• Equipe Biotechnologie et signalisation cellulaire
• UMR 7242
• ESBS - 300 Bld S Brant
• 67 412 Illkirch
• Tél : +33 3 68 85 47 59
• Tél : +33 6 68 02 84 21
• Email : galzi@unistra.fr
• Site internet : irebs.fr

Equipe

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• TechMedIll - UMR 7242 - Illkirch

Brevets / Publications / Communications

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Palanche, T., Ilien, B., Zoffmann, S., Reck, M.P., Bucher, B., Edelstein, S., Galzi, J.L.(2001) Dual responses and desensitization of the NK2 tachykinin receptor are mediated by multiple conformational states as revealed by rapid kinetic measurements. J.Biol. Chem 276, 34853-34861

Lecat, S., Bucher, B., Mely, Y. and Galzi, J.L.(2002) Mutations in the extracellular amino-terminal domain of the NK2 neurokinin receptor abolish cAMP signaling but preserve intracellular calcium responses, J. Biol. Chem 277, 42034-42048

Ilien,B., Franchet, C., Bernard, P, Morisset, S., Weill, C., Bourguignon J.-J., Hibert, M. & Galzi, J.L. (2003) Fluorescence resonance energy transfer to probe human muscarinic receptor structure and drug binding properties J. Neurochem 85, 768-778.

Tahtaoui, C., Parrot, I., Klotz, P., Guillier, F., Galzi, J.L., Hibert, M., Ilien, B. (2004) Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor. J. Med. Chem. 47, 4300-4315.

 Cézanne, L., Lagane, B., Lecat, S., Millot, C. Vollmer, J.Y., Matthes, H. Galzi, J.L.and Lopez, A. (2004) Dynamic confinement of the NK2 receptors : improved FRAP analysis and biological relevance. J. Biol. Chem. 43, 45057-45067.

Tahtaoui, C., Guillier, F., Klotz, P., Galzi, J.L., Hibert, M., Ilien, B. (2005) On the use of non fluorescent dye-labeled ligands in FRET-based receptor binding studies. J. Med. Chem 48, 7847-7859.

Galzi JL, Maillet E., Lecat S, Hachet-Haas M, Haiech J, Hibert M, Ilien, B. (2006) Allosteric properties and regulation of G protein-coupled receptors. In “Ligand-design for GPCRs, Volume 30” Wiley eds. Pp 99-114.

Haiech J., JL Galzi, MC Kilhoffer, M. Hibert & D. Rognan. « Why G protein-coupled receptors databases are needed ». In “Ligand-design for GPCRs, Volume 30” Wiley eds. pp 27-38, 2006

Bonnet D., B. Ilien, J.L. Galzi, S. Riche, C. Antheaume and M. Hibert. A Rapid and Versatile Method to Label Receptor Ligands Using “Click” Chemistry: Validation with the Muscarinic M1 Antagonist Pirenzepine (2006) Bioconjugate Chem. 17, 1618-1623

Kellenberger, E., Springael, JY, Parmentier, M., Hachet-Haas, M., Galzi, J.L., Rognan, D. (2007) Identification of CCR5 non-peptide agonists using structure-base virtual screening. J. Med. Chem. 50, 1294-1303.

Zoffmann, S., Bertrand S., Do, Q.T., Bertrand D., Rognan, D., Hibert M., Galzi J.L. Topological analysis of the complex formed between Neurokinin A and the NK2 tachykinin receptor (2007) J. Neurochem. 101, 506-516.

Maillet E, N. Pellegrini, C Valant, B. Bucher, M. Hibert, J.J. Bourguignon and J.L. Galzi. (2007). A novel conformation-specific allosteric inhibitor of the tachykinin NK2 receptor with functionally selective properties FASEB J. vol 21, 2124-2134.

Ouédraogo, M., Lecat, S., Rochdi, M.D., Hachet-Haas, M., Matthes, H., Gicquiaux, H., Verrier, S., Gaire, M., Glasser, N., Mély, Y., Takeda, K., Bouvier, M., Galzi, J.L. and Bucher, B. (2008) Distinct motifs of neuropeptide Y receptors differentially regulate trafficking and desensitization, Traffic, 9, 305-324.

Hachet-Haas M., Balabanian K., Rohmer F., Pons F., Franchet C., Lecat S., Chow KYC, Dagher R., Gizzi P., Didier B., Lagane B., Kellenberger E., Bonnet D., Baleux F., Haiech J., Parmentier M., Frossard N., Arenzana-Seisdedos F., Hibert M, Galzi J.-L.(2008) Small neutralizing molecules to inhibit actions of the chemokine CXCL12. J. Biol. Chem. Vol. 283, 23189-23199.

JP Changeux, A Devillers-Thiéry, JL Galzi, F Revah (2008) The acetylcholine receptor: a model of an allosteric membrane protein mediating intercellular communication. Interactions Among Cell Signalling Systems, 745, page 66.

Ilien, B., Glasser, N., Clamme, J.P., Didier, P., Piemont, E. Chinnappan, R., Daval, S.B., Galzi, J.L., Mely, Y. (2009) Pirenzepine promotes the dimerization of muscarinic M1 receptors through a three-step binding process J. Biol. Chem. 284, 19533-19543.

Valant, C., Maillet, E., Bourguignon, J.J., Bucher, B., Utard, V., Galzi, J.L., Hibert, M. (2009) Allosteric Functional Switch of Neurokinin A-mediated Signalling at the Neurokinin NK2 Receptor: Structural Exploration. J. Med. Chem. 52, 5999-6011.

Galzi JL., Hachet-haas M., Bonnet D., Lecat, S., Hibert M., Haiech J., Daubeuf F., Frossard N. (2010). Neutralising endogeneous chemokines with small molecules: Principles and potential therapeutic applications, Pharmacol. Ther. 126, 39-55.

Iturrioz, X., Alvear-Perez, R., De Mota, N., Franchet, C., Guillier, F., Leroux, V., Dabire, H., Le Jouan, M.,Chabane, H., Bonnet, D., Berdeaux, A., Maigret, B., Galzi, J.L., Hibert, M., Llorens-Cortes, C. (2010) Identification and Characterization of E339-3D6, the First Non Endogenous Apelin Receptor Agonist. Faseb, J. 2010 24: 1506-1517.

 De Mota, N., Iturrioz, X., Alvear, R., Reaux, A., Chartrel, N., Bonnet, D., Dabire, H., Gerbier, R., Berdeaux, A., Moos, F., Maigret, B., Galzi, J-L., Hibert, M., Vaudry, H., Llorens-Cortes, C. (2010) The apelin receptor: from ligand discovery to physiological role. Regul. Pept.: 164   Issue: 1   Special Issue: Sp. Iss. SI   Pages: 26-26.

Perez, AR., Iturrioz, X., de Mota, N., Franchet, C., Guillier, F., Le Jouan, M., Chabane, H., Gerbier, R., Bonnet, D., Galzi, J. L., Hibert, M., Cortes, Llorens C. (2010) identification and characterization of E339-3D6, the first non peptidic apelin receptor agonist. Hypertension: 54 Issue: 5 Pages: 1177-1177.

Lecat S., Ouédraogo M., Cherrier T., Noulet F., Rondé P., Glasser N. Galzi J.L., Mely Y.,Takeda K., Bucher B. (2010) Contribution of a tyrosine-based motif to cellular trafficking of wild type and truncated NPY Y1 receptors Cell. Signal. Volume 23, Pages 228-238

Chow, K.Y.C., Brotin, E., Ben Khalifa Y., Carthagena, L., Teissier, S., Danckaert, A., Galzi, J.L., Arenzana-Seisdedos, F., Thierry, F. and Bachelerie, F. (2010), functional interplay between human papillomavirus (HPV) and the CXCL12-signaling axis in transformation of keratinocytes. Cell Host&Microbes Volume 8, Issue 5, 523-533.

Daubeuf, F., Gasparik, V., Hachet-Haas, M., Rohmer, F., Gizzi, P., Haiech, J., Galzi, J.-L., Hibert, M., Bonnet, D., Frossard, N. (2011) Activity of soluble CXCL12 neutraligands in vivo in a short model of asthma. Inflammation research, 60, 112-113.

Hachet-Haas, M., Bonnet D., Daubeuf F., Hibert M., Haiech J., Frossard N., Galzi J.L. (2011) Les neutraligands à l'assaut des chimiokines BIOFUTUR, 319, 52-55.

Andersson, D.A., C. Gentry, L. Alenmyr, D. Killander, S.E. Lewis, A. Andersson, B. Bucher, J.-L. Galzi, O.Sterner, S. Bevan, E. D, Högestätt P.M. Zygmunt (2011). TRPA1 mediates spinal antinociception induced by acetaminophen and the cannabinoid Δ9-tetrahydrocannabiorcol, Nature Communications 2:551 doi:10.1038/ncomms1559 (2011).

Gasparik, V., Daubeuf, F. Hachet-Haas, M., Rohmer, F., Gizzi, P., Haiech, J., Galzi, J.L., Hibert, M., Bonnet, D., Frossard, N. (2012) Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo , ACS Med Chem Letters, 3, 10-14.

Daval SB, Valant C, Bonnet D, Hibert M, Galzi JL and Ilien  B (2012) Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors. J.Med. Chem. 2012, 55 (5), pp 2125–2143. DOI: 10.1021/jm201348t

Bouchery T., Dénécé, G., Attout, T., Eberhard, K., Lhermitte-Vallarino, N., Galzi, J.L., Bachelerie, F., Brotin E., Gavotte, L., Moulia, C., Bain, O., Martin, C. (2012) The development and the survival of the filaria Litomosoides sigmodontis in mouse is dependent on the CXCL12/CXCR4 axis. PLOS one;7(4):e34971. Epub 2012 Apr 12.

Galzi, JL., Haas, M., Frossard, N., Hibert, M. (2012) Why and how to find neutraligands targeting chemokines? Drug Discovery Today: Technologies, Volume 9, Issue 4, Winter 2012, Pages e245-e251

Galzi, JL, Ilien, B (2012) GPCRs: allosteric regulators of cell metabolism. Medecine/Science October issue

Daubeuf, F.*, Hachet-Haas, M.*, Gizzi, P., Gasparik, V., Bonnet, D., Hibert, M., Frossard, N., Galzi, JL. (*equal first authors) (2013). antedrugs of the chemokine CXCL12 neutraligand show selectivity in an in vivo model of asthma J. Biol. Chem. 288, 11865-11876

Daval, S. Kellenberger,  E., Bonnet, D., Utard, V., Galzi, JL., Ilien, B. (2013) Exploration of the orthosteric/allosteric interface in human M1 muscarinic receptors by bitopic fluorescent ligands. Mol. Pharmacol. 84:71–85.

Michel, G., H W.D. Matthes, M Hachet-Haas, K El Baghdadi, J de Mey, R Pepperkok, J C. Simpson, J-L Galzi, and S Lecat. (2014) Plasma membrane translocation of REDD1 governed by GPCRs contributes to mTORC1 activation. J. Cell Sci. .127: 773-787.  doi:10.1242/jcs.136432

Romain, B. Hachet-Haas, M., Rohr, S., Brigand, C., Galzi, JL. Gaub, MP., Pencreach E., Guenot, D. (2014) Differential regulation of CXCL12 signaling by CXCR4 and CXCR7 in colon cancer in hypoxic conditions. Molecular Cancer, 2014, 13:58 (14 March 2014)

Ruggiu, F.*, Gizzi, P.*, Galzi, JL., Hibert, M., Haiech, J.,  Baskin, I., Horvath, D., Marcou G., Varnek A. (2014) QSPR modelling – a valuable support in HTS quality control, Analytical chemistry, 86 (5), pp 2510–2520

S Lecat, L Belemnaba, J-L Galzi, B. Bucher. (2015) Neuropeptide Y receptor mediates ERK1/2 activation via transactivation of the IGF receptor, Cellular signaling Volume 27, Issue 7, July 2015, Pages 1297-1304.

Zirafi, O., Kim, KE., Ständker, L., Mohr, K., Sauter, D., Heigele, A., Kluge, S.F., Wiershinska, E., Chudziak, D., Richter, R., Möpps, 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, J.L., Perez-Castells, J., Canales-Mayordomo, A., Jiménez-Barbero, J., Giménez-Gallego, G., Schneider, M., Shorter, J., Telenti, A., Hocher, B., Forssmann, W.G., Boenig, H., Kirchhoff, F., Münch, J. (2015) Discovery and characterization of a natural CXCR4 antagonist, Cell Reports 11, 737-747.

Sandra Lecat, Hans W. D. Matthes, Rainer Pepperkok, Jeremy C. Simpson, and Jean-Luc Galzi (2015) A fluorescent live imaging screening assay based on translocation criteria identifies novel cytoplasmic proteins implicated in GPCR signalling pathways. (2015) Mol Cell Proteomics. 2015 May;14(5):1385-99. doi: 10.1074/mcp.M114.046698. Epub 2015 Mar 10. PMID:25759509

Galzi, JL, Ruggiu, F., Gizzi, P., Didier, B. (2015) Contrôle qualité des chimiothèques, Medecine/Science,31, 660-666.

Abboud, D., Villa, P., Daubeuf, F., Utard, V., Haiech, J., Bonnet, D., Hibert, M., Bernard, P., Galzi, J.L.*, Frossard, N.* (2015) A strategy to discover decoy chemokine ligands with an anti-inflammatory activity, Sci Rep. 2015 Oct 7;5:14746. doi: 10.1038/srep14746

Guilini, C., Schaeffer, E., Baehr, C., Gizzi, P., Rufi, F., Haiech J., Weiss, E., Bonnet, D., Galzi, J.L. (2015) improved precursor of fluorescein for live bacteria detection Anal Chem. 2015 Sep 1;87(17):8858-66. doi: 10.1021/acs.analchem.5b02100. Epub 2015 Aug 20.

- Europe patent n° 0 986 759 (26 april 2006) French Patent n° 97.06977 (5 june 1997) for: "On the use of a fluorescent protein to detect target protein ligand interactions. Inventors: Galzi, J.L. & ALix P.

Europe patent n° 1 514 112 (6 september 2006) and French patent n° 2 840 993 (8 april 2005) : « new process to identify allosteric effectors», inventors: Galzi, J.L., Maillet, E., Hibert, M., Bourguignon, J.J.

French Patent n° 2 871 465 (8 september 2006) for "collections of traceable compounds and uses thereof» C Franchet, JL Galzi, F Guillier, M Hibert, F Pattus. WO2006003330, 12 janvier 2006

French Patent n° 2 871 464 (8 september 2006) for "process for ligands of biological macromolecules using fluorescence transfer of collections of traceable molecules" Inventors : C Franchet, JL Galzi, F Guillier, M Hibert, F Pattus WO2006003329, 12 january 2006

Frossard, N., Haiech, J., Lehalle, C., Kessler, R., Magnan, A., Chanez, P. Galzi, JL. Biomarqueur pour les maladies inflammatoires pulmonaires chroniques. FRA 1250917, déposé le 31 janvier 2012. Extension internationale Europe le 5/09/2014.

Galzi, JL., Abboud, D., Frossard, N., Do, Q.T., Bernard, P. Composition contenant au moins un inhibitieur de certaines chimiokines, son procédé d’obtention et son utilisation en dermocosmétique pharmaceutique (INPI 14/02163, septembre 2014)

Galzi, JL., Abboud, D., Frossard, N., Do, Q.T., Bernard, P. Composition contenant au moins un inhibitieur de certaines chimiokines, son procédé d’obtention et son utilisation en dermocosmétique pharmaceutique (INPI 14/02162, septembre 2014)

Galzi, JL, Bonnet, D., Lelant, C. (2015) Fluorescent Dyes and Dye Precursors.  European Patent Appliction No. 15143463.3