Institut de
Génomique
Fonctionnelle

2012

Loison S, Cottet M, Orcel H, Adihou H, Rahmeh R, Lamarque L, Trinquet E, Kellenberger E, Hibert M, Durroux T, Mouillac B, Bonnet D. Selective Fluorescent Nonpeptidic Antagonists For Vasopressin V(2) GPCR : Application To Ligand Screening and Oligomerization Assays. J Med Chem. 2012 Oct 25 ;55(20):8588-602.

Banères JL, Mouillac B. Handling G-protein-coupled receptors : expression, purification and in vitro stabilization. Med Sci (Paris). 2012 Oct ;28(10):837-44. Granier S. Structure of mu and delta opioid receptors. Med Sci (Paris). 2012 Oct ;28(10):870-5.

Cottet M, Faklaris O, Trinquet E, Pin JP, Durroux T. New fluorescent strategies shine light on the evolving concept of GPCR oligomerization. In Fluorescent Methods to study biological membranes ed Y Mely and G Duportail. Springer Series on Fluorescence 13 Ed Marti Hof. Springer.

Cottet M, Faklaris O, Maurel D, Scholler P, Doumazane E, Trinquet E, Pin JP, Durroux T. BRET and Time-resolved FRET strategy to study GPCR oligomerization : from cell lines toward native tissues. Front Endocrinol (Lausanne). 2012 ;3:92.

El Moustaine D., Granier S., Doumazane E., Scholler P., Rahmeh R., Bron P., Mouillac B., Banères J.L., Rondard P., and Pin, J.P. Distinct roles of metabotropic glutamate receptor dimerization in agonist activation and G-protein coupling. Proc Natl Acad Sci U S A. 2012 Oct 2 ;109(40):16342-7.

Granier S, and Kobilka B.K. A new era of GPCR structural and chemical biology. Nat. Chem. Biol. 2012 Jul 18 ;8(8):670-3.

Granier S, Manglik A, Kruse AC, Kobilka TS, Thian FS, Weis WI, Kobilka BK.(2012).Structure of the δ-opioid receptor bound to naltrindole. Nature. 2012 May 16 ;485(7398):400-4.

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. (2012). Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy. Proc Natl Acad Sci 24 ;109(17):6733-8.

Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S.(2012). Crystal structure of the µ-opioid receptor bound to a morphinan antagonist. Nature. 2012 Mar 21 ;485(7398):321-6

Manning M, Misicka A, Olma A, Bankowski K, Stoev S, Chini B, Durroux T, Mouillac B, Corbani M, Guillon G.(2012). Oxytocin and vasopressin agonists and antagonists as research tools and potential therapeutics.J Neuroendocrinol. 2012 Apr ;24(4):609-28

Morin D, Tenenbaum J, Ranchin B, Durroux T.(2012).Nephrogenic syndrome of inappropriate antidiuresis.Int J Pediatr. 2012 ;2012:937175

2011

Zwier, J. M., T. Roux, M. Cottet, T. Durroux, S. Douzon, S. Bdioui, N. Gregor, E. Bourrier, N. Oueslati, L. Nicolas, N. Tinel, C. Boisseau, P. Yverneau, F. Charrier-Savournin, M. Fink and E. Trinquet (2010). "A fluorescent ligand-binding alternative using Tag-lite(R) technology." J Biomol Screen 15(10) : 1248-1259.

Cottet M, Albizu L, Comps-Agrar L, Trinquet E, Pin JP, Mouillac B, Durroux T. (2011) Time resolved FRET strategy with fluorescent ligands to analyze receptor interactions in native tissues : application to GPCR oligomerization. Methods Mol Biol. 746 ;373-87.

Cottet M, Faklaris O, Zwier J, Trinquet E, Pin J, Durroux T. (2011) Original Fluorescent Ligand-Based Assays Open New Perspectives in G-Protein Coupled Receptor Drug Screening. Pharmaceuticals 4(1), 202-214.

Bellot G, Pascal R, Mendre C, Urbach S, Mouillac B, Déméné H. (2011) Expression, purification and NMR characterization of the cyclic recombinant form of the third intracellular loop of the vasopressin type 2 receptor. Protein Expr Purif. 78(2):131-8.

Banères JL, Popot JL, Mouillac B. (2011) New advances in production and functional folding of G-protein-coupled receptors. Trends Biotechnol. 29(7):314-22.

Comps-Agrar L, Kniazeff J, Nørskov-Lauritsen L, Maurel D, Gassmann M, Gregor N, Prézeau L, Bettler B, Durroux T, Trinquet E, Pin JP.(2011) The oligomeric state sets GABA(B) receptor signalling efficacy. EMBO J.30(12):2336-49.

2010

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. (2010) Time-resolved FRET between GPCR ligands reveals oligomers in native tissues. Nat Chem Biol. Aug ;6(8):587-94.

Laure Arcemisbehere, Tuhinadri Sen, Laure Boudier, Marie-Noelle Balestre, Gerald Gaibelet, Emilie Detouillon, Helene Orcel, Christiane Mendre, Rita Rahmeh, Sebastien Granier, Corinne Vives, Franck Fieschi, Marjorie Damian, Thierry Durroux, Jean-Louis Banères and Bernard Mouillac (2010) Leukotriene BLT2 receptor monomers activate the Gi2 GTP-binding protein more efficiently than dimers. J Biol Chem, 285 (9), 6337-47

Cottet M., Albizu L., Perkovska S., Jean-Alphonse F., Rahmeh R., Orcel H., Méjean C., Granier S., Mendre C., Mouillac B., Durroux T. (2010) Past, present and future of vasopressin and oxytocin receptor oligomers, prototypical GPCR models to study dimerization processes. Current Opinion in Pharmacology, 10 (1), 59-66.

Mendre C, Mouillac B. (2010) Pharmacological chaperones : a potential therapeutic treatment for conformational diseases. Med Sci (Paris). Jun-Jul ;26(6-7):627-35.

2009

Tenenbaum J, Ayoub MA, Perkovska S, Adra-Delenne AL, Mendre C, Ranchin B, Bricca G, Geelen G, Mouillac B, Durroux T, Morin D. (2009) The constitutively active V2 receptor mutants conferring NSIAD are weakly sensitive to agonist and antagonist regulation. PLoS One, Dec 21 ;4(12):e8383.

Jean-Alphonse F, Perkovska S, Frantz M, Durroux T, Méjean C, Morin D, Loison S, Bonnet D, Hibert M, Mouillac B, Mendre C (2009) Biased agonists of the arginine-vasopressin V2 receptor : novel pharmacochaperones with therapeutic potential for treating congenital nephrogenic diabetes insipidus. J Am Soc Nephrol. 20 : 2190-2203

Orcel H, Albizu L, Perkovska S, Durroux T, Mendre C, Ansanay H, Mouillac B, Rabié A (2009) Differential coupling of the vasopressin V1b receptor through compartmentalization within plasma membrane. Mol Pharmacol 75:637-647.

Bellot G, Granier S, Bourguet W, Seyer R, Rahmeh R, Mouillac B, Pascal R, Mendre C, Déméné H (2009) Structure of the third intracellular loop of the vasopressin V2 receptor and conformational changes upon binding to gC1qR. J Mol Biol 388:491-507.

2008

Maurel D, Comps-Agrar L, Brock C, Rives ML, Bourrier E, Ayoub MA, Bazin H, Tinel N, Durroux T, Prezeau L, Trinquet E, Pin JP (2008) Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies : application to GPCR oligomerization. Nat Methods 5:561-567.

Granier S, Jean-Alphonse F, Bacqueville D, Monteil A, Pascal R, Poncet J, Guillon G, Boudier L, Arcemisbehere L, Mouillac B, Bellot G, Demene H, Mendre C (2008) The multifunctional protein GC1q-R interacts specifically with the i3 loop arginine cluster of the vasopressin V2 receptor. Regul Pept 148:76-87.

Bonnet D, Riche S, Loison S, Dagher R, Frantz MC, Boudier L, Rahmeh R, Mouillac B, Haiech J, Hibert M (2008) Solid-phase organic tagging resins for labeling biomolecules by 1,3-dipolar cycloaddition : application to the synthesis of a fluorescent non-peptidic vasopressin receptor ligand. Chemistry 14:6247-6254.

Mouillac B, Manning M, Durroux T (2008) Fluorescent agonists and antagonists for vasopressin/oxytocin g protein-coupled receptors : usefulness in ligand screening assays and receptor studies. Mini Rev Med Chem 8:996-1005.

Manning M, Stoev S, Chini B, Durroux T, Mouillac B, Guillon G (2008) Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V(1a), V(1b), V(2) and OT receptors : research tools and potential therapeutic agents. Prog Brain Res 170:473-512.

2007

Szwarc I, Soullier S, Gayrard N, Mejean C, Mourad G, Argiles A (2007) Ischemic postconditioning prevents ischemic acute renal failure. Transplant Proc 39:2554-2556.

Rodrigo J, Pena A, Murat B, Trueba M, Durroux T, Guillon G, Rognan D (2007) Mapping the binding site of arginine vasopressin to V1a and V1b vasopressin receptors. Mol Endocrinol 21:512-523.

Albizu L, Teppaz G, Seyer R, Bazin H, Ansanay H, Manning M, Mouillac B, Durroux T (2007) Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. J Med Chem 50:4976-4985.

2006

Trinquet E, Fink M, Bazin H, Grillet F, Maurin F, Bourrier E, Ansanay H, Leroy C, Michaud A, Durroux T, Maurel D, Malhaire F, Goudet C, Pin JP, Naval M, Hernout O, Chretien F, Chapleur Y, Mathis G (2006) D-myo-inositol 1-phosphate as a surrogate of D-myo-inositol 1,4,5-tris phosphate to monitor G protein-coupled receptor activation. Anal Biochem 358:126-135.

Granier S, Jean-Alphonse F, Demene H, Guillon G, Pascal R, Mendre C (2006) Design and synthesis of cyclic and linear peptide-agarose tools for baiting interacting protein partners of GPCRs. Bioorg Med Chem Lett 16:521-524.

Alves ID, Delaroche D, Mouillac B, Salamon Z, Tollin G, Hruby VJ, Lavielle S, Sagan S (2006) The two NK-1 binding sites correspond to distinct, independent, and non-interconvertible receptor conformational states as confirmed by plasmon-waveguide resonance spectroscopy. Biochemistry 45:5309-5318.

Albizu L, Balestre MN, Breton C, Pin JP, Manning M, Mouillac B, Barberis C, Durroux T (2006) Probing the existence of G protein-coupled receptor dimers by positive and negative ligand-dependent cooperative binding. Mol Pharmacol 70:1783-1791.

2005

Ponthieux S, Cabot J, Mouillac B, Seyer R, Barberis C, Carnazzi E (2005) Design of benzophenone-containing photoactivatable linear vasopressin antagonists : pharmacological and photoreactive properties. J Med Chem 48:3379-3388.

Manning M, Cheng LL, Stoev S, Wo NC, Chan WY, Szeto HH, Durroux T, Mouillac B, Barberis C (2005) Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban. J Pept Sci 11:593-608.

Levoye A, Mouillac B, Riviere G, Vieau D, Salzet M, Breton C (2005) Cloning, expression and pharmacological characterization of a vasopressin-related receptor in an annelid, the leech Theromyzon tessulatum. J Endocrinol 184:277-289.

Durroux T (2005) Principles : a model for the allosteric interactions between ligand binding sites within a dimeric GPCR. Trends Pharmacol Sci 26:376-384.

Duroux-Richard I, Vassault P, Subra G, Guichou JF, Richard E, Mouillac B, Barberis C, Marie J, Bonnafous JC (2005) Crosslinking photosensitized by a ruthenium chelate as a tool for labeling and topographical studies of G-protein-coupled receptors. Chem Biol 12:15-24.

Levoye A., Mouillac B., Rivière G., Vieau D., Salzet M. and Breton C. Cloning, expression and pharmacological characterization of a vasopressin-related receptor in an annelid, the leech Theromizon tessulatum. J. Endocrinol. 2005, 184, 277-289.

2004

Derick S., Pena A., Durroux T., Wagnon J., Serradeil-Le Gal C., Hibert M., Rognan D. and Guillon G. Key amino acids located within the transmembrane domains 5 and 7 account for the pharmacological specificity of the human V1b vasopressin receptor. Mol. Endocrinol. 2004, 18, 2777-2789.

2003

Terrillon S., Durroux T., Mouillac B., Breit A., Ayoub M.A., Taulan M., Jockers R., Barberis C. and Bouvier M. Oxytocin and vasopressin V1a and V2 receptors Form constitutive homo- and heterodimers during biosynthesis. Mol Endocrinol. 2003,17, 677-91.

Tahtaoui C., Balestre M-N., Klotz P., Rognan D., Barberis C., Mouillac B. and Hibert M. Identification of the binding sites of the SR49059 nonpeptide antagonist into the V1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors. J. Biol. Chem. 2003, 278, 40010-40019.

2002

Mouillac B., Sen T., Durroux T., Gaibelet G. and Barberis C. Expression of human vasopressin and oxytocin receptors in Escherichia coli. Prog. Brain Res. 2002, 139, 163-177.

Terrillon S., Cheng L.L., Stoev S., Mouillac B., Barberis C., Manning M. and Durroux T. Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V1a receptors. J Med Chem. 2002, 45, 2579-2588.

2001

Breton C., Chellil H., Kabbaj-Benmansour M., Carnazzi E., Seyer R., Phalipou S., Morin D., Durroux T., Zingg H., Barberis C. and Mouillac B. Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist : comparison with the human V1a vasopressin receptor. J. Biol. Chem. 2001, 276, 26931-26941.

Carnazzi E., Aumelas A., Mouillac B., Breton C., Guillou L., Barberis C. and Seyer R. Design, synthesis and pharmacological characterization of a potent radioiodinated and photoactivatable peptidic oxtocin antagonist. J. Med. Chem. 2001, 44, 3022-3030.

2000

Cotte N., Balestre M-N., Aumelas A., Mahé E., Phalipou S., Morin D., Hibert M., Manning M., Durroux T., Barberis C. and Mouillac B. Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding. Eur. J. Biochem. 2000, 267, 4253-4263.

1999

Tran D., Durroux T., Stelly N., Seyer R., Tordjmann T., Combettes L. and Claret M. Visualization of cell surface vasopressin V1a receptors in rat hepatocytes with a fluorescent linear antagonist. J Histochem Cytochem. 1999, 47, 401-410.

Phalipou S., Seyer R., Cotte N., Breton C., Barberis C., Hibert M. and Mouillac B. Docking of linear peptide antagonists into the human V1a vasopressin receptor : identification of binding domains by photoaffinity labeling. J. Biol. Chem. 1999, 274, 23316-23327.

Barberis C., Morin D., Durroux T., Mouillac B., Guillon G., Seyer R., Hibert M., Tribollet E. and Barberis C. Molecular pharmacology of AVP and OT receptors and therapeutic potential. Drug News Perspect. 1999, 12, 279-292.

Tran D., Stelly N., Tordjmann T., Durroux T., Dufour M-N., Forchioni A., Seyer R., Claret M. and Guillon G. Distribution of signaling molecules involved in vasopressin-induced Ca2+ mobilization in rat hepatocyte multiplets. J Histochem Cytochem.1999, 47, 601-616.

Durroux T., Peter M., Turcatti G., Chollet A., Balestre M-N., Barberis C. and Seyer R. Fluorescent pseudo-peptide linear vasopressin antagonists : design, synthesis, and applications. J Med Chem. 1999, 42, 1312-1319.