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Items: 1 to 50 of 264

1.

D1-mGlu5 heteromers mediate noncanonical dopamine signaling in Parkinson's disease.

Sebastianutto I, Goyet E, Andreoli L, Font-Ingles J, Moreno-Delgado D, Bouquier N, Jahannault-Talignani C, Moutin E, Di Menna L, Maslava N, Pin JP, Fagni L, Nicoletti F, Ango F, Cenci MA, Perroy J.

J Clin Invest. 2020 Feb 10. pii: 126361. doi: 10.1172/JCI126361. [Epub ahead of print]

2.

LSP5-2157 a new inhibitor of vesicular glutamate transporters.

Poirel O, Mamer LE, Herman MA, Arnulf-Kempcke M, Kervern M, Potier B, Miot S, Wang J, Favre-Besse FC, Brabet I, Laras Y, Bertrand HO, Acher F, Pin JP, Puel JL, Giros B, Epelbaum J, Rosenmund C, Dutar P, Daumas S, El Mestikawy S, Pietrancosta N.

Neuropharmacology. 2020 Mar 1;164:107902. doi: 10.1016/j.neuropharm.2019.107902. Epub 2019 Dec 4.

PMID:
31811873
3.

Infiltrating Myeloid Cells Drive Osteosarcoma Progression via GRM4 Regulation of IL23.

Kansara M, Thomson K, Pang P, Dutour A, Mirabello L, Acher F, Pin JP, Demicco EG, Yan J, Teng MWL, Smyth MJ, Thomas DM.

Cancer Discov. 2019 Nov;9(11):1511-1519. doi: 10.1158/2159-8290.CD-19-0154. Epub 2019 Sep 16.

PMID:
31527131
4.

Rearrangement of the transmembrane domain interfaces associated with the activation of a GPCR hetero-oligomer.

Xue L, Sun Q, Zhao H, Rovira X, Gai S, He Q, Pin JP, Liu J, Rondard P.

Nat Commun. 2019 Jun 24;10(1):2765. doi: 10.1038/s41467-019-10834-5.

5.

Nonclassical Ligand-Independent Regulation of Go Protein by an Orphan Class C G-Protein-Coupled Receptor.

Hajj M, De Vita T, Vol C, Renassia C, Bologna JC, Brabet I, Cazade M, Pastore M, Blahos J, Labesse G, Pin JP, Prézeau L.

Mol Pharmacol. 2019 Aug;96(2):233-246. doi: 10.1124/mol.118.113019. Epub 2019 Jun 12.

6.

Context-Dependent Signaling of CXC Chemokine Receptor 4 and Atypical Chemokine Receptor 3.

Heuninck J, Perpiñá Viciano C, Işbilir A, Caspar B, Capoferri D, Briddon SJ, Durroux T, Hill SJ, Lohse MJ, Milligan G, Pin JP, Hoffmann C.

Mol Pharmacol. 2019 Dec;96(6):778-793. doi: 10.1124/mol.118.115477. Epub 2019 May 15.

PMID:
31092552
7.

Time-Resolved FRET-Based Assays to Characterize G Protein-Coupled Receptor Hetero-oligomer Pharmacology.

Heuninck J, Hounsou C, Dupuis E, Trinquet E, Mouillac B, Pin JP, Bonnet D, Durroux T.

Methods Mol Biol. 2019;1947:151-168. doi: 10.1007/978-1-4939-9121-1_8.

PMID:
30969415
8.

GPCR interaction as a possible way for allosteric control between receptors.

Pin JP, Kniazeff J, Prézeau L, Liu JF, Rondard P.

Mol Cell Endocrinol. 2019 Apr 15;486:89-95. doi: 10.1016/j.mce.2019.02.019. Epub 2019 Mar 5. Review.

PMID:
30849406
9.

HTRF® Total and Phospho-YAP (Ser127) Cellular Assays.

Zindel D, Vol C, Lecha O, Bequignon I, Bilgic M, Vereecke M, Charrier-Savournin F, Romier M, Trinquet E, Pin JP, Pannequin J, Roux T, Dupuis E, Prézeau L.

Methods Mol Biol. 2019;1893:153-166. doi: 10.1007/978-1-4939-8910-2_13.

10.

Chloride ions stabilize the glutamate-induced active state of the metabotropic glutamate receptor 3.

Tora AS, Rovira X, Cao AM, Cabayé A, Olofsson L, Malhaire F, Scholler P, Baik H, Van Eeckhaut A, Smolders I, Rondard P, Margeat E, Acher F, Pin JP, Goudet C.

Neuropharmacology. 2018 Sep 15;140:275-286. doi: 10.1016/j.neuropharm.2018.08.011. Epub 2018 Aug 11.

PMID:
30102917
11.

Profiling of orthosteric and allosteric group-III metabotropic glutamate receptor ligands on various G protein-coupled receptors with Tag-lite® assays.

Belhocine A, Veglianese P, Hounsou C, Dupuis E, Acher F, Durroux T, Goudet C, Pin JP.

Neuropharmacology. 2018 Sep 15;140:233-245. doi: 10.1016/j.neuropharm.2018.07.032. Epub 2018 Aug 9.

PMID:
30099051
12.

Oligomerization of a G protein-coupled receptor in neurons controlled by its structural dynamics.

Møller TC, Hottin J, Clerté C, Zwier JM, Durroux T, Rondard P, Prézeau L, Royer CA, Pin JP, Margeat E, Kniazeff J.

Sci Rep. 2018 Jul 10;8(1):10414. doi: 10.1038/s41598-018-28682-6.

13.

Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs.

Nasrallah C, Rottier K, Marcellin R, Compan V, Font J, Llebaria A, Pin JP, Banères JL, Lebon G.

Sci Rep. 2018 Mar 13;8(1):4407. doi: 10.1038/s41598-018-22729-4.

14.

Inhibition of neuronal FLT3 receptor tyrosine kinase alleviates peripheral neuropathic pain in mice.

Rivat C, Sar C, Mechaly I, Leyris JP, Diouloufet L, Sonrier C, Philipson Y, Lucas O, Mallié S, Jouvenel A, Tassou A, Haton H, Venteo S, Pin JP, Trinquet E, Charrier-Savournin F, Mezghrani A, Joly W, Mion J, Schmitt M, Pattyn A, Marmigère F, Sokoloff P, Carroll P, Rognan D, Valmier J.

Nat Commun. 2018 Mar 12;9(1):1042. doi: 10.1038/s41467-018-03496-2.

15.

Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.

Selvam C, Lemasson IA, Brabet I, Oueslati N, Karaman B, Cabaye A, Tora AS, Commare B, Courtiol T, Cesarini S, McCort-Tranchepain I, Rigault D, Mony L, Bessiron T, McLean H, Leroux FR, Colobert F, Daniel H, Goupil-Lamy A, Bertrand HO, Goudet C, Pin JP, Acher FC.

J Med Chem. 2018 Mar 8;61(5):1969-1989. doi: 10.1021/acs.jmedchem.7b01438. Epub 2018 Feb 14.

PMID:
29397723
16.

Correction: Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator.

Font J, López-Cano M, Notartomaso S, Scarselli P, Di Prieto P, Bresolí-Obach R, Battaglia G, Malhaire F, Rovira X, Catena J, Giraldo J, Pin JP, Fernández-Dueñas V, Goudet C, Nonell S, Nicoletti F, Llebaria A, Ciruela F.

Elife. 2018 Jan 8;7. pii: e34752. doi: 10.7554/eLife.34752. No abstract available.

17.

Allosteric interactions between GABAB1 subunits control orthosteric binding sites occupancy within GABAB oligomers.

Stewart GD, Comps-Agrar L, Nørskov-Lauritsen LB, Pin JP, Kniazeff J.

Neuropharmacology. 2018 Jul 1;136(Pt A):92-101. doi: 10.1016/j.neuropharm.2017.12.042. Epub 2018 Jan 2.

18.

Class C G protein-coupled receptors: reviving old couples with new partners.

Møller TC, Moreno-Delgado D, Pin JP, Kniazeff J.

Biophys Rep. 2017;3(4):57-63. doi: 10.1007/s41048-017-0036-9. Epub 2017 Feb 28.

19.

From the Promiscuous Asenapine to Potent Fluorescent Ligands Acting at a Series of Aminergic G-Protein-Coupled Receptors.

Hounsou C, Baehr C, Gasparik V, Alili D, Belhocine A, Rodriguez T, Dupuis E, Roux T, Mann A, Heissler D, Pin JP, Durroux T, Bonnet D, Hibert M.

J Med Chem. 2018 Jan 11;61(1):174-188. doi: 10.1021/acs.jmedchem.7b01220. Epub 2017 Dec 22.

PMID:
29219316
20.

Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation.

Scholler P, Nevoltris D, de Bundel D, Bossi S, Moreno-Delgado D, Rovira X, Møller TC, El Moustaine D, Mathieu M, Blanc E, McLean H, Dupuis E, Mathis G, Trinquet E, Daniel H, Valjent E, Baty D, Chames P, Rondard P, Pin JP.

Nat Commun. 2017 Dec 6;8(1):1967. doi: 10.1038/s41467-017-01489-1.

21.

Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer.

Liu J, Zhang Z, Moreno-Delgado D, Dalton JA, Rovira X, Trapero A, Goudet C, Llebaria A, Giraldo J, Yuan Q, Rondard P, Huang S, Liu J, Pin JP.

Elife. 2017 Aug 10;6. pii: e26985. doi: 10.7554/eLife.26985.

22.

RgIA4 Potently Blocks Mouse α9α10 nAChRs and Provides Long Lasting Protection against Oxaliplatin-Induced Cold Allodynia.

Christensen SB, Hone AJ, Roux I, Kniazeff J, Pin JP, Upert G, Servent D, Glowatzki E, McIntosh JM.

Front Cell Neurosci. 2017 Jul 21;11:219. doi: 10.3389/fncel.2017.00219. eCollection 2017.

23.

Analysis of positive and negative allosteric modulation in metabotropic glutamate receptors 4 and 5 with a dual ligand.

Dalton JAR, Pin JP, Giraldo J.

Sci Rep. 2017 Jul 10;7(1):4944. doi: 10.1038/s41598-017-05095-5.

24.

Pharmacological evidence for a metabotropic glutamate receptor heterodimer in neuronal cells.

Moreno Delgado D, Møller TC, Ster J, Giraldo J, Maurel D, Rovira X, Scholler P, Zwier JM, Perroy J, Durroux T, Trinquet E, Prezeau L, Rondard P, Pin JP.

Elife. 2017 Jun 29;6. pii: e25233. doi: 10.7554/eLife.25233.

25.

Antibodies targeting G protein-coupled receptors: Recent advances and therapeutic challenges.

Ayoub MA, Crépieux P, Koglin M, Parmentier M, Pin JP, Poupon A, Reiter E, Smit M, Steyaert J, Watier H, Wilkinson T.

MAbs. 2017 Jul;9(5):735-741. doi: 10.1080/19420862.2017.1325052. Epub 2017 May 5.

26.

Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator.

Font J, López-Cano M, Notartomaso S, Scarselli P, Di Pietro P, Bresolí-Obach R, Battaglia G, Malhaire F, Rovira X, Catena J, Giraldo J, Pin JP, Fernández-Dueñas V, Goudet C, Nonell S, Nicoletti F, Llebaria A, Ciruela F.

Elife. 2017 Apr 11;6. pii: e23545. doi: 10.7554/eLife.23545. Erratum in: Elife. 2018 Jan 08;7:.

27.

FRET-Based Sensors Unravel Activation and Allosteric Modulation of the GABAB Receptor.

Lecat-Guillet N, Monnier C, Rovira X, Kniazeff J, Lamarque L, Zwier JM, Trinquet E, Pin JP, Rondard P.

Cell Chem Biol. 2017 Mar 16;24(3):360-370. doi: 10.1016/j.chembiol.2017.02.011. Epub 2017 Mar 9.

28.

Illuminating Phenylazopyridines To Photoswitch Metabotropic Glutamate Receptors: From the Flask to the Animals.

Gómez-Santacana X, Pittolo S, Rovira X, Lopez M, Zussy C, Dalton JA, Faucherre A, Jopling C, Pin JP, Ciruela F, Goudet C, Giraldo J, Gorostiza P, Llebaria A.

ACS Cent Sci. 2017 Jan 25;3(1):81-91. doi: 10.1021/acscentsci.6b00353. Epub 2016 Dec 19.

29.

HTS-compatible FRET-based conformational sensors clarify membrane receptor activation.

Scholler P, Moreno-Delgado D, Lecat-Guillet N, Doumazane E, Monnier C, Charrier-Savournin F, Fabre L, Chouvet C, Soldevila S, Lamarque L, Donsimoni G, Roux T, Zwier JM, Trinquet E, Rondard P, Pin JP.

Nat Chem Biol. 2017 Apr;13(4):372-380. doi: 10.1038/nchembio.2286. Epub 2017 Jan 30.

PMID:
28135236
30.

Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu5 negative allosteric modulation.

Gómez-Santacana X, Dalton JAR, Rovira X, Pin JP, Goudet C, Gorostiza P, Giraldo J, Llebaria A.

Eur J Med Chem. 2017 Feb 15;127:567-576. doi: 10.1016/j.ejmech.2017.01.013. Epub 2017 Jan 12.

PMID:
28109949
31.

Dynamic modulation of inflammatory pain-related affective and sensory symptoms by optical control of amygdala metabotropic glutamate receptor 4.

Zussy C, Gómez-Santacana X, Rovira X, De Bundel D, Ferrazzo S, Bosch D, Asede D, Malhaire F, Acher F, Giraldo J, Valjent E, Ehrlich I, Ferraguti F, Pin JP, Llebaria A, Goudet C.

Mol Psychiatry. 2018 Mar;23(3):509-520. doi: 10.1038/mp.2016.223. Epub 2016 Dec 20.

PMID:
27994221
32.

Organization and functions of mGlu and GABAB receptor complexes.

Pin JP, Bettler B.

Nature. 2016 Dec 1;540(7631):60-68. doi: 10.1038/nature20566. Review.

PMID:
27905440
33.

Identification of key phosphorylation sites in PTH1R that determine arrestin3 binding and fine-tune receptor signaling.

Zindel D, Engel S, Bottrill AR, Pin JP, Prézeau L, Tobin AB, Bünemann M, Krasel C, Butcher AJ.

Biochem J. 2016 Nov 15;473(22):4173-4192. Epub 2016 Sep 13.

34.

OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity.

Rovira X, Trapero A, Pittolo S, Zussy C, Faucherre A, Jopling C, Giraldo J, Pin JP, Gorostiza P, Goudet C, Llebaria A.

Cell Chem Biol. 2016 Aug 18;23(8):929-34. doi: 10.1016/j.chembiol.2016.06.013. Epub 2016 Jul 28.

35.

New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III.

Huynh TH, Erichsen MN, Tora AS, Goudet C, Sagot E, Assaf Z, Thomsen C, Brodbeck R, Stensbøl TB, Bjørn-Yoshimoto WE, Nielsen B, Pin JP, Gefflaut T, Bunch L.

J Med Chem. 2016 Feb 11;59(3):914-24. doi: 10.1021/acs.jmedchem.5b01333. Epub 2016 Jan 27.

PMID:
26814576
36.

A negative allosteric modulator modulates GABAB-receptor signalling through GB2 subunits.

Sun B, Chen L, Liu L, Xia Z, Pin JP, Nan F, Liu J.

Biochem J. 2016 Mar 15;473(6):779-87. doi: 10.1042/BJ20150979. Epub 2016 Jan 15.

PMID:
26772870
37.

Shining Light on an mGlu5 Photoswitchable NAM: A Theoretical Perspective.

Dalton JA, Lans I, Rovira X, Malhaire F, Gómez-Santacana X, Pittolo S, Gorostiza P, Llebaria A, Goudet C, Pin JP, Giraldo J.

Curr Neuropharmacol. 2016;14(5):441-54.

38.

G Protein-Coupled Receptor Multimers: A Question Still Open Despite the Use of Novel Approaches.

Vischer HF, Castro M, Pin JP.

Mol Pharmacol. 2015 Sep;88(3):561-71. doi: 10.1124/mol.115.099440. Epub 2015 Jul 2. Review.

PMID:
26138074
39.

Allosteric modulation of metabotropic glutamate receptors by chloride ions.

Tora AS, Rovira X, Dione I, Bertrand HO, Brabet I, De Koninck Y, Doyon N, Pin JP, Acher F, Goudet C.

FASEB J. 2015 Oct;29(10):4174-88. doi: 10.1096/fj.14-269746. Epub 2015 Jun 26.

PMID:
26116702
40.

GABAB receptor promotes its own surface expression by recruiting a Rap1-dependent signaling cascade.

Zhang Z, Zhang W, Huang S, Sun Q, Wang Y, Hu Y, Sun N, Zhang Y, Jiang Z, Minato N, Pin JP, Su L, Liu J.

J Cell Sci. 2015 Jun 15;128(12):2302-13. doi: 10.1242/jcs.167056. Epub 2015 May 12.

41.

Synthesis and studies on the mGluR agonist activity of FAP4 stereoisomers.

Ivashkin P, Lemonnier G, Tora AS, Pin JP, Goudet C, Jubault P, Pannecoucke X.

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2523-6. doi: 10.1016/j.bmcl.2015.04.043. Epub 2015 Apr 22.

PMID:
25958247
42.

Multicolor time-resolved Förster resonance energy transfer microscopy reveals the impact of GPCR oligomerization on internalization processes.

Faklaris O, Cottet M, Falco A, Villier B, Laget M, Zwier JM, Trinquet E, Mouillac B, Pin JP, Durroux T.

FASEB J. 2015 Jun;29(6):2235-46. doi: 10.1096/fj.14-260059. Epub 2015 Feb 17.

PMID:
25690655
43.

Editorial overview: neurosciences: targeting glutamatergic signaling in CNS diseases: new hopes?

Paoletti P, Pin JP.

Curr Opin Pharmacol. 2015 Feb;20:iv-vi. doi: 10.1016/j.coph.2015.01.001. Epub 2015 Jan 15. No abstract available.

PMID:
25601440
44.

Time-resolved FRET strategy to screen GPCR ligand library.

Oueslati N, Hounsou C, Belhocine A, Rodriguez T, Dupuis E, Zwier JM, Trinquet E, Pin JP, Durroux T.

Methods Mol Biol. 2015;1272:23-36. doi: 10.1007/978-1-4939-2336-6_2.

PMID:
25563174
45.

Generic GPCR residue numbers - aligning topology maps while minding the gaps.

Isberg V, de Graaf C, Bortolato A, Cherezov V, Katritch V, Marshall FH, Mordalski S, Pin JP, Stevens RC, Vriend G, Gloriam DE.

Trends Pharmacol Sci. 2015 Jan;36(1):22-31. doi: 10.1016/j.tips.2014.11.001. Epub 2014 Dec 22. Review.

46.

Dynamics and modulation of metabotropic glutamate receptors.

Rondard P, Pin JP.

Curr Opin Pharmacol. 2015 Feb;20:95-101. doi: 10.1016/j.coph.2014.12.001. Epub 2014 Dec 17. Review.

PMID:
25529199
47.

Major ligand-induced rearrangement of the heptahelical domain interface in a GPCR dimer.

Xue L, Rovira X, Scholler P, Zhao H, Liu J, Pin JP, Rondard P.

Nat Chem Biol. 2015 Feb;11(2):134-40. doi: 10.1038/nchembio.1711. Epub 2014 Dec 15.

PMID:
25503927
48.

Determination of the absolute configuration of phosphinic analogues of glutamate.

Commare B, Rigault D, Lemasson IA, Deschamps P, Tomas A, Roussel P, Brabet I, Goudet C, Pin JP, Leroux FR, Colobert F, Acher FC.

Org Biomol Chem. 2015 Jan 28;13(4):1106-12. doi: 10.1039/c4ob01960a. Epub 2014 Nov 24.

PMID:
25417857
49.

Untangling dopamine-adenosine receptor-receptor assembly in experimental parkinsonism in rats.

Fernández-Dueñas V, Taura JJ, Cottet M, Gómez-Soler M, López-Cano M, Ledent C, Watanabe M, Trinquet E, Pin JP, Luján R, Durroux T, Ciruela F.

Dis Model Mech. 2015 Jan;8(1):57-63. doi: 10.1242/dmm.018143. Epub 2014 Nov 14.

50.

Time-resolved FRET binding assay to investigate hetero-oligomer binding properties: proof of concept with dopamine D1/D3 heterodimer.

Hounsou C, Margathe JF, Oueslati N, Belhocine A, Dupuis E, Thomas C, Mann A, Ilien B, Rognan D, Trinquet E, Hibert M, Pin JP, Bonnet D, Durroux T.

ACS Chem Biol. 2015 Feb 20;10(2):466-74. doi: 10.1021/cb5007568. Epub 2014 Nov 11.

PMID:
25350273

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