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Items: 1 to 50 of 59

1.

The pharmacologic characterization of allosteric molecules: Gq protein activation.

Bdioui S, Verdi J, Pierre N, Trinquet E, Roux T, Kenakin T.

J Recept Signal Transduct Res. 2019 Apr;39(2):106-113. doi: 10.1080/10799893.2019.1634101. Epub 2019 Jul 19.

PMID:
31322035
2.

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
3.

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.

PMID:
30565133
4.

Gain of affinity for VEGF165 binding within the VEGFR2/NRP1 cellular complex detected by an HTRF-based binding assay.

Auriau J, Roujeau C, Belaid Choucair Z, Oishi A, Derviaux C, Roux T, Trinquet E, Hermine O, Jockers R, Dam J.

Biochem Pharmacol. 2018 Dec;158:45-59. doi: 10.1016/j.bcp.2018.09.014. Epub 2018 Sep 17.

PMID:
30236477
5.

Equilibrium Assays Are Required to Accurately Characterize the Activity Profiles of Drugs Modulating Gq-Protein-Coupled Receptors.

Bdioui S, Verdi J, Pierre N, Trinquet E, Roux T, Kenakin T.

Mol Pharmacol. 2018 Sep;94(3):992-1006. doi: 10.1124/mol.118.112573. Epub 2018 Jun 28.

PMID:
29954837
6.

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.

7.

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.

8.

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.

9.

A Time-Resolved FRET Cell-Based Binding Assay for the Apelin Receptor.

Valencia C, Dujet C, Margathe JF, Iturrioz X, Roux T, Trinquet E, Villa P, Hibert M, Dupuis E, Llorens-Cortes C, Bonnet D.

ChemMedChem. 2017 Jun 21;12(12):925-931. doi: 10.1002/cmdc.201700106. Epub 2017 Apr 20.

PMID:
28374567
10.

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.

11.

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
12.

Protein-Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery.

Milhas S, Raux B, Betzi S, Derviaux C, Roche P, Restouin A, Basse MJ, Rebuffet E, Lugari A, Badol M, Kashyap R, Lissitzky JC, Eydoux C, Hamon V, Gourdel ME, Combes S, Zimmermann P, Aurrand-Lions M, Roux T, Rogers C, Müller S, Knapp S, Trinquet E, Collette Y, Guillemot JC, Morelli X.

ACS Chem Biol. 2016 Aug 19;11(8):2140-8. doi: 10.1021/acschembio.6b00286. Epub 2016 Jun 3.

PMID:
27219844
13.

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.

Raux B, Voitovich Y, Derviaux C, Lugari A, Rebuffet E, Milhas S, Priet S, Roux T, Trinquet E, Guillemot JC, Knapp S, Brunel JM, Fedorov AY, Collette Y, Roche P, Betzi S, Combes S, Morelli X.

J Med Chem. 2016 Feb 25;59(4):1634-41. doi: 10.1021/acs.jmedchem.5b01708. Epub 2016 Jan 6.

PMID:
26735842
14.

A Broad G Protein-Coupled Receptor Internalization Assay that Combines SNAP-Tag Labeling, Diffusion-Enhanced Resonance Energy Transfer, and a Highly Emissive Terbium Cryptate.

Levoye A, Zwier JM, Jaracz-Ros A, Klipfel L, Cottet M, Maurel D, Bdioui S, Balabanian K, Prézeau L, Trinquet E, Durroux T, Bachelerie F.

Front Endocrinol (Lausanne). 2015 Nov 9;6:167. doi: 10.3389/fendo.2015.00167. eCollection 2015.

15.

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
16.

Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor:Gq complex.

Damian M, Mary S, Maingot M, M'Kadmi C, Gagne D, Leyris JP, Denoyelle S, Gaibelet G, Gavara L, Garcia de Souza Costa M, Perahia D, Trinquet E, Mouillac B, Galandrin S, Galès C, Fehrentz JA, Floquet N, Martinez J, Marie J, Banères JL.

Proc Natl Acad Sci U S A. 2015 Feb 3;112(5):1601-6. doi: 10.1073/pnas.1414618112. Epub 2015 Jan 20.

17.

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
18.

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.

19.

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
20.

Homogeneous time-resolved fluorescence-based assay to monitor extracellular signal-regulated kinase signaling in a high-throughput format.

Ayoub MA, Trebaux J, Vallaghe J, Charrier-Savournin F, Al-Hosaini K, Gonzalez Moya A, Pin JP, Pfleger KD, Trinquet E.

Front Endocrinol (Lausanne). 2014 Jun 23;5:94. doi: 10.3389/fendo.2014.00094. eCollection 2014.

21.

Hypothalamic tanycytes are an ERK-gated conduit for leptin into the brain.

Balland E, Dam J, Langlet F, Caron E, Steculorum S, Messina A, Rasika S, Falluel-Morel A, Anouar Y, Dehouck B, Trinquet E, Jockers R, Bouret SG, Prévot V.

Cell Metab. 2014 Feb 4;19(2):293-301. doi: 10.1016/j.cmet.2013.12.015.

22.

A single glycine in extracellular loop 1 is the critical determinant for pharmacological specificity of dopamine D2 and D3 receptors.

Michino M, Donthamsetti P, Beuming T, Banala A, Duan L, Roux T, Han Y, Trinquet E, Newman AH, Javitch JA, Shi L.

Mol Pharmacol. 2013 Dec;84(6):854-64. doi: 10.1124/mol.113.087833. Epub 2013 Sep 23.

23.

Time-resolved fluorescence ligand binding for G protein-coupled receptors.

Emami-Nemini A, Roux T, Leblay M, Bourrier E, Lamarque L, Trinquet E, Lohse MJ.

Nat Protoc. 2013;8(7):1307-20. doi: 10.1038/nprot.2013.073. Epub 2013 Jun 13.

PMID:
23764938
24.

Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors.

Doumazane E, Scholler P, Fabre L, Zwier JM, Trinquet E, Pin JP, Rondard P.

Proc Natl Acad Sci U S A. 2013 Apr 9;110(15):E1416-25. doi: 10.1073/pnas.1215615110. Epub 2013 Mar 4.

25.

Fluorescent ligands to investigate GPCR binding properties and oligomerization.

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

Biochem Soc Trans. 2013 Feb 1;41(1):148-53. doi: 10.1042/BST20120237.

PMID:
23356275
26.

Design and validation of a homogeneous time-resolved fluorescence-based leptin receptor binding assay.

Vauthier V, Derviaux C, Douayry N, Roux T, Trinquet E, Jockers R, Dam J.

Anal Biochem. 2013 May 1;436(1):1-9. doi: 10.1016/j.ab.2012.12.013. Epub 2013 Jan 17.

PMID:
23333588
27.

Rapid sensing of circulating ghrelin by hypothalamic appetite-modifying neurons.

Schaeffer M, Langlet F, Lafont C, Molino F, Hodson DJ, Roux T, Lamarque L, Verdié P, Bourrier E, Dehouck B, Banères JL, Martinez J, Méry PF, Marie J, Trinquet E, Fehrentz JA, Prévot V, Mollard P.

Proc Natl Acad Sci U S A. 2013 Jan 22;110(4):1512-7. doi: 10.1073/pnas.1212137110. Epub 2013 Jan 7.

28.

Time-resolved Förster resonance energy transfer-based technologies to investigate G protein-coupled receptor machinery: high-throughput screening assays and future development.

Scholler P, Zwier JM, Trinquet E, Rondard P, Pin JP, Prézeau L, Kniazeff J.

Prog Mol Biol Transl Sci. 2013;113:275-312. doi: 10.1016/B978-0-12-386932-6.00007-7. Review.

PMID:
23244793
29.

Selective fluorescent nonpeptidic antagonists for vasopressin V₂ GPCR: application to ligand screening and oligomerization assays.

Loison S, Cottet M, Orcel H, Adihou H, Rahmeh R, Lamarque L, Trinquet E, Kellenberger E, Hibert M, Durroux T, Mouillac B, Bonnet D.

J Med Chem. 2012 Oct 25;55(20):8588-602. doi: 10.1021/jm3006146. Epub 2012 Oct 5.

PMID:
22984902
30.

BRET and Time-resolved FRET strategy to study GPCR oligomerization: from cell lines toward native tissues.

Cottet M, Faklaris O, Maurel D, Scholler P, Doumazane E, Trinquet E, Pin JP, Durroux T.

Front Endocrinol (Lausanne). 2012 Jul 23;3:92. doi: 10.3389/fendo.2012.00092. eCollection 2012.

31.

Monitoring Gq-coupled receptor response through inositol phosphate quantification with the IP-One assay.

Trinquet E, Bouhelal R, Dietz M.

Expert Opin Drug Discov. 2011 Oct;6(10):981-94. doi: 10.1517/17460441.2011.608658. Epub 2011 Sep 8.

PMID:
22646860
32.

Stability of GABAB receptor oligomers revealed by dual TR-FRET and drug-induced cell surface targeting.

Comps-Agrar L, Kniazeff J, Brock C, Trinquet E, Pin JP.

FASEB J. 2012 Aug;26(8):3430-9. doi: 10.1096/fj.12-203646. Epub 2012 May 21.

PMID:
22613777
33.

Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy.

Rahmeh R, Damian M, Cottet M, Orcel H, Mendre C, Durroux T, Sharma KS, Durand G, Pucci B, Trinquet E, Zwier JM, Deupi X, Bron P, Banères JL, Mouillac B, Granier S.

Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6733-8. doi: 10.1073/pnas.1201093109. Epub 2012 Apr 9.

34.

Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to G protein-coupled receptor oligomerization.

Comps-Agrar L, Maurel D, Rondard P, Pin JP, Trinquet E, Prézeau L.

Methods Mol Biol. 2011;756:201-14. doi: 10.1007/978-1-61779-160-4_10.

PMID:
21870227
35.

Time resolved FRET strategy with fluorescent ligands to analyze receptor interactions in native tissues: application to GPCR oligomerization.

Cottet M, Albizu L, Comps-Agrar L, Trinquet E, Pin JP, Mouillac B, Durroux T.

Methods Mol Biol. 2011;746:373-87. doi: 10.1007/978-1-61779-126-0_21.

PMID:
21607869
36.

The oligomeric state sets GABA(B) receptor signalling efficacy.

Comps-Agrar L, Kniazeff J, Nørskov-Lauritsen L, Maurel D, Gassmann M, Gregor N, Prézeau L, Bettler B, Durroux T, Trinquet E, Pin JP.

EMBO J. 2011 May 6;30(12):2336-49. doi: 10.1038/emboj.2011.143.

37.

G protein activation by serotonin type 4 receptor dimers: evidence that turning on two protomers is more efficient.

Pellissier LP, Barthet G, Gaven F, Cassier E, Trinquet E, Pin JP, Marin P, Dumuis A, Bockaert J, Banères JL, Claeysen S.

J Biol Chem. 2011 Mar 25;286(12):9985-97. doi: 10.1074/jbc.M110.201939. Epub 2011 Jan 19.

38.

Investigation of prolactin receptor activation and blockade using time-resolved fluorescence resonance energy transfer.

Tallet E, Fernandez I, Zhang C, Salsac M, Gregor N, Ayoub MA, Pin JP, Trinquet E, Goffin V.

Front Endocrinol (Lausanne). 2011 Sep 16;2:29. doi: 10.3389/fendo.2011.00029. eCollection 2011.

39.

Trans-activation between 7TM domains: implication in heterodimeric GABAB receptor activation.

Monnier C, Tu H, Bourrier E, Vol C, Lamarque L, Trinquet E, Pin JP, Rondard P.

EMBO J. 2011 Jan 5;30(1):32-42. doi: 10.1038/emboj.2010.270. Epub 2010 Nov 9.

40.

A fluorescent ligand-binding alternative using Tag-lite® technology.

Zwier JM, Roux T, Cottet M, Durroux T, Douzon S, Bdioui S, Gregor N, Bourrier E, Oueslati N, Nicolas L, Tinel N, Boisseau C, Yverneau P, Charrier-Savournin F, Fink M, Trinquet E.

J Biomol Screen. 2010 Dec;15(10):1248-59. doi: 10.1177/1087057110384611. Epub 2010 Oct 25.

PMID:
20974902
41.

Homogeneous time-resolved fluorescence-based assay to screen for ligands targeting the growth hormone secretagogue receptor type 1a.

Leyris JP, Roux T, Trinquet E, Verdié P, Fehrentz JA, Oueslati N, Douzon S, Bourrier E, Lamarque L, Gagne D, Galleyrand JC, M'kadmi C, Martinez J, Mary S, Banères JL, Marie J.

Anal Biochem. 2011 Jan 15;408(2):253-62. doi: 10.1016/j.ab.2010.09.030. Epub 2010 Sep 24.

PMID:
20937574
42.

A new approach to analyze cell surface protein complexes reveals specific heterodimeric metabotropic glutamate receptors.

Doumazane E, Scholler P, Zwier JM, Trinquet E, Rondard P, Pin JP.

FASEB J. 2011 Jan;25(1):66-77. doi: 10.1096/fj.10-163147. Epub 2010 Sep 8.

PMID:
20826542
43.

Time-resolved FRET between GPCR ligands reveals oligomers in native tissues.

Albizu L, Cottet M, Kralikova M, Stoev S, Seyer R, Brabet I, Roux T, Bazin H, Bourrier E, Lamarque L, Breton C, Rives ML, Newman A, Javitch J, Trinquet E, Manning M, Pin JP, Mouillac B, Durroux T.

Nat Chem Biol. 2010 Aug;6(8):587-94. doi: 10.1038/nchembio.396. Epub 2010 Jul 11.

44.

Differential association modes of the thrombin receptor PAR1 with Galphai1, Galpha12, and beta-arrestin 1.

Ayoub MA, Trinquet E, Pfleger KD, Pin JP.

FASEB J. 2010 Sep;24(9):3522-35. doi: 10.1096/fj.10-154997. Epub 2010 Apr 21.

PMID:
20410441
45.

HTRF: A technology tailored for drug discovery - a review of theoretical aspects and recent applications.

Degorce F, Card A, Soh S, Trinquet E, Knapik GP, Xie B.

Curr Chem Genomics. 2009 May 28;3:22-32. doi: 10.2174/1875397300903010022.

46.

G-protein-coupled receptor oligomers: two or more for what? Lessons from mGlu and GABAB receptors.

Pin JP, Comps-Agrar L, Maurel D, Monnier C, Rives ML, Trinquet E, Kniazeff J, Rondard P, Prézeau L.

J Physiol. 2009 Nov 15;587(Pt 22):5337-44. doi: 10.1113/jphysiol.2009.179978. Epub 2009 Sep 1. Review.

47.

Crosstalk between GABAB and mGlu1a receptors reveals new insight into GPCR signal integration.

Rives ML, Vol C, Fukazawa Y, Tinel N, Trinquet E, Ayoub MA, Shigemoto R, Pin JP, Prézeau L.

EMBO J. 2009 Aug 5;28(15):2195-208. doi: 10.1038/emboj.2009.177. Epub 2009 Jul 9.

48.

Functional adhesiveness of the CX3CL1 chemokine requires its aggregation. Role of the transmembrane domain.

Hermand P, Pincet F, Carvalho S, Ansanay H, Trinquet E, Daoudi M, Combadière C, Deterre P.

J Biol Chem. 2008 Oct 31;283(44):30225-34. doi: 10.1074/jbc.M802638200. Epub 2008 Aug 25.

49.

Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to GPCR oligomerization.

Maurel D, Comps-Agrar L, Brock C, Rives ML, Bourrier E, Ayoub MA, Bazin H, Tinel N, Durroux T, Prézeau L, Trinquet E, Pin JP.

Nat Methods. 2008 Jun;5(6):561-7. doi: 10.1038/nmeth.1213. Epub 2008 May 18.

50.

Functioning of the dimeric GABA(B) receptor extracellular domain revealed by glycan wedge scanning.

Rondard P, Huang S, Monnier C, Tu H, Blanchard B, Oueslati N, Malhaire F, Li Y, Trinquet E, Labesse G, Pin JP, Liu J.

EMBO J. 2008 May 7;27(9):1321-32. doi: 10.1038/emboj.2008.64. Epub 2008 Apr 3.

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