Publications Contributions scientifiques de la plateforme

Summary

2022

  • Eguida M., Schmitt-Valencia C., Hibert M., Villa P., Rognan D. Target-focused library design by pocket-applied computer vision and fragment deep generative linking. J. Med. Chem. 2022, 65, 13771-83. Doi :10.1021/acs.jmedchem.2c00931

  • Rady T, Turelli L, Nothisen M, Tobaldi E, Erb S, Thoreau F, Hernandez-Alba O, Cianferani S, Daubeuf F, Wagner A, Chaubet G. A Novel Family of Acid-Cleavable Linker Based on Cyclic Acetal Motifs for the Production of Antibody-Drug Conjugates with High Potency and Selectivity. Bioconjug Chem. 2022 Sep 15. doi: 10.1021/acs.bioconjchem.2c00314

  • Pierrevelcin M, Flacher V, Mueller CG, Vauchelles R, Guerin E, Lhermitte B, Pencreach E, Reisch A, Muller Q, Doumard L, Boufenghour W, Klymchenko AS, Foppolo S, Nazon C, Weingertner N, Martin S, Briandet C, Laithier V, Di Marco A, Bund L, Obrecht A, Villa P, Dontenwill M, Entz-Werlé N. Engineering Novel 3D Models to Recreate High-Grade Osteosarcoma and its Immune and Extracellular Matrix Microenvironment. Adv Healthc Mater. 2022 Sep 4:e2200195. doi: 10.1002/adhm.202200195

  • Segaud J, Yao W, Marschall P, Daubeuf F, Lehalle C, German B, Meyer P, Hener P, Hugel C, Flatter E, Guivarch M, Clauss L, Martin SF, Oulad-Abdelghani M, Li M. Context-dependent function of TSLP and IL-1β in skin allergic sensitization and atopic march. Nat Commun. 2022 Sep 1;13(1):4703. doi: 10.1038/s41467-022-32196-1

  • Poirot A, Wacht G, Lehalle C, Saas P, Frossard N, Geny B, de Blay F, Barnig C; NK cells and lipoxin A4 promote resolution of eosinophilic inflammation after nasal allergen challenge; Allergy. (2022) Jan;77(1):309-313; doi: 10.1111/all.15103

  • Houel E, Ginouves M, Azas N, Bourreau E, Eparvier V, Hutter S, Knittel-Obrecht A, Jahn-Oyac A, Prévot G, Villa P, Vonthron-Sénécheau C, Odonne G. Treating leishmaniasis in Amazonia, part 2: Multi-target evaluation of widely used plants to understand medicinal practices. J. of Ethnopharmacology 289 (2022) 115054. Doi: /10.1016/j.jep.2022.115054
     
  • Megat S, Hugel S, Journée SH, Bohren Y, Lacaud A, Lelièvre V, Doridot S, Villa P, Bourguignon JJ, Salvat E, Schlichter R, Freund-Mercier MJ, Yalcin I and M Barrot Antiallodynic action of phosphodiesterase inhibitors in a mouse model of peripheral nerve injury. Neuropharmacology 205 (2022) DOI: 10.1016/j.neuropharm.2021.108909
     
  • Hany R, Leyris J-P, Bret G, Mallié S, Sar C, Thouaye M, Hamze A, Provot O, Sokoloff P, Valmier J, Villa P, and Rognan D
    High-Throughput Screening for Extracellular Inhibitors of the FLT3 Receptor Tyrosine Kinase Reveals Chemically Diverse and Druggable Negative Allosteric Modulators. ACS Chemical Biology 17 (3), 709-722 (2022). DOI: 10.1021/acschembio.2c00048

2021

  • Schall N, Daubeuf F, Marsol C, Gizzi P, Frossard N, Bonnet D, Galzi JL, Muller S. A Selective Neutraligand for CXCL12/SDF-1α With Beneficial Regulatory Functions in MRL/Lpr Lupus Prone Mice. Front Pharmacol. 2021 Oct 21;12:752194. doi: 10.3389/fphar.2021.752194. eCollection 2021.

  • Daubeuf F, Schall N, Petit-Demoulière N, Frossard N, Muller S. An Autophagy Modulator Peptide Prevents Lung Function Decrease and Corrects Established Inflammation in Murine Models of Airway Allergy. Cells. 2021 Sep 18;10(9):2468. doi: 10.3390/cells10092468
  • Mascret A, Mouhsine H, Attia G, Cabrera D, Benchekroun M, Gizzi P, Zerrouki C, Fourati N, Zagury JF, Veitia MS, Port M. New contributions to the drug profile of TNFα inhibitor SPD304: Affinity, selectivity and ADMET considerations. Eur J Pharmacol. 2021 Sep 15;907. doi: 10.1016/j.ejphar.2021.174285
  • Mertes PM, Collange O, Coliat P, Banerjee M, Diringer MC, Roche A, Delabranche X, Chaban V, Voegelin M, Bernard A, Sartori V, Velten M, Dhindsa N, Defuria J, Gwangseong K, Xu H, Theodorou M, Huang R, Kalifa K, Geng B, Niyikiza C, Moyo V, Gizzi P, Villa P, Detappe A, Pivot X Liposomal Encapsulation of Trans-Crocetin Enhances Oxygenation in Patients with COVID-19-Related ARDS Receiving Mechanical Ventilation (2021) J Control Release. 2021  in press doi.org/10.1016/j.jconrel.2021.06.033
  •  Quillet R, Schneider S, Utard V, Drieu la Rochelle A, Elhabazi K, Henningsen JB, Gizzi P, Schmitt M, Kugler V, Simonneaux V, Ilien B, Simonin F, Bihel F. Identification of an N-acylated-DArg-Leu-NH2 Dipeptide as a Highly Selective Neuropeptide FF1 Receptor Antagonist That Potently Prevents Opioid-Induced Hyperalgesia. J Med Chem. 2021 May 19. doi: 10.1021/acs.jmedchem.1c00256
  •  Fourmois L, Poyer F, Sourdon A, Naud-Martin D, Nagarajan S, Chennoufi R, Deprez E, Teulade-Fichou MP, Mahuteau-Betzer F. Modulation of Cellular Fate of Vinyl Triarylamines through Structural Fine Tuning: To Stay or Not To Stay in the Mitochondria? Chembiochem. 2021 May 19. doi: 10.1002/cbic.202100168
  • Virlogeux A, Scaramuzzino C, Lenoir S, Carpentier R, Louessard M, Genoux A, Lino P, Hinckelmann MV, Perrier AL, Humbert S, Saudou F. Increasing brain palmitoylation rescues behavior and neuropathology in Huntington disease mice. Sci Adv. 2021 Mar 31;7(14): eabb0799. doi: 10.1126/sciadv.abb0799
  • Hanser F, Marsol C, Valencia C, Villa P, Klymchenko A, Bonnet D, Karpenko I. Nile Red-Based GPCR Ligands as Ultrasensitive Probes of the Local Lipid Microenvironment of the Receptor (2021) ACS Chem Biol in press.  DOI: 10.1021/acschembio.0c00897
  • Daubeuf F, Frossard N. Eosinophils in Asthma Models to House Dust Mite for Drug Development. Methods Mol Biol. 2021; 2241:75-87.
  • Flahault A, Girault-Sotias PE, Keck M, Alvear-Perez R, De Mota N, Estéoulle L, Ramanoudjame SM, Iturrioz X, Bonnet D, Llorens-Cortes C. A metabolically stable apelin-17 analog decreases AVP-induced antidiuresis and improves hyponatremia. Nat Commun. 2021 Jan 12;12(1):305.
  • Demay J, Halary S, Knittel-Obrecht A, Villa P, Duval C, Hamlaoui S, Roussel T, Yéprémian C, Reinhardt A, Bernard C* , B Marie (2021) Anti-inflammatory, Antioxidant and Wound Healing Properties of Cyanobacteria from Thermal Mud of Balaruc-les-Bains, France: a Multi-approach Study. Biomolecules 2021, 11, 28. https://doi.org/10.3390/biom11010028
  • Bollenbach M, Nemska S, Wagner P, Camelin G, Daubeuf F, Obrecht A, Villa P, Rognan D, Bihel F, Bourguignon JJ, Schmitt M*, N Frossard * (2021) Design, synthesis and biological evaluation of arylpyridin-2-yl guanidine derivatives and cyclic mimetics as novel MSK1 inhibitors. An application in an asthma model. Molecules 2021, 26(2), 391. https://0d125oi.org/10.3390/molecules26020391
  • Nemska S, Daubeuf F, Obrecht A, Israel-Biet D, Stern M, Kessler R, Roux R, Tavakoli A, Villa P, Tissot A, Danger R, Reber L, Durand E, Brouard S, Magnan A, Frossard N and the COLT consortium (2020) Overexpression of the MSK1 kinase in patients with chronic lung allograft dysfunction and its confirmed role in a murine model. Transplantation in press
  • Eydoux C, Fattorini V, Shannon A, Le TT, Didier B, Canard B, Guillemot JC. A fluorescence-based high throughput-screening assay for the SARS-CoV RNA synthesis complex. J Virol Methods. 2021 Feb; 288:114013

2020

  • Tang SQ, Leloire M, Schneider S, Mohr J, Bricard J, Gizzi P, Garnier D, Schmitt M, Bihel F. Diastereoselective Synthesis of Nonplanar 3-Amino-1,2,4-oxadiazine Scaffold: Structure Revision of Alchornedine. J Org Chem. 2020 Nov 16. doi: 10.1021/acs.joc.0c01764.
  • Esteoulle L, Daubeuf F, Collot M, Riche S, Durroux T, Brasse D, Marchand P, Karpenko IA, Klymchenko AS and Bonnet D (2020) A near-infrared fluorogenic dimer enables background-free imaging of endogenous GPCRs in living mice. Chem. Science Jun 17;11(26):6824-6829 DOI: 10.1039/d0sc01018a.
  • Calas AG, Hanak AS, Jaffré N, Nervo A, Dias J, Rousseau C, Courageux C, Brazzolotto X, Villa P, Obrecht A, Goossens JF, Landry C, Hachani J, Gosselet F, Dehouck MP, Yerri J, Klyachina M, Baati R, Nachon F (2020) Efficacy assessment of an uncharged reactivator of NOP-inhibited acetylcholinesterase based on tetrahydroacridine pyridine-aldoxime hybrid in Mouse compared to pralidoxime. Biomolecules 2020, 10(6), 858. doi.org/10.3390/biom10060858.
  • Bordenave J, Thuillet R, Tu L, Phan C, Cumont A, Marsol C, Huertas A, Savale L, Hibert M, Galzi JL, Bonnet D, Humbert M, Frossard N, Guignabert C (2020). Neutralization of CXCL12 attenuates established pulmonary hypertension in rats. Cardiovascular Research (2020) 116, 686–697.
  • Fichez J, Soulie C, Le Corre L, Sayon S, Priet S, Alvarez K, Delelis O, Gizzi P, Prestat G, Gravier-Pelletier C, Marcelin AG, Calvez V, Busca P. Discovery, SAR study and ADME properties of methyl 4-amino-3-cyano-1-(2-benzyloxyphenyl)-1H-pyrazole-5-carboxylate as an HIV-1 replication inhibitor. RSC Med Chem. 2020 Apr 27;11(5):577-582.
  • Hilfiger L, Zhao Q, Kerspern D, inquimbert P, Andry V, Goumon Y, Darbon P, Hibert M & A Charlet (2020) A nonpeptide oxytocin Receptor Agonist for a Durable Relief of Inflammatory Pain. Sc. Report (2020) 10:3017.

2019

  • Blandin A.F., Durand A., Litzler M., Tripp A., Guérin E., Ruhland E., Obrecht A., Keime C., Fuchs Q., Reita D., Lhermitte B., Andres C., Jones C., Lelong Rebel I., Villa P., Namer I.J., Dontenwill M., Guenot D., and N Entz-Werle (2019) Hypoxic environment and paired hierarchical 3D and 2D models of pediatric H3.3 mutated gliomas recreate the patient tumor complexity. Cancers 2019, 11 (12), 1875.
  • Bouressam ML, Lecat S, Raoul A, Gaucher C, Perrin‐Sarrado C,  Lartaud I, Dupuis F. (2019) S-nitrosoglutathione inhibits cerebrovascular angiotensin II-dependent and -independent AT1 receptor responses: A possible role of S-nitrosation Br J Pharmacol. 1–14.
  • Hua G., Zein N., Daubeuf F. and P. Chambon (2019) Glucocorticoid receptor modulators CpdX and CpdX-D3 exhibit the same in vivo antiinflammatory activities as synthetic glucocorticoids Proc Natl Acad Sci U S A. 2019 Jun 21. pii: 201908258. DOI: 10.1073/pnas.1908258116.

2018

  • Frantz MC, Pellissier L, Pflimlin E, Loison S, Gandia J, Marsol C, Durroux T, Mouillac B, Becker J, Le Merrer J, Valencia C, Villa P, Bonnet D, Hibert M. (2018) LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. J. Med. Chem. 2018, 61, 8670−8692.
  •  Aviolat H, Nominé Y, Gioria S, Bonhoure A, Hoffmann D, Ruhlmann C, Nierengarten H, Ruffenach F, Villa P, Trottier Y and F Klein (2018) SynAggreg: a Multifunctional High-Throughput Technology for Precision Study of Amyloid Aggregation and Systematic Discovery of Synergistic Inhibitor Compounds. J Mol Biol 2018 430, 5257-79.
  • Regenass P, Abboud D, Daubeuf F, Lehalle C, Gizzi P, Riché S, Hachet-Haas M, Rohmer F, Gasparik V, Boeglin D, Haiech J, Knehans T, Rognan D, Heissler D, Marsol C, Villa P, Galzi JL, Hibert M, Frossard N, Bonnet D (2018) Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia J Med Chem 13;61(17):7671-7686.
  • Chen W., Nguekeu ZL, Dong J, Chézeau L, Inquimbert P, Hugel S, Niu S, Bihel F, Boutant E, Réal E, Villa P., Junier MP, Chneiweiss H, Hibert M, Haiech J, Kilhoffer MC, M Zeniou (2018) WNK1 kinase and its partners Akt, SGK1 and NBC-family Na+/HCO3- cotransporters are potential therapeutic targets for glioblastoma stem-like cells linked to Bisacodyl signaling. Oncotarget, 2018, Vol. 9, (No. 43): 27197-27219.
  • Hammoud H, Elhabazi K, Quillet R, Bertin I, Utard V, Laboureyras E, Bourguignon JJ, Bihel F, Simonnet G, Simonin F, Schmitt M. Aminoguanidine Hydrazone Derivatives as Nonpeptide NPFF1 Receptor Antagonists Reverse Opioid Induced Hyperalgesia.ACS Chem Neurosci. 2018 Nov 21;9(11):2599-2609. (Remerciements)
  • Heck S, Daubeuf F, Le DD, Sester M, Bonnet D, Bals R, Frossard N, Dinh QT (2018) Decreased Migration of Dendritic Cells into the Jugular-Nodose Ganglia by the CXCL12 Neutraligand Chalcone 4 in Ovalbumin-Sensitized Asthmatic Mice. Neuroimmunomodulation. 2017;24(6):331-340 Apr 20.
  • Drieu la Rochelle A, Guillemyn K, Dumitrascuta M, Martin C, Utard V, Quillet R, Schneider S, Daubeuf F, Willemse T, Mampuys P, Maes BUW, Frossard N, Bihel F, Spetea M, Simonin F, Ballet S (2018) A bifunctional biased mu opioid agonist - neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects. Pain. 2018 Sep;159(9):1705-1718.
  • Bollenbach M., Salvat E., Daubeuf F., Wagner P., Yalcin I., Humo M., Letellier B., Becker LJ., Bihel F., Bourguignon JJ., Villa P., Obrecht A., Frossard N., Barrot M., M. Schmitt (2018) Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation. European Journal of Medicinal Chemistry 147: 163-182.
  • Cam M, Durieu E, Bodin M, Manousopoulou A, Koslowski S, Vasylieva N, Barnych B, Hammock BD, Bohl B, Koch P, Omori C, Yamamoto K, Hata S, Suzuki T, Karg F, Gizzi P, Erakovic-Haber V, Bencetic Mihaljevic V, Tavcar B, Portelius E, Pannee J, Blennow K, Zetterberg H, Garbis SD, Auvray P, Gerber H, Fraering J, Fraering PC, Meijer L. (2018) Induction of Amyloid-β42 Production by Fipronil and Other Pyrazole Insecticides. J Alzheimers Dis. vol. 62, no. 4, pp. 1663-168.
  • Chakraborty M, Sellier C, Ney M, Villa P, Charlet-Berguerand N, Artero R, Llamusi B (2018) Daunorubicin reduces MBNL1 titration by expanded CUG repeat RNA and rescues cardiac dysfunctions in a Drosophila model of myotonic dystrophy. Disease Models & Mechanisms 2018 Apr 23;11(4).
  • Aulestia FJ, Néant I, Dong J, Haiech J, Kilhoffer MC, Moreau M, Leclerc C. (2018) Quiescence status of glioblastoma stem-like cells involves remodelling of Ca2+ signalling and mitochondrial shape. Sci Rep. 2018 Jun 27;8(1):9731.
  • Bouressam ML, Lartaud I, Dupuis F, Lecat S*. (2018) No answer to the lack of specificity: mouse monoclonal antibody targeting the angiotensin II type 1 receptor AT1 fails to recognize its target. Naunyn-Schmiedeberg’s Archives of Pharmacology. 391(8):883-889.
  • Feng Liwen, Don Antoine Lanfranchi, Leandro Cotos, Elena Cesar-Rodo, Katharina Ehrhardt, Alice-Anne Goetz,b Herbert Zimmermann, François Fenaille, Stephanie A. Blandin and Elisabeth Davioud-Charvet (2018) Synthesis of plasmodione metabolites and 13C-enriched plasmodione as chemical tools for drug metabolism investigation Org. Biomol. Chem., 2018, 16, 2647.

2017

  • Ayme-Dietrich, E., Lawson, R., Côté, F., de Tapia, C., Da Silva, S., Ebel, C., Hechler, B., Gachet, C., Guyonnet, J., Rouillard, H., Stoltz, J., Quentin, E., Banas, S., Daubeuf, F., Frossard, N., Gasser, B., Mazzucotelli, J.-P., Hermine, O., Maroteaux, L., and Monassier, L. (2017) Serotonergic 5-HT2B receptors in mitral valvulopathy: bone marrow mobilization of endothelial progenitors. British Journal of Pharmacology, doi: 10.1111/bph.13981.
  • Mouhsine H, Guillemain H, Moreau G, Fourati N, Zerrouki C, Baron B, Desallais L, Gizzi P, Ben Nasr N, Perrier J, Ratsimandresy R, Spadoni JL, Do H, England P, Montes M, Zagury JF (2017) Identification of an in vivo orally active dual-binding protein-protein interaction inhibitor targeting TNFα through combined in silico/in vitro/in vivo screening. Sci Rep. 2017 Jun 13;7(1):3424.
  • Elhabazi K, Humbert JP, Bertin I, Quillet R, Utard V, Schneider S, Schmitt M, Bourguignon JJ, Laboureyras E, Ben Boujema M, Simonnet G, Ancel C, Simonneaux V, Beltramo M, Bucher B, Sorg T, Meziane H, Schneider E, Petit-Demoulière B, Ilien B, Bihel F, Simonin  F (2017). RF313, an orally bioavailable neuropeptide FF receptor antagonist, opposes effects of RF-amide-related peptide-3 and opioid-induced hyperalgesia in rodents. Neuropharmacology 2017 May 15;118:188-198.
  • Ursuegui S, Recher M, Krężel W, Wagner A. (2017) An in vivo strategy to counteract post-administration anticoagulant activity of azido-Warfarin. Nat Commun. 2017 May 19;8:15242.
  • Gerbier R, Alvear-Perez R, Margathe JF, Flahault A, Couvineau P, Gao J, De Mota N, Dabire H, Li B, Ceraudo E, Hus-Citharel A, Esteoulle L, Bisoo C, Hibert M, Berdeaux A, Iturrioz X, Bonnet D, Llorens-Cortes C (2017).Development of original metabolically stable apelin-17 analogs with diuretic and cardiovascular effects. FASEB J. 2017 Feb;31(2):687-700.
  • Roeckel LA, Utard V, Reiss D, Mouheiche J, Maurin H, Robé A, Audouard E, Wood JN, Goumon Y, Simonin F, Gaveriaux-Ruff C Morphine-induced hyperalgesia involves mu opioid receptors and the metabolite morphine-3-glucuronide. Sci Rep. 2017 Sep 4;7(1):10406. doi: 10.1038/s41598-017-11120-4.
  • Daubeuf F, Becker J, Aguilar-Pimentel JA, Ebel C, Hrabě de Angelis M, Hérault Y, Frossard N (2017) A Fast, Easy, and Customizable Eight-Color Flow Cytometric Method for Analysis of the Cellular Content of Bronchoalveolar Lavage Fluid in the Mouse. Curr Protoc Mouse Biol. 2017 Jun 19;7(2):88-99.
  • Villa P. (2017) La miniaturisation pour la découverte de candidats médicaments. L’actualité chimique 418-419. 67-70.
  • García‐Palmero I., Pompas‐Veganzones N., Villalobo E., Gioria S., Haiech J., Villalobo A. The adaptors Grb10 and Grb14 are calmodulin‐binding proteins. FEBS Lett. 2017 Apr;591(8):1176-1186.
  • Schaeffer E., Haiech J., Galzi JL. (2017). New Culture Media for Fast, Sensitive and User-Friendly Detection of E.Coli and/or Coliform Bacteria. J. Microbiol Biotechnol Vol6/3 2017 : 50-61.
  • Valencia C., Dujet C., Margathe JF., Iturrioz X., Roux T., Trinquet E., Villa P., Hibert M., Dupuis E., Llorens-Cortes C., Bonnet D. (2017). Time-Resolved FRET Cell-Based Binding Assay For Apelin Receptor. ChemMedChem 2017, 12, 1-8.
  • Regenass P., Bosc D., Riché S., Gizzi P., Hibert M., Brelot L., Ganesan A., Bonnet, D. (2017) A Comparative Study of the Synthesis, Structural and Physicochemical Properties of Diketopiperazines vs Aza-Diketopiperazines J Org Chem. 2017 Mar 17;82(6):3239.
  • Dong J, Aulestia FJ, Assad Kahn S, Zeniou M, Dubois LG, El-Habr EA, Daubeuf F, Tounsi N, Cheshier SH, Frossard N, Junier MP, Chneiweiss H, Néant I, Moreau M, Leclerc C, Haiech J, Kilhoffer MC. (2016) Bisacodyl and its cytotoxic activity on human glioblastoma stem-like cells. Implication of inositol 1,4,5-triphosphate receptor dependent calcium signaling. Biochim Biophys Acta. 2017 Jun;1864(6):1018-1027.

2016

  • Le DD, Schmit D, Heck S, Omlor AJ, Sester M, Herr C, Schick B, Daubeuf F, Fähndrich S, Bals R, Frossard N, Al Kadah B, Dinh QT. (2016) Increase of Mast Cell-Nerve Association and Neuropeptide Receptor Expression on Mast Cells in Perennial Allergic Rhinitis. Neuroimmunomodulation. 2016 ;23(5-6):261-270.
  • Doebelin C, Bertin I, Schneider S, Schmitt M, Bourguignon JJ, Ancel C, Simonneaux V, Simonin F, Bihel F.Development of Dipeptidic hGPR54 Agonists. ChemMedChem. 2016 Oct 6;11(19):2147-2154.
  • Assad Kahn S, Costa SL, Gholamin S, Nitta RT, Dubois LG, Fève M, Zeniou M, Coelho PL, El-Habr E, Cadusseau J, Varlet P, Mitra SS, Devaux B, Kilhoffer MC, Cheshier SH, Moura-Neto V, Haiech J, Junier MP, Chneiweiss H.(2016) The anti-hypertensive drug prazosin inhibits glioblastoma growth via the PKCδ-dependent inhibition of the AKT pathway. EMBO Mol Med.8(5):511-26.
  • Karpenko IA, Niko Y, Yakubovskyi VP, Gerasov AO, Bonnet D, Kovtun YP, Klymchenko AS. Push-pull dioxaborine as fluorescent molecular rotor: far-red fluorogenic probe for ligand-receptor interactions. J Mater Chem C Mater Opt Electron Devices. 2016 Apr 14;4(14):3002-3009 26.
  • Guillemyn K, Starnowska J, Lagard C, Dyniewicz J, Rojewska E, Mika J, Chung NN, Utard V, Kosson P, Lipkowski AW, Chevillard L, Arranz-Gibert P, Teixidó M, Megarbane B, Tourwé D, Simonin F, Przewlocka B, Schiller PW, Ballet S. Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain. J Med Chem. 2016 Apr 28;59(8):3777-92.
  • Houel E, Nardella F, Julliand V, Valentin A,  Vonthron-Senecheau C Villa, P., Obrecht A., Kaiser M., Bourreau E., Odonne G, Fleury M, Bourdy G, Eparvier V., Deharo E. and D. Stien (2016). Wayanin and guaijaverin, two active metabolites found in a Psidium acutangulum Mart. ex DC (syn. P. persoonii McVaugh) (Myrtaceae) antimalarial decoction from the Wayana Amerindians. J. of Ethnopharmacology 187: 241-48.
  • Nemska S, Daubeuf F & N Frossard (2016) Revascularization of the graft in obliterative bronchiolitis after heterotopic tracheal transplantation Physiological reports Vol. 4 | Iss. 4 | e12690

2015

  • Flacher V, Neuberg P, Point F, Daubeuf F, Muller Q, Sigwalt D, Fauny JD, Remy JS, Frossard N, Wagner A, Mueller CG, Schaeffer E. (2015) Mannoside Glycolipid Conjugates Display Anti-inflammatory Activity by Inhibition of Toll-like Receptor-4 Mediated Cell Activation. ACS Chem Biol.
  • Guilini C, Baehr C, Schaeffer E, Gizzi P, Rufi F, Haiech J, Weiss E, Bonnet D, Galzi JL.(2015)  New fluorescein precursors for live bacteria detection. Anal Chem. 2015 87(17):8858-66.
  • Abboud D, Daubeuf F, Do QT, Utard V, Villa P, Haiech J, Bonnet D, Hibert M, Bernard P, Galzi JL, and N Frossard (2015) A strategy to discover decoy chemokine ligands with an anti-inflammatory activity. Scientific Reports 2015;5:14746.
  • Zeniou M, Fève M, Mameri S, Dong J, Salomé C, Bousson F, El-Habr EA, Sy M, Obszynski J, Boh A, Villa P, Kahn SA, Didier B, Bagnard D, Junier MP, Chneiweiss H, Haiech H, Hibert M and MC Kilhoffer (2015) Chemical library screening and structure-function relationship studies identify bisacodyl as a potent and selective cytotoxic agent towards quiescent human glioblastoma tumor stem-like cells. PlosOne PLoS ONE 09/2015; 10(8): e013479.
  • Daubeuf F, Jung F, Douglas GJ, Chevalier E, Frossard N. (2015) Protective effect of a Protein Epitope Mimetic CCR10 antagonist, POL7085, in a model of allergic eosinophilic airway inflammation. Respir Res. 27;16:77.
  • Galzi JL, Ruggiu F, Gizzi P, Didier B (2015) Quality control of chemical libraries. Med Sci (Paris) 31(6-7):660-6.
  • Karpenko I, Collot M, Richert L, Valencia C, Villa P, Mély Y, Hibert M, Bonnet D, Klymchenko A (2015) Fluorogenic squaraine dimers with polarity-sensitive folding as bright far-red probes for background-free bioimaging. J Am Chem Soc. 137(1):405-12.
  • Rouméas L, Humbert JP, Schneider S, Doebelin C, Bertin I, Schmitt M, Bourguignon JJ, Simonin F, Bihel F. Effects of systematic N-terminus deletions and benzoylations of endogenous RF-amide peptides on NPFF1R, NPFF2R, GPR10, GPR54 and GPR103. Peptides. 2015 Sep;71:156-61.
  • Karpenko I. A., Klymchenko A., Gioria, S. Kreder, S. Shulov, R I. Villa, P. Mély Y., Hibert M. and D. Bonnet (2015) Squaraine as a bright, stable and environment-sensitive far-red label for receptor-specific cellular imaging. Chem. Commun. 51(14):2960-3.
  • Hamdi A, Lesnard A, Suzanne P, RobertT, Miteva MA, Pellerano M, Didier B, Ficko-Blean E, Lobstein A, Hibert M, Rault S, Morris MC and P Colas (2015) Tampering with Cell Division by Using Small-Molecule Inhibitors of CDK–CKS Protein Interactions. Chembiochem 2015 Feb 9;16(3):432-9.
  • Houel E, Fleury M, Odonne G, Nardella F, Bourdy G, Vonthron-Senecheau C, Villa, P., Obrecht A. Eparvier V. Deharo E. and D. Stien (2015) Antiplasmodial and anti-inflammatory effects of an antimalarial remedy from the Wayana Amerindians, French Guiana: Takamalaimë (Psidium acutangulum Mart. Ex DC., Myrtaceae) J. of Ethnopharmacology 166; 279–285.
  • Mailly L, Xiao F, Lupberger J,  Wilson G K, Aubert P, Duong PHT, Calabrese D, Leboeuf C, Fofana I, Thumann C, Bandiera S, Lütgehetmann M, Volz T, Davis C,  Harris HJ, Mee C, Girardi E, Chane-Woon-Ming B, Ericsson M, Fletcher N, Bartenschlager R, Pessaux P, Vercauteren K, Meuleman P, Villa P, Kaderali L, Pfeffer S, Heim MH, Neunlist M, Zeisel MB, Dandri M, McKeating JA, Robinet E and Baumert TF (2015) Clearance of persistent hepatitis C virus infection using a monoclonal antibody specific for tight junction protein claudin-1. Nature Biotech 33(5):549-54.
  • Zirafi O, Kim KA, Ständker L, Mohr KB, Sauter D, Heigele A, Kluge SF, Wiercinska E, Chudziak D, Richter R, Moepps B, Gierschik P, Vas V, Geiger H, Lamla M, Weil T, Burster T, Zgraja A, Daubeuf F, Frossard N, Hachet-Haas M, Heunisch F, Reichetzeder C, Galzi JL, Pérez-Castells J, Canales-Mayordomo A, Jiménez-Barbero J, Giménez-Gallego G, Schneider M, Shorter J, Telenti A, Hocher B, Forssmann WG, Bonig H, Kirchhoff F, Münch J. Discovery and characterization of an endogenous CXCR4 antagonist. Cell Report 2015, 11(5): 737-47.
  • Beck IM, Van Crombruggen K, Holtappels G, Daubeuf F, Frossard N, Bachert C, De Bosscher K. Differential Cytokine Profiles upon Comparing Selective versus Classic Glucocorticoid Receptor Modulation in Human Peripheral Blood Mononuclear Cells and Inferior Turbinate Tissue. PLoSOne 2015, 10(4).
  • Tavakoli R, Auf der Maur C, Mueller X, Schläpfer R, Jamshidi P, Daubeuf F, Frossard N. Full-root aortic valve replacement with stentless xenograft achieves superior regression of left ventricular hypertrophy compared to pericardial stented aortic valves. J Cardiothorac Surg 2015, 10(1): 15.

2014

  • Maletta M, Orlov I, Roblin P, Beck Y, Moras D, Billas IM, Klaholz BP. (2014) The palindromic DNA-bound USP/EcR nuclear receptor adopts an asymmetric organization with allosteric domain positioning. Nat Commun. 5:4139.
  • Margathe JF, Iturrioz X, Alvear-Perez R, Marsol C, Riché S, Chabane H, Tounsi N, Kuhry M, Heissler D, Hibert M, Llorens-Cortes C and D Bonnet (2014) Structure-Activity Relationship Studies toward the Discovery of Selective Apelin Receptor Agonists. J Med Chem. 57(7): 2908-19.
  • Houel, E. Fleury, M. Jullian, V Vonthron-Senecheau, C. Nardella, F. Villa, P. Odonne, G. Eparvier, V Deharo, E. Stien, D. (2014) Takamalalme (Psidium acutangulum Mart ex. DC): Understanding the use of an antimalarial traditional remedy from French Guiana. Planta Medica 80(10) 797.
  • Ruggiu F, Gizzi P, Galzi JL, Hibert M, Haiech J, Baskin I, Horvath D, Marcou G, and A Varnek (2014) QSPR modelling – a valuable support in HTS quality control. Analytical Chemistry.86(5):2510-20.
  • Karpenko I.A., Kreder R., Valencia C., Villa P., Mendre C., Mouillac B., Mély Y., Hibert M., Bonnet D. and Klymchenko A. S. (2014), Red Fluorescent Turn-On Ligands for Imaging and Quantifying G Protein-Coupled Receptors in Living Cells. ChemBioChem. 15: 359-363.
  • F. Daubeuf, N. Frossard. Eosinophils and the Ovalbumin Mouse Model Of Asthma. In: Methods Mol Biol 2014; 1178: 283-9.
  • L.L. Reber, F. Daubeuf, Pejler G, Abrink M, Frossard N. Mast Cells Contribute to Bleomycin-Induced Lung Inflammation and Injury in Mice through a Chymase/Mast Cell Protease 4-Dependent Mechanism. J Immunol 2014; 192(4): 1847-54.
  • MA. Benahmed, K. Elbayed, F. Daubeuf, N. Santelmo, N. Frossard, IJ. Namer. NMR HRMAS spectroscopy of lung biopsy samples: Comparison study between human, pig, rat, and mouse metabolomics. Magn Reson Med 2014; 71(1): 35-43.
  • Ray AM, Schaffner F, Janouskova H, Rognan D, Lelong-Rebel I, Choulier L, Blandin AF, Lehmann M, Martin S, Kapp T, Neubauer S, Rechenmacher F, Kessler H, Dontenwill M. (2014) Single cell tracking assay reveals an opposite effect of selective small non-peptidic α5β1 or αvβ3/β5 integrin antagonists in U87MG glioma cells. BBActa 1840: 2978-87.
  • 10   Michel G, Matthes HW, Hachet-Haas M, El Baghdadi K, de Mey J, Pepperkok R, Simpson JC, Galzi JL, Lecat S. Plasma membrane translocation of REDD1 governed by GPCRs contributes to mTORC1 activation. J Cell Sci. 2014 Feb 15;127(Pt 4):773-87.

2013

  • Audran E, Dagher R, Gioria S, Kilhoffer MC, Haiech J. (2013) New aspects of calmodulin-calmodulin binding domains recognition. Methods Mol Biol. 963:57-72.
  • Audran E, Dagher R, Gioria S, Tsvetkov PO, Kulikova AA, Didier B, Villa P, Makarov AA, - Kilhoffer MC, Haiech J. (2013) A general framework to characterize inhibitors of Calmodulin: Use of calmodulin inhibitors to study the interaction between calmodulin and its calmodulin binding domains. Biochim Biophys Acta. MCR ; 1833(7):1720-31.
  • Daubeuf F, Hachet-Haas M, Gizzi P, Gasparik V, Bonnet D, Utard V, Hibert M, Frossard N, Galzi JL. (2013) An antedrug of the CXCL12 neutraligand blocks experimental allergic asthma without systemic effect in the mouse. J Biol Chem. 288(17):11865-76.
  • Elhabazi K,  Humbert JP, Bertin I, Schmitt M, Bihel F,  Bourguignon JJ, Bucher B,  Becker JAJ, Sorg T, Meziane H, Petit-Demoulière B Ilien B, Simonin F. (2013) Endogenous mammalian RF-amide peptides, including PrRP, kisspeptin and 26RFa, modulate nociception and morphine analgesia via NPFF receptors Neuropharmacology (75) 164–171.
  • Michel G, Matthes HW, Hachet-Haas M, El Baghdadi K, de Mey J, Pepperkok R, Simpson JC, Galzi JL, Lecat S. (2013) Plasma membrane translocation of REDD1 governed by GPCRs contributes to mTORC1 activation. J Cell Sci. 15;127(Pt 4):773-87.
  • F. Daubeuf, N. Frossard. Acute Ovalbumin Asthma Model In The Mouse. Current Protocols in Mouse Biology 2013; 3:31–37.
  • Anton, M. Atzenhoffer, F. Daubeuf, X. Li, V.B. Schini-Kerth, B. Delmotte, T.F. Vandamme, T. Chataigneau. Do iodinated nano-emulsions designed for preclinical vascular imaging alter the endothelial function in rat aorta? Int J Pharm 2013; 454(1): 143-148.

2012

  • Daval SB, Valant C, Bonnet D, Kellenberger E, Hibert M, Galzi JL, Ilien B. Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding  mechanisms on muscarinic M1 receptors. J Med Chem. 2012 Mar 8;55(5):2125-43.
  • Kümmerle AE, Schmitt M, Cardozo SV, Lugnier C, Villa P, Lopes AB, Romeiro NC, Justiano H, Martins MA, Fraga CA, Bourguignon JJ, Barreiro EJ. Design, Synthesis and Pharmacological Evaluation of N-acylhydrazones (NAH) and Novel Conformationally Constrained Compounds as Selective and Potent Orally Active PDE4 Inhibitors. J Med Chem. 2012 Sep 13;55 (17):7525-45.
  • Zeder-Lutz G, Choulier L, Besse M, Cousido-Siah A, Ruiz Figueras FX, Didier B, Jung ML, Podjarny A, Altschuh D. (2012) Validation of surface plasmon resonance screening of a diverse chemical library for the discovery of protein tyrosine phosphatase 1b binders Anal Biochem. 2012 Feb 15; 421 (2):417-27.
  • F. Daubeuf, Frossard N. Performing Bronchoalveolar Lavage in the Mouse. Current Protocols in Mouse Biology 2012; 2: 167-175N.
  • V. Gasparik, F. Daubeuf, M. Hachet-Haas, F. Rohmer, P. Gizzi, J. Haiech, JL. Galzi, M. Hibert, D. Bonnet, N. Frossard. Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo. ACS Med Chem Lett 2012, 3 (1), pp 10–14.
  • L.L. Reber, F. Daubeuf, N. Frossard. The AGC kinase inhibitor attenuates airway inflammation in mouse models of asthma. PloSOne, 2012;7(11): e49512.
  • L.L. Reber, F. Daubeuf, M. Plantinga, L. De Cauwer, S. Gerlo, W. Waelput, S. Van Calenbergh, J. Tavernier, G. Haegeman, BN. Lambrecht, N. Frossard, K. De Bosscher. A dissociated glucocorticoid receptor modulator reduces airway hyperresponsiveness and inflammation in a mouse model of asthma. J Immunol 2012; 188(7): 3478-87.

2011

  • J Proudfoot, O Nosjean, J Blanchard, J Wang, D Besson, D Crankshaw, G Gauglitz R Hertzberg, C Homon, L Llewellyn, R Neubig, L Walker, and P Villa. (2011) Glossary of terms used in biomolecular screening (IUPAC Recommendations 2011) Pure Appl. Chem; 83(5): 1129-1158.
  • Weill N., Valencia C., Gioria S., Villa P., Hibert M. and D. Rognan (2011) Identification of non peptide Oxytocin receptor ligands by receptor-ligand fingerprint similarity research. Molecular Informatics 30: 521-526.
  • Dagher R, Peng S, Gioria S, Fève M, Zeniou M, Zimmermann M, Pigault C, Haiech J, Kilhoffer MC.A general strategy to characterize calmodulin-calcium complexes involved in CaM-target recognition: DAPK and EGFR calmodulin binding domains interact with different calmodulin-calcium complexes. Biochim Biophys Acta. 2011 May;1813(5):1059-67.
  • M. Hachet-Haas, D. Bonnet, F. Daubeuf, M. Hibert, J. Haiech, N. Frossard, JL. Galzi. Les neutraligands à l’assaut des chimiokines. Biofutur 2011; no319, pp. 52-55.

2010

  • Frantz MC, Rodrigo J, Boudier L, Durroux T, Mouillac B, Hibert M. Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. J Med Chem. 2010 Feb 25;53(4):1546-62.
  • Kuhn I, Kellenberger E, Said-Hassane F, Villa P, Rognan D, Lobstein A, Haiech  J, Hibert M, Schuber F, Muller-Steffner H. Identification by high-throughput screening of inhibitors of Schistosoma mansoni NAD(+) catabolizing enzyme. Bioorg Med Chem. 2010 Nov 15;18(22):7900-10. Epub 2010 Sep 25. PubMed PMID: 20951593.
  • Zimmermann M, Atmanene C, Xu Q, Fouillen L, Van Dorsselaer A, Bonnet D, Marsol C, Hibert M, Sanglier-Cianferani S, Pigault C, McNamara LK, Watterson DM, Haiech J, Kilhoffer MC. Homodimerization of the death-associated protein kinase catalytic domain: development of a new small molecule fluorescent reporter. PLoS One. 2010 Nov 30;5(11):e14120.
  • JL. Galzi, M. Hachet-Haas, D. Bonnet, F. Daubeuf, S. Lecat, M. Hibert, J. Haiech, N. Frossard. Neutralizing endogenous chemokines with small molecules. Principles and potential therapeutic applications. Pharmacol Ther 2010; 126(1): 39-55. Review.

2009

  • Iturrioz X, Alvear-Perez R, De Mota N, Franchet C, Guillier F, Leroux V, Dabire H, Le Jouan M, Chabane H, Gerbier R, Bonnet D, Berdeaux A, Maigret B, Galzi JL, Hibert M, Llorens-Cortes C. Identification and pharmacological properties of E339-3D6, the first nonpeptidic apelin receptor agonist. FASEB J. 2010 May;24(5):1506-17.
  • Dagher R, Brière C, Fève M, Zeniou M, Pigault C, Mazars C, Chneiweiss H, Ranjeva R, Kilhoffer MC, Haiech J. Calcium fingerprints induced by calmodulin interactors in eukaryotic cells. Biochim Biophys Acta. 2009 Jun;1793(6):1068-77.
  • Shvadchak V, Sanglier S, Rocle S, Villa P, Haiech J, Hibert M, Van Dorsselaer  A, Mély Y, de Rocquigny H. Identification by high throughput screening of small compounds inhibiting the nucleic acid destabilization activity of the HIV-1 nucleocapsid protein. Biochimie. 2009 Jul;91(7):916-23.
  • Calmels N, Seznec H, Villa P, Reutenauer L, Hibert M, Haiech J, Rustin P, Koenig M, Puccio H. Limitations in a frataxin knockdown cell model for Friedreich ataxia in a high-throughput drug screen. BMC Neurol. 2009 Aug 24;9:46.
  • Hibert MF. French/European academic compound library initiative. Drug Discov Today. 2009 Aug;14(15-16):723-5.
  • Betzi S, Eydoux C, Bussetta C, Blemont M, Leyssen P, Debarnot C, Ben-Rahou M, Haiech J, Hibert M, Gueritte F, Grierson DS, Romette JL, Guillemot JC, Neyts J, Alvarez K, Morelli X, Dutartre H, Canard B. Identification of allosteric inhibitors blocking the hepatitis C virus polymerase NS5B in the RNA synthesis initiation step. Antiviral Res. 2009 Oct;84(1):48-59.
  • Valant C, Maillet E, Bourguignon JJ, Bucher B, Utard V, Galzi JL, Hibert M. Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration. J Med Chem. 2009 Oct 8;52(19):5999-6011.