Publications

Healey RD, Saied EM, Cong X, Karsai G, Gabeller L, Saint-Paul J, Del Nero E, Jeannot S, Drapeau M, Fontanel S, Maurel D, Basu S, Leyrat C, Golebiowski J, Bossis G, Bechara C, Hornemann T, Arenz C, Granier S. Discovery and mechanisms of action of small molecule inhibitors of ceramidases. Angew Chem int Ed Engl. 2021 Oct 20: doi: 10.1002/anie.202109967. 

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Grison CM, Lambey P, Jeannot S, Del Nero E, Fontanel S, Peysson F, Heuninck J, Sounier R, Durroux T, Leyrat C, Granier S, Bechara C. Molecular insights into mechanism of GPCR hijacking by Staphylococcus aureus. Proc Natl Acad Sci USA. 2021 Oct 19;118(42):e2108856118. doi: 10.1073/pnas.2108856118.PUBMED 
Cong X, Maurel D, Déméné H, Vasiliauskaité-Brooks I, Hagelberger J, Peysson F, Saint-Paul J, Golebiowski J, Granier S, Sounier R. Molecular insights into the biased signaling mechanism of the μ-opioid receptor. Mol Cell. 2021 Aug 18:S1097-2765(21)00611-0. doi: 10.1016/j.molcel.2021.07.033. PUBMED 
Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Déméné H, Granier S, Bron P, Mouillac B. Cryo-electron microscopy structure of the antidiuretic hormone arginine-vasopressin V2 receptor signaling complex. Sci Adv. 2021 May 21;7(21):eabg5628.PUBMED
Lemel L, Nieścierowicz K, García-Fernández MD, Darré L, Durroux T, Busnelli M, Pezet M, Rebeille F, Jouhet J, Mouillac B, Domene C, Chini B, Cherezov V, Moreau CJ. The ligand-bound state of a G protein-coupled receptor stabilizes the interaction of functional cholesterol molecules. J Lipid Res. 2021 Feb 26:100059.PUBMED
Aissaoui N, Lai-Kee-Him J, Mills A, Declerck N, Morichaud Z, Brodolin K, Baconnais S, Le Cam E, Charbonnier JB, Sounier R, Granier S, Ropars V, Bron P, Bellot G. Modular Imaging Scaffold for Single-Particle Electron Microscopy. ACS Nano. 2021 Mar 23;15(3):4186-4196.PUBMED
Droctové L, Lancien M, Tran VL, Susset M, Jego B, Theodoro F, Kessler P, Mourier G, Robin P, Diarra SS, Palea S, Flahault A, Chorfa A, Corbani M, Llorens-Cortes C, Mouillac B, Mendre C, Pruvost A, Servent D, Truillet C, Gilles N. A snake toxin as a theranostic agent for the type 2 vasopressin receptor. Theranostics. 2020 Sep 18;10(25):11580-11594.PUBMED
Gentzsch C, Seier K, Drakopoulos A, Jobin ML, Lanoiselée Y, Koszegi Z, Maurel D, Sounier R, Hübner H, Gmeiner P, Granier S, Calebiro D, Decker M. Selective and Wash-Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single-Molecule Imaging of μ-Opioid Receptor Dimerization. Angew Chem Int Ed Engl. 2020 Apr 6;59(15):5958-5964.
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Ramanoudjame SM, Esteoulle L, Riché S, Margathe JF, Durroux T, Karpenko IA, Bonnet D. Chemoselective Acylation of Hydrazinopeptides to Access Fluorescent Probes for Time-Resolved FRET Assays on GPCRs. Methods Mol Biol. 2019;1947:137-147. PUBMED 
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors. Br J Pharmacol. 2019 Dec;176 Suppl 1(Suppl 1):S21-S141. PUBMED 
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. Context-Dependent Signaling of CXC Chemokine Receptor 4 and Atypical Chemokine Receptor 3. Mol Pharmacol. 2019 Dec;96(6):778-793. PUBMED 
Mendre C, Mouillac B. Misfolding of vasopressin receptors: biased agonist pharmacochaperones as potential therapeutics. Adv Protein Chem Struct Biol. 2019;118:249-272. PUBMED 
Heuninck J, Hounsou C, Dupuis E, Trinquet E, Mouillac B, Pin JP, Bonnet D, Durroux T. Time-Resolved FRET-Based Assays to Characterize G Protein-Coupled Receptor Hetero-oligomer Pharmacology. Methods Mol Biol. 2019;1947:151-168. PUBMED 
Jespersen NE, Leyrat C, Gérard FC, Bourhis JM, Blondel D, Jamin M, Barbar E. The LC8-RavP ensemble Structure Evinces A Role for LC8 in Regulating Lyssavirus Polymerase Functionality. J Mol Biol. 2019 Dec 6;431(24):4959-4977. PUBMED 
Boullet H, Bentot F, Hequet A, Ganem-Elbaz C, Bechara C, Pacreau E, Launay P, Sagan S, Jolivalt C, Lacombe C, Moumné R, Karoyan P. Small AntiMicrobial Peptide With in Vivo Activity Against Sepsis. Molecules. 2019 May 1;24(9):1702. PUBMED 
Vasiliauskaité-Brooks I, Healey RD, Granier S. 7TM proteins are not necessarily GPCRs. Mol Cell Endocrinol. 2019 Jul 1;491:110397. PUBMED 
Gauto DF, Estrozi LF, Schwieters CD, Effantin G, Macek P, Sounier R, Sivertsen AC, Schmidt E, Kerfah R, Mas G, Colletier JP, Güntert P, Favier A, Schoehn G, Schanda P, Boisbouvier J. Integrated NMR and cryo-EM atomic-resolution structure determination of a half-megadalton enzyme complex. Nat Commun. 2019 Jun 19;10(1):2697. PUBMED 
Allison TM, Bechara C. Structural mass spectrometry comes of age: new insight into protein structure, function and interactions. Biochem Soc Trans. 2019 Feb 28;47(1):317-327. PUBMED 
Schmidt V, Sidore M, Bechara C, Duneau JP, Sturgis JN. The lipid environment of Escherichia coli Aquaporin Z. Biochim Biophys Acta Biomembr. 2019 Feb 1;1861(2):431-440. PUBMED 

Belhocine A, Veglianese P, Hounsou C, Dupuis E, Acher F, Durroux T, Goudet C, Pin JP. Profiling of orthosteric and allosteric group-III metabotropic glutamate receptor ligands on various G protein-coupled receptors with Tag-lite® assays. Neuropharmacology. 2018 Sep 15;140:233-245.

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Møller TC, Hottin J, Clerté C, Zwier JM, Durroux T, Rondard P, Prézeau L, Royer CA, Pin JP, Margeat E, Kniazeff J. Oligomerization of a G protein-coupled receptor in neurons controlled by its structural dynamics. Sci Rep. 2018 Jul 10;8(1):10414. PUBMED 
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. From the Promiscuous Asenapine to Potent Fluorescent Ligands Acting at a Series of Aminergic G-Protein-Coupled Receptors. J Med Chem. 2018 Jan 11;61(1):174-188. PUBMED 
Vasiliauskaité-Brooks I, Healey RD, Rochaix P, Saint-Paul J, Sounier R, Grison C, Waltrich-Augusto T, Fortier M, Hoh F, Saied EM, Arenz C, Basu S, Leyrat C, Granier S. Structure of a human intramembrane ceramidase explains enzymatic dysfunction found in leukodystrophy. Nat Commun. 2018 Dec 21;9(1):5437. PUBMED 
Berry L, Chen CT, Francia ME, Guerin A, Graindorge A, Saliou JM, Grandmougin M, Wein S, Bechara C, Morlon-Guyot J, Bordat Y, Gubbels MJ, Lebrun M, Dubremetz JF, Daher W. Toxoplasma gondii chromosomal passenger complex is essential for the organization of a functional mitotic spindle: a prerequisite for productive endodyogeny. Cell Mol Life Sci. 2018 Dec;75(23):4417-4443. PUBMED 
Mouillac B, Mendre C. Pharmacological Chaperones as Potential Therapeutic Strategies for Misfolded Mutant Vasopressin Receptors. Handb Exp Pharmacol. 2018;245:63-83. PUBMED 
Perkovska S, Méjean C, Ayoub MA, Li J, Hemery F, Corbani M, Laguette N, Ventura MA, Orcel H, Durroux T, Mouillac B, Mendre C. V1b vasopressin receptor trafficking and signaling: Role of arrestins, G proteins and Src kinase. Traffic. 2018 Jan;19(1):58-82. PUBMED 
Frantz MC, Pellissier LP, Pflimlin E, Loison S, Gandía J, Marsol C, Durroux T, Mouillac B, Becker JAJ, Le Merrer J, Valencia C, Villa P, Bonnet D, Hibert M. LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. J Med Chem. 2018 Oct 11;61(19):8670-8692. PUBMED 
Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK. Structure of the µ-opioid receptor-Gi protein complex. Nature. 2018 Jun ;558(7711):547-552. PUBMED 
Gupta K, Li J, Liko I, Gault J, Bechara C, Wu D, Hopper JTS, Giles K, Benesch JLP, Robinson CV. Identifying key membrane protein lipid interactions using mass spectrometry. Nat Protoc. 2018 May;13(5):1106-1120. PUBMED 
Kurauskas V, Hessel A, Ma P, Lunetti P, Weinhäupl K, Imbert L, Brutscher B, King MS, Sounier R, Dolce V, Kunji ERS, Capobianco L, Chipot C, Dehez F, Bersch B, Schanda P. How Detergent Impacts Membrane Proteins: Atomic-Level Views of Mitochondrial Carriers in Dodecylphosphocholine. J Phys Chem Lett. 2018 Mar 1;9(5):933-938. PUBMED 
Smith N, Pietrancosta N, Davidson S, Dutrieux J, Chauveau L, Cutolo P, Dy M, Scott-Algara D, Manoury B, Zirafi O, McCort-Tranchepain I, Durroux T, Bachelerie F, Schwartz O, Münch J, Wack A, Nisole S, Herbeuval JP. Natural amines inhibit activation of human plasmacytoid dendritic cells through CXCR4 engagement. Nat Commun. 2017 Feb 9;8:14253. PUBMED 
Recio R, Vengut-Climent E, Mouillac B, Orcel H, López-Lázaro M, Calderón-Montaño JM, Álvarez E, Khiar N, Fernández I. Design, synthesis and biological studies of a library of NK1-Receptor Ligands Based on a 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyran core: Switch from antagonist to agonist effect by chemical modification. Eur J Med Chem. 2017 Sep 29;138:644-660. PUBMED 
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. Pharmacological evidence for a metabotropic glutamate receptor heterodimer in neuronal cells. Elife. 2017 Jun 29;6:e25233. PUBMED 
Ciolek J, Reinfrank H, Quinton L, Viengchareun S, Stura EA, Vera L, Sigismeau S, Mouillac B, Orcel H, Peigneur S, Tytgat J, Droctové L, Beau F, Nevoux J, Lombès M, Mourier G, De Pauw E, Servent D, Mendre C, Witzgall R, Gilles N. Green mamba peptide targets type-2 vasopressin receptor against polycystic kidney disease. Proc Natl Acad Sci U S A. 2017 Jul 3;114(27):7154-7159. PUBMED 
Renner M, Paesen GC, Grison CM, Granier S, Grimes JM, Leyrat C. Structural dissection of human metapneumovirus phosphoprotein using small angle x-ray scattering. Sci Rep. 2017 Nov 1;7(1):14865. PUBMED 
Kurauskas V, Schanda P, Sounier R. Methyl-Specific Isotope Labeling Strategies for NMR Studies of Membrane Proteins. Methods Mol Biol. 2017;1635:109-123. PUBMED 
Vasiliauskaité-Brooks I, Sounier R, Rochaix P, Bellot G, Fortier M, Hoh F, De Colibus L, Bechara C, Saied EM, Arenz C, Leyrat C, Granier S. Structural insights into adiponectin receptors suggest ceramidase activity. Nature. 2017 Apr 6;544(7648):120-123. PUBMED 
Sounier R, Yang Y, Hagelberger J, Granier S, Déméné H. 1H, 13C and 15N backbone chemical shift assignments of camelid single-domain antibodies against active state µ-opioid receptor. Biomol NMR Assign. 2017 Apr;11(1):117-121. PUBMED 
Rossato M, Miralles G, M’Kadmi C, Maingot M, Amblard M, Mouillac B, Gagne D, Martinez J, Subra G, Enjalbal C, Cantel S. Quantitative MALDI-MS Binding Assays: An Alternative to Radiolabeling. ChemMedChem. 2016 Dec 6;11(23):2582-2587. PUBMED 
Broad J, Maurel D, Kung VW, Hicks GA, Schemann M, Barnes MR, Kenakin TP, Granier S, Sanger GJ. Human native kappa opioid receptor functions not predicted by recombinant receptors: Implications for drug design. Sci Rep. 2016 Aug 5;6:30797. PUBMED 
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. Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor:Gq complex. Proc Natl Acad Sci U S A. 2015 Feb 3;112(5):1601-6. PUBMED 
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. Untangling dopamine-adenosine receptor-receptor assembly in experimental parkinsonism in rats. Dis Model Mech. 2015 Jan;8(1):57-63. PUBMED 
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. A Broad G Protein-Coupled Receptor Internalization Assay that Combines SNAP-Tag Labeling, Diffusion-Enhanced Resonance Energy Transfer, and a Highly Emissive Terbium Cryptate. Front Endocrinol (Lausanne). 2015 Nov 9;6:167. PUBMED 
Oueslati N, Hounsou C, Belhocine A, Rodriguez T, Dupuis E, Zwier JM, Trinquet E, Pin JP, Durroux T. Time-resolved FRET strategy to screen GPCR ligand library. Methods Mol Biol. 2015;1272:23-36. PUBMED 
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. Time-resolved FRET binding assay to investigate hetero-oligomer binding properties: proof of concept with dopamine D1/D3 heterodimer. ACS Chem Biol. 2015 Feb 20;10(2):466-74. PUBMED 
Blanc E, Wagner P, Plaisier F, Schmitt M, Durroux T, Bourguignon JJ, Partiseti M, Dupuis E, Bihel F. Design and validation of a homogeneous time-resolved fluorescence cell-based assay targeting the ligand-gated ion channel 5-HT3A. Anal Biochem. 2015 Sep 1;484:105-12. PUBMED 
Faklaris O, Cottet M, Falco A, Villier B, Laget M, Zwier JM, Trinquet E, Mouillac B, Pin JP, Durroux T. Multicolor time-resolved Förster resonance energy transfer microscopy reveals the impact of GPCR oligomerization on internalization processes. FASEB J. 2015 Jun;29(6):2235-46. PUBMED
Sounier R, Mas C, Steyaert J, Laeremans T, Manglik A, Huang W, Kobilka BK, Déméné H, Granier S. Propagation of conformational changes during μ-opioid receptor activation. Nature. 2015 Aug 20;524(7565):375-8. PUBMED
Huang W, Manglik A, Venkatakrishnan AJ, Laeremans T, Feinberg EN, Sanborn AL, Kato HE, Livingston KE, Thorsen TS, Kling RC, Granier S, Gmeiner P, Husbands SM, Traynor JR, Weis WI, Steyaert J, Dror RO, Kobilka BK. Structural insights into µ-opioid receptor activation. Nature. 2015 Aug 20;524(7565):315-21. PUBMED
Karpenko IA, Margathe JF, Rodriguez T, Pflimlin E, Dupuis E, Hibert M, Durroux T, Bonnet D. Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay. J Med Chem. 2015 Mar 12;58(5):2547-52. PUBMED 
Karpenko IA, Kreder R, Valencia C, Villa P, Mendre C, Mouillac B, Mély Y, Hibert M, Bonnet D, Klymchenko AS. Red fluorescent turn-on ligands for imaging and quantifying G protein-coupled receptors in living cells. Chembiochem. 2014 Feb 10;15(3):359-63. PUBMED 
Mary S, Damian M, Rahmeh R, Mouillac B, Marie J, Granier S, Banères JL. Amphipols in G protein-coupled receptor pharmacology: what are they good for? J Membr Biol. 2014 Oct;247(9-10):853-60. PUBMED 
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. Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy. Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6733-8. PMC3340029. PUBMED 
Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S. Crystal structure of the µ-opioid receptor bound to a morphinan antagonist. Nature. 2012 Mar 21;485(7398):321-6. PUBMED 
Granier S, Manglik A, Kruse AC, Kobilka TS, Thian FS, Weis WI, Kobilka BK. Structure of the δ-opioid receptor bound to naltrindole. Nature. 2012 May 16;485(7398):400-4. PUBMED 
Granier S, Kobilka B. A new era of GPCR structural and chemical biology. Nat Chem Biol. 2012 Jul 18;8(8):670-3. PUBMED 
Granier S. Structure of mu and delta opioid receptors. Med Sci (Paris). 2012 Oct;28(10):870-5. PUBMED 
El Moustaine D, Granier S, Doumazane E, Scholler P, Rahmeh R, Bron P, Mouillac B, Banères JL, Rondard P, Pin JP. 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. PUBMED
Cottet M, Albizu L, Perkovska S, Jean-Alphonse F, Rahmeh R, Orcel H, Méjean C, Granier S, Mendre C, Mouillac B, Durroux T. Past, present and future of vasopressin and oxytocin receptor oligomers, prototypical GPCR models to study dimerization processes. Curr Opin Pharmacol. 2010 Feb;10(1):59-66. PUBMED
Arcemisbéhère L, Sen T, Boudier L, Balestre MN, Gaibelet G, Detouillon E, Orcel H, Mendre C, Rahmeh R, Granier S, Vivès C, Fieschi F, Damian M, Durroux T, Banères JL, Mouillac B. Leukotriene BLT2 receptor monomers activate the G(i2) GTP-binding protein more efficiently than dimers. J Biol Chem. 2010 Feb 26;285(9):6337-47. PUBMED
Granier S, Kim S, Fung JJ, Bokoch MP, Parnot C. FRET-based measurement of GPCR conformational changes. Methods Mol Biol. 2009;552:253-68. PUBMED
Bellot G, Granier S, Bourguet W, Seyer R, Rahmeh R, Mouillac B, Pascal R, Mendre C, Déméné H. Structure of the third intracellular loop of the vasopressin V2 receptor and conformational changes upon binding to gC1qR. J Mol Biol. 2009 May 8;388(3):491-507. PUBMED
Richter W, Day P, Agrawal R, Bruss MD, Granier S, Wang YL, Rasmussen SG, Horner K, Wang P, Lei T, Patterson AJ, Kobilka B, Conti M. Signaling from beta1- and beta2-adrenergic receptors is defined by differential interactions with PDE4. EMBO J. 2008 Jan 23;27(2):384-93. PUBMED
Granier S, Jean-Alphonse F, Bacqueville D, Monteil A, Pascal R, Poncet J, Guillon G, Boudier L, Arcemisbéhère L, Mouillac B, Bellot G, Déméné H, Mendre C. The multifunctional protein GC1q-R interacts specifically with the i3 loop arginine cluster of the vasopressin V2 receptor. Regul Pept. 2008 Jun 5;148(1-3):76-87. PUBMED
Huang B, Wu H, Bhaya D, Grossman A, Granier S, Kobilka BK, Zare RN. Counting low-copy number proteins in a single cell. Science. 2007 Jan 5;315(5808):81-4. PUBMED
Granier S, Kim S, Shafer AM, Ratnala VR, Fung JJ, Zare RN, Kobilka B. Structure and conformational changes in the C-terminal domain of the beta2-adrenoceptor: insights from fluorescence resonance energy transfer studies. J Biol Chem. 2007 May 4;282(18):13895-905. PUBMED 
Granier S, Jean-Alphonse F, Déméné H, Guillon G, Pascal R, Mendre C. Design and synthesis of cyclic and linear peptide-agarose tools for baiting interacting protein partners of GPCRs. Bioorg Med Chem Lett. 2006 Feb;16(3):521-4. PUBMED
Granier S, Terrillon S, Pascal R, Déméné H, Bouvier M, Guillon G, Mendre C. A cyclic peptide mimicking the third intracellular loop of the V2 vasopressin receptor inhibits signaling through its interaction with receptor dimer and G protein. J Biol Chem. 2004 Dec 3;279(49):50904-14. PUBMED
Déméné H, Granier S, Muller D, Guillon G, Dufour MN, Delsuc MA, Hibert M, Pascal R, Mendre C. Active peptidic mimics of the second intracellular loop of the V(1A) vasopressin receptor are structurally related to the second intracellular rhodopsin loop: a combined 1H NMR and biochemical study. Biochemistry. 2003 Jul 15;42(27):8204-13. PUBMED