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Repurposing HAMI3379 to Block GPR17 and Promote Rodent and Human Oligodendrocyte Differentiation.

Merten N, Fischer J, Simon K, Zhang L, Schröder R, Peters L, Letombe AG, Hennen S, Schrage R, Bödefeld T, Vermeiren C, Gillard M, Mohr K, Lu QR, Brüstle O, Gomeza J, Kostenis E.

Cell Chem Biol. 2018 Jun 21;25(6):775-786.e5. doi: 10.1016/j.chembiol.2018.03.012. Epub 2018 Apr 26.


The Orphan G Protein-coupled Receptor GPR17 Negatively Regulates Oligodendrocyte Differentiation via Gαi/o and Its Downstream Effector Molecules.

Simon K, Hennen S, Merten N, Blättermann S, Gillard M, Kostenis E, Gomeza J.

J Biol Chem. 2016 Jan 8;291(2):705-18. doi: 10.1074/jbc.M115.683953. Epub 2015 Nov 30.


Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist.

Hennen S, Wang H, Peters L, Merten N, Simon K, Spinrath A, Blättermann S, Akkari R, Schrage R, Schröder R, Schulz D, Vermeiren C, Zimmermann K, Kehraus S, Drewke C, Pfeifer A, König GM, Mohr K, Gillard M, Müller CE, Lu QR, Gomeza J, Kostenis E.

Sci Signal. 2013 Oct 22;6(298):ra93. doi: 10.1126/scisignal.2004350.


Olig2-Targeted G-Protein-Coupled Receptor Gpr17 Regulates Oligodendrocyte Survival in Response to Lysolecithin-Induced Demyelination.

Ou Z, Sun Y, Lin L, You N, Liu X, Li H, Ma Y, Cao L, Han Y, Liu M, Deng Y, Yao L, Lu QR, Chen Y.

J Neurosci. 2016 Oct 12;36(41):10560-10573.


Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.

Wunder F, Tinel H, Kast R, Geerts A, Becker EM, Kolkhof P, Hütter J, Ergüden J, Härter M.

Br J Pharmacol. 2010 May;160(2):399-409. doi: 10.1111/j.1476-5381.2010.00730.x.


UDP-glucose enhances outward K(+) currents necessary for cell differentiation and stimulates cell migration by activating the GPR17 receptor in oligodendrocyte precursors.

Coppi E, Maraula G, Fumagalli M, Failli P, Cellai L, Bonfanti E, Mazzoni L, Coppini R, Abbracchio MP, Pedata F, Pugliese AM.

Glia. 2013 Jul;61(7):1155-71. doi: 10.1002/glia.22506. Epub 2013 May 2.


The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repair.

Lecca D, Trincavelli ML, Gelosa P, Sironi L, Ciana P, Fumagalli M, Villa G, Verderio C, Grumelli C, Guerrini U, Tremoli E, Rosa P, Cuboni S, Martini C, Buffo A, Cimino M, Abbracchio MP.

PLoS One. 2008;3(10):e3579. doi: 10.1371/journal.pone.0003579. Epub 2008 Oct 31.


The oligodendrocyte-specific G protein-coupled receptor GPR17 is a cell-intrinsic timer of myelination.

Chen Y, Wu H, Wang S, Koito H, Li J, Ye F, Hoang J, Escobar SS, Gow A, Arnett HA, Trapp BD, Karandikar NJ, Hsieh J, Lu QR.

Nat Neurosci. 2009 Nov;12(11):1398-406. doi: 10.1038/nn.2410. Epub 2009 Oct 18.


Phenotypic changes, signaling pathway, and functional correlates of GPR17-expressing neural precursor cells during oligodendrocyte differentiation.

Fumagalli M, Daniele S, Lecca D, Lee PR, Parravicini C, Fields RD, Rosa P, Antonucci F, Verderio C, Trincavelli ML, Bramanti P, Martini C, Abbracchio MP.

J Biol Chem. 2011 Mar 25;286(12):10593-604. doi: 10.1074/jbc.M110.162867. Epub 2011 Jan 5.


Enigmatic GPCR finds a stimulating drug.

Harden TK.

Sci Signal. 2013 Oct 22;6(298):pe34. doi: 10.1126/scisignal.2004755.


The P2Y-like receptor GPR17 as a sensor of damage and a new potential target in spinal cord injury.

Ceruti S, Villa G, Genovese T, Mazzon E, Longhi R, Rosa P, Bramanti P, Cuzzocrea S, Abbracchio MP.

Brain. 2009 Aug;132(Pt 8):2206-18. doi: 10.1093/brain/awp147. Epub 2009 Jun 15.


Differential local tissue permissiveness influences the final fate of GPR17-expressing oligodendrocyte precursors in two distinct models of demyelination.

Coppolino GT, Marangon D, Negri C, Menichetti G, Fumagalli M, Gelosa P, Dimou L, Furlan R, Lecca D, Abbracchio MP.

Glia. 2018 May;66(5):1118-1130. doi: 10.1002/glia.23305. Epub 2018 Feb 9.


A new role for the P2Y-like GPR17 receptor in the modulation of multipotency of oligodendrocyte precursor cells in vitro.

Boccazzi M, Lecca D, Marangon D, Guagnini F, Abbracchio MP, Ceruti S.

Purinergic Signal. 2016 Dec;12(4):661-672. Epub 2016 Aug 20.


SNX27, a protein involved in down syndrome, regulates GPR17 trafficking and oligodendrocyte differentiation.

Meraviglia V, Ulivi AF, Boccazzi M, Valenza F, Fratangeli A, Passafaro M, Lecca D, Stagni F, Giacomini A, Bartesaghi R, Abbracchio MP, Ceruti S, Rosa P.

Glia. 2016 Aug;64(8):1437-60. doi: 10.1002/glia.23015. Epub 2016 Jun 6.


The ubiquitin ligase Mdm2 controls oligodendrocyte maturation by intertwining mTOR with G protein-coupled receptor kinase 2 in the regulation of GPR17 receptor desensitization.

Fumagalli M, Bonfanti E, Daniele S, Zappelli E, Lecca D, Martini C, Trincavelli ML, Abbracchio MP.

Glia. 2015 Dec;63(12):2327-39. doi: 10.1002/glia.22896. Epub 2015 Jul 31.


Pharmacological Properties and Biological Functions of the GPR17 Receptor, a Potential Target for Neuro-Regenerative Medicine.

Fumagalli M, Lecca D, Coppolino GT, Parravicini C, Abbracchio MP.

Adv Exp Med Biol. 2017;1051:169-192. doi: 10.1007/5584_2017_92. Review.


The G Protein-Coupled Receptor GPR17: Overview and Update.

Marucci G, Dal Ben D, Lambertucci C, Santinelli C, Spinaci A, Thomas A, Volpini R, Buccioni M.

ChemMedChem. 2016 Dec 6;11(23):2567-2574. doi: 10.1002/cmdc.201600453. Epub 2016 Nov 14. Review.


The regulated expression, intracellular trafficking, and membrane recycling of the P2Y-like receptor GPR17 in Oli-neu oligodendroglial cells.

Fratangeli A, Parmigiani E, Fumagalli M, Lecca D, Benfante R, Passafaro M, Buffo A, Abbracchio MP, Rosa P.

J Biol Chem. 2013 Feb 15;288(7):5241-56. doi: 10.1074/jbc.M112.404996. Epub 2013 Jan 3.


Does GRK-β arrestin machinery work as a "switch on" for GPR17-mediated activation of intracellular signaling pathways?

Daniele S, Trincavelli ML, Fumagalli M, Zappelli E, Lecca D, Bonfanti E, Campiglia P, Abbracchio MP, Martini C.

Cell Signal. 2014 Jun;26(6):1310-25. doi: 10.1016/j.cellsig.2014.02.016. Epub 2014 Mar 5.


Expression of the new P2Y-like receptor GPR17 during oligodendrocyte precursor cell maturation regulates sensitivity to ATP-induced death.

Ceruti S, Viganò F, Boda E, Ferrario S, Magni G, Boccazzi M, Rosa P, Buffo A, Abbracchio MP.

Glia. 2011 Mar;59(3):363-78. doi: 10.1002/glia.21107. Epub 2010 Dec 1.

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