo and in vitro, it protects against acute spinal cord injury via miR-146a-5p regulating the expression of GPR17.
This article suggests GPR17 as the common molecular target mediating brain damage by nucleotides and CysLTs. Moreover, the deorphanization of GPR17 displayed a dualistic receptor for two endogenous unrelated ligand families. These findings may result in dualistic drugs of previously unexplored therapeutic potential.
GPR17 Preparation Options
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