• Publications

  • General public

  • Scientific Advisory Board:
    Francesco Barrantes and Angela Vincent
  • Relevant publications

    List of relevant publications

    leading up to the Neurocypres consortium:

    Partner 1: Vrije Universiteit Amsterdam (VUA), Center for Neurogenomics & Cognitive Research (CNCR), The Netherlands.

    Prof. dr. A.B. Smit

    1. Brejc K, van Dijk WJ, Klaassen RV, Schuurmans M, van Der Oost J, Smit AB, Sixma TK. Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nAChRs. Nature (2001) 411:269-76.
    2. Smit AB, Syed NI, Schaap D, van Minnen J, Klumperman J, Kits KS, Lodder H, van der Schors RC, van Elk R, Sorgedrager B, Brejc K, Sixma TK, Geraerts WP. A glia-derived acetylcholine-binding protein that modulates synaptic transmission. Nature 2001. 411(6835):261-8.
    3. Celie PH, van Rossum-Fikkert SE, van Dijk WJ, Brejc K, Smit AB, Sixma TK. Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron (2004) 41(6):907-14.
    4. Celie PH, Kasheverov IE, Mordvintsev DY, Hogg RC, van Nierop P, van Elk R, van Rossum-Fikkert SE, Zhmak MN, Bertrand D, Tsetlin V, Sixma TK, Smit AB. Crystal structure of nicotinic acetylcholine receptor homolog AChBP in complex with an alpha-conotoxin PnIA variant. Nat Struct Mol Biol. (2005) 12(7):582-8.
    5. Ulens C, Hogg RC, Celie PH, Bertrand D, Tsetlin V, Smit AB, Sixma TK. Structural determinants of selective alpha-conotoxin binding to a nicotinic acetylcholine receptor homolog AChBP. Proc Natl Acad Sci USA (2006) 103(10):3615-20.

    Partner 2:  Netherlands Cancer Institute (NKI), Amsterdam, The Netherlands

    Prof. Titia K. Sixma

    1. Brejc, K., van Dijk, W.J., Klaassen, R.V., Schuurmans, M., van der Oost, J., Smit, A.B., Sixma, TKThe crystal structure of AChBP, homolog of the N-terminal domain of the nicotinic acetylcholine receptor, Nature, 411, 269-276. (2001)
    2. Celie, P.H.N, van Rossum-Fikkert, S.E. van Dijk, W.J., Brejc, K., Smit, A.B., Sixma, TK (2004) Nicotine and carbamylcholine binding to nicotinic receptors studied by AChBP structures, Neuron, 41, 907-914.
    3. Celie, P.H., Klaassen, R.V., van Rossum-Fikkert, S.E., van Elk, R., van Nierop, P., Smit, A.B., Sixma, TKCrystal structure of AChBP from Bulinus truncatus reveals the conserved structural scaffold and sites of variation in nicotinic acetylcholine receptors, J Biol Chem. 280, 26457-26466 (2005)
    4. Celie, P.H., Kasheverov, I.E., Mordvintsev, D.Y., Hogg, R.C., van Nierop, P., van Elk, R., van Rossum-Fikkert, S.E., Zhmak, M.N., Bertrand, D., Tsetlin, V., Sixma, TK, Smit, A.B. (2005) Crystal structure of AChBP in complex with an a-Conotoxin PnIA variant, Nat. Struct. Mol. Biol. 12, 582-588.
    5. Ulens, C., Hogg, R.C., Celie, P., Bertrand, D., Tsetlin, V., Smit, A.B., Sixma, TK (2006) Structural determinants of selective @-conotoxin binding to a nicotinic acetylcholine receptor homolog AChBP,Proc. Natl. Acad. Sci. USA, 103, 3615-3620.

    Partner 3: Katholieke Universiteit Leuven (KULeuven), Leuven, Belgium

    Dr. Chris Ulens

    1. Ulens C, Tytgat J. (2001) Gi- and Gs-coupled receptors up-regulate the cAMP cascade to modulate HCN2, but not HCN1 pacemaker channels. Pflugers Arch. 442:928-42.
    2. Ulens C, Tytgat J. (2001) Functional heteromerization of HCN1 and HCN2 pacemaker channels. J. Biol. Chem. 276:6069-72.
    3. Ulens C, Siegelbaum S.A. (2003) Regulation of hyperpolarization-activated HCN channels by cAMP through a gating switch in binding domain symmetry. Neuron 40: 959-70.
    4. Ulens C, Hogg R.C., Celie P., Bertrand D., Tsetlin V., Smit A.B., Sixma T.K. (2006) Structural determinants of selective alpha-conotoxin binding to a nicotinic acetylcholine receptor homolog AChBP. Proc. Natl. Acad. Sci. USA 103: 3615-20.
    5. Dutertre S.*, Ulens C*, Büttner R., Fish A., van Elk R., Kendel Y., Hopping G., Alewood P.F., Schroeder C., Nicke A., Smit A.B., Sixma T.K. and Lewis R.J. (2007) AChBP-targeted alpha-conotoxin correlates distinct binding orientations with nAChR subtype selectivity. EMBO J. (revision pending). * shared first authorship

    Partner 4: Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), Erlangen, Germany

    Prof. M.D. Cord-Michael Becker

    1. Butler, M.H., Hayashi, A., Ohkoshi, N., Villmann, C., Becker, C.-M., Feng, G., de Camilli, P. Solimena, M. (2000) Autoimmunity against gephyrin in stiff man syndrome. Neuron 26, 307–312.
    2. Breitinger, U., Breitinger, H.-G., Bauer, F., Fahmy, K., Glockenhammer, D., Becker, C.-M. (2004) Conserved high affinity ligand binding and membrane association in the native and refolded extra–cellular domain of the human glycine receptor alpha 1 subunit. J. Biol. Chem. 279, 1627-1636.
    3. Seeber, S., Humeny, A., Herkert, M., Rau, T., Eschenhagen, T., Becker, C.-M. (2004) Formation of molecular complexes by N-methyl-D-aspartate receptor subunit NR2B and ryanodine receptor 2 in neonatal rat myocard. J. Biol. Chem. 279, 21062-21068.
    4. Breitinger, H.-G., Lanig, H., Vohwinkel, C., Grewer, C., Breitinger, U., Clark, T., Becker, C.-M. (2004) Molecular dynamics simulation links conformation of a pore-flanking region to hyperek–plexia–related dysfunction of the inhibitory glycine receptor. Chem. Biol. 279, 21062-21068.
    5. Oertel, J., Villmann, C., Kettenmann, H., Kirchhoff, F., Becker, C.-M. (2007) A novel glycine receptor beta subunit splice variant predicts an unorthodox transmembrane topology: Assembly into heteromeric receptor complexes. J. Biol. Chem. 282, 2798-2807.

    Partner 5: University of Cambridge (Univ Cambridge), Cambridge, UK

    Dr. Sarah Lummis

    1. Lummis, S.C.R., Beene, D.L., Lee, L.W., Lester, H.A., Broadhurst, R.W. and Dougherty, D.A. (2005) Cis-trans isomerisation of a proline opens the pore of a neurotransmitter–gated ion channel.Nature 438:248-52
    2. Harrison, N.J and Lummis, S.C.R. (2006) Molecular modelling of the GABAC receptor ligand-binding domain. J Molecular Modeling;12:317-24.
    3. Harrison N.H .and Lummis, S.C.R. (2006) Locating the carboxylate group of GABA in the GABAC receptor ligand-binding domain. J Biol Chem 281:24455-61
    4. Thompson A.J. and Lummis, S.C.R. (2006) Membrane channels as therapeutic targets: 5-HT3 receptors. Current Pharmaceutical Design12:24-49
    5. Padgett C.L, Hanek A.P., Lester H.A., Dougherty D.A., Lummis, S.C.R. (2007) Unnatural amino acid mutagenesis of the GABAA receptor binding site residues reveals a novel cation-pi interaction between GABA and beta2Tyr97. J Neurosci. 27:886-92

    Partner 6: Medizinische Universität Wien (MUW), Vienna, Austria

    Prof. Dr. Werner Sieghart

    1. W. Sieghart (1995) Structure and pharmacology of GABAA receptor subtypes. Pharmacol. Rev. 47, 181-234.
    2. V. Tretter, N. Ehya, K. Fuchs and W. Sieghart (1997) Stoichiometry and assembly of a recombinant GABAA receptor subtype. J. Neurosci., 17, 2728-2737.
    3. T. Klausberger, N. Ehya, K. Fuchs, T. Fuchs, V. Ebert, I. Sarto, and W. Sieghart (2001) Detection and binding properties of GABAA receptor assembly intermediates. J. Biol. Chem. 276, 16024-32.
    4. M. Ernst, S. Bruckner, S. Boresch, and W. Sieghart (2005) Comparative models of GABAA receptor extracellular and transmembrane domains: important insights in  pharmacology and function. Mol. Pharmacol. 68, 1291-1300.
    5. I. Sarto-Jackson, R. Furtmüller, M. Ernst, S. Huck, and W. Sieghart(2007) Spontaneous cross-link of mutated a1 subunits during GABAA receptor assembly. J. Biol. Chem. 282, 4354-4363.

    Partner 7: Institute Pasteur (Pinstitut), Paris, France

    Dr. Pierre-Jean Corringer

    1. Corringer, P.J., Bertrand, S, Galzi, J.L., Devillers-Thiéry, A., Changeux J.P. & Bertrand, D. Mutational analysis of the charge selectivity filter of the alpha7 nicotinic acetylcholine receptor. Neuron, 22: 831-843 (1999)
    2. Sallette, J.,Pons, S., Devillers-Thiery A., Soudant, M., Prado de Carvalho, L., Changeux J.P. and Corringer, P.J., Nicotine up-regulates its own receptors through enhanced intracellular maturation, Neuron, 46:595-607 (2005)
    3. Maskos U, Molles BE, Pons S, Besson M, Guiard BP, Guilloux JP, Evrard A, Cazala P, Cormier A, Mameli-Engvall M, Dufour N, Cloez-Tayarani I, Bemelmans AP, Mallet J, Gardier AM, David V, Faure P, Granon S, Changeux JP. Nicotine reinforcement and cognition restored by targeted expression of nicotinic receptors. Nature. 436(7047):103-7 (2005)
    4. Delarue M, Duclert-Savatier N, Miclet E, Haouz A, Giganti D, Ouazzani J, Lopez P, Nilges M, Stoven V. Three dimensional structure and implications for the catalytic mechanism of 6-phosphogluconolactonase from Trypanosoma brucei. J Mol Biol. 366(3):868-81 (2007)
    5. Bocquet, N., Prado de Carvalho, L., Cartaud, J., Neyton, J., Le Poupon, C., Taly, A., Grutter, T., Changeux, J.P., Corringer, P.J. A prokaryotic proton-gated ion channel from the nicotinic acetylcholine receptor family, Nature, 445:116-119 (2007)

    Partner 8: Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry (IBCH), Moscow, Russia

    Prof. Victor Tsetlin

    1. Osipov AV, Astapova MV, Tsetlin VI, Utkin YN. (2004) The first representative of glycosylated 3-fingered toxins. Cytotoxin from the Naja kaouthia cobra venom. Eur J Biochem. 271: 2018-2027.
    2. Celie PH, Kasheverov IE, Mordvintsev DY, Hogg RC, van Nierop P, van Elk R, van Rossum-Fikkert SE, Zhmak MN, Bertrand D, Tsetlin V, Sixma TK, Smit AB. (2005) Crystal structure of nAChR homolog AChBP in complex with an a-conotoxin PnIA variant. Nat. Struct. Mol. Biol. 12:582-588.
    3. Ulens C, Hogg RC, Celie PH, Bertrand D, Tsetlin V, Smit AB, Sixma TK. (2006) Structural determinants of selective alpha-conotoxin binding to a nicotinic acetylcholine receptor homolog AChBP. Proc. Natl. Acad. Sci. USA. 103: 3615-3620.
    4. Kasheverov IE, Zhmak MN, Vulfius CA, Gorbacheva EV, Mordvintsev DY, Utkin YN, van Elk R, Smit AB, Tsetlin VI. (2006) Alpha-conotoxin analogs with additional positive charge show increased selectivity towards T. californica and some neuronal subtypes of nAChR. FEBS J. 273: 4470-4481.
    5. Mordvitsev DY, Polyak YL, Kuzmin DA, Levtsova OV, Utkin YN, Shaitan KV, Tsetlin VI. (2007) Computer modeling of binding of diverse weak toxins to nAChR. Comput. Biol. Chem. 31: 72-81.

    Partner 9: Mediterranean Institute of Neurobiology (INMED), Marseille, France

    Dr. Piotr Bregestovski

    1. Fucile S., De Saint Jan D., Prado de Carvalho L., Bregestovski P. (2000). Fast potentiation of glycine receptor channels by intracellular calcium in neurons and transfected cells. Neuron, 28:571-583.
    2. Zhorov B., Bregestovski P. (2000). Chloride channels of glycine and GABA receptors with blockers: Monte Carlo minimization and structure-activity relationships. Biophys. J., 78:1786-803.
    3. Grailhe R, de Carvalho LP, Paas Y, Le Poupon C, Soudant M, Bregestovski P., Changeux JP, Corringer PJ. (2004) Distinct subcellular targeting of fluorescent nicotinic alpha 3 beta 4 and serotoninergic 5-HT3A receptors in hippocampal neurons. Eur J Neurosci. 19:855-62.
    4. Diana MA, Bregestovski P. (2005) Calcium and endocannabinoids in the modulation of inhibitory synaptic transmission. Cell Calcium. 37:497-505
    5. Mukhtarov M, Ragozzino D, Bregestovski P. (2005) Dual Ca2+ modulation of glycinergic synaptic currents in rodent hypoglossal motoneurones. J Physiol. 569:817-831.

    Participant 10: European Molecular Biology Laboratory (EMBL), Mouse Biology Unit, Italy.

    Dr. C. Gross

    1. Gross, C., Zhuang, X., Stark, K., Ramboz, S., Oosting, R., Kirby, L., Beck, S., and Hen, R. (2002) Serotonin 1A Receptor is Required During Development to Establish Normal Emotional Behavior.Nature 416, 396-400.
    2. Santarelli, L., Saxe, M., Gross, C., Surget, A., Battaglia, F., Dulawa, S., Weisstaub, N., Lee, J., Duman, R., Arancio, O., Belzung, C., and Hen, R. (2003). Requirement of Hippocampal Neurogenesis for the Behavioral Effects of Antidepressants. Science 301, 805-809.
    3. Gross, C. and Hen, R. (2004). The Developmental Origins of Anxiety. Nature Rev. Neurosci. 5, 545-552.
      Carola, V., Frazzetto, G., Gross, C. (2006) Identifying interactions between genes and early environment in the mouse. Genes Brain Behavior 5, 189-199.
    4. Mirabeau, O., Perlas, E. , Severini, C., Audero, E., Gascuel, O. , Possenti, R., Birney, E., Rosenthal, N., Gross, C. (2007) Identification of novel peptide hormones in the human proteome by hidden Markov model screening. Genome Research 17:320-7.

    Participant 11: University College London (UCL), UK

    Prof. Trevor G. Smart

    1. Hosie AM, Dunne EL, Harvey RJ, Smart TG. (2003). Zinc-mediated inhibition of GABAA receptors: discrete binding sites underlie subtype specificity. Nature Neurosci. 6, 362-369.
    2. Duguid IC & Smart TG. (2004). Retrograde activation of presynaptic NMDA receptors enhances GABA release at cerebellar interneuron-Purkinje cell synapses. Nature Neurosci. 7, 525-533.
    3. Thomas P, Mortensen M, Hosie AM & Smart TG. (2005). Dynamic mobility of functional GABAA receptors at inhibitory synapses. Nature Neurosci. 8, 889-897.
    4. Mortensen M & Smart TG. (2006). Extrasynaptic alpha-beta subunit GABAA receptors on rat hippocampal pyramidal neurons. J Physiol. 577, 841-856.
    5. Hosie AM, Wilkins ME, da Silva HM & Smart TG. (2006). Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites. Nature.444, 486-489.

    Partner 12: Centre Médical Universitaire (UniGe), Geneva Switzerland

    Prof. Daniel Bertrand

    1. van Nierop P, Keramidas A, Bertrand S, van Minnen J, Gouwenberg Y, Bertrand D, Smit AB Identification of molluscan nicotinic acetylcholine receptor (nAChR) subunits involved in formation of cation- and anion-selective nAChRs. J Neurosci 25, 10617-10626,2005.
    2. van Nierop P, Bertrand S, Munno DW, Gouwenberg Y, van Minnen J, Spafford JD, Syed NI, Bertrand D, Smit AB Identification and functional expression of a family of nicotinic acetylcholine receptor subunits in the central nervous system of the mollusc Lymnaea stagnalis. J Biol Chem 281, 1680-1691,2006.
    3. Charpantier E, Wiesner A, Huh KH, Ogier R, Hoda JC, Allaman G, Raggenbass M, Feuerbach D, Bertrand D, Fuhrer C Alpha7 neuronal nicotinic acetylcholine receptors are negatively regulated by tyrosine phosphorylation and Src-family kinases. J Neurosci 25, 9836-9849,2005.
    4. Bertrand D,, Elmslie, F., Hughes, E., Trounce, J., Sander, T., Bertrand, S., and Steinlein, O. K. The CHRNB2 mutation I312M is associated with epilepsy and distinct memory deficits. Neurobiol Dis 20, 799-804,2005.
    5. Celie, P. H., Kasheverov, I. E., Mordvintsev, D. Y., Hogg, R. C., van Nierop, P., van Elk, R., van Rossum-Fikkert, S. E., Zhmak, M. N., Bertrand D,, Tsetlin, V., Sixma, T. K., and Smit, A. B. Crystal structure of nicotinic acetylcholine receptor homolog AChBP in complex with an alpha-conotoxin PnIA variant. Nat Struct Mol Biol, 12, 582-588, 2005.

    Partner 13: Consiglio Nazionale delle Ricerche (CNR), Milano Italy

    Dr. Cecilia Gotti

    1. Zoli M, Moretti M, Zanardi A, McIntosh JM, Clementi F and Gotti C (2002) Identification of the nAChR subtypes expressed on dopaminergic terminals in the rat striatum. J. Neurosci. 22:8785-8789.
    2. Champtiaux N, Gotti C Cordero-Erausquin M, David D, Przybylski C, Léna C, Le Novère N, , Clementi F, Moretti M, Rossi FM, McIntosh JM, Gardier A, and Changeux J-P (2003) Subunit composition of functional nAChRs in dopaminergic neurons investigated with knockout mice. J. Neurosci. 23: 7820-7829.
    3. Gotti C Moretti M, Zanardi A, Gaimarri A, Champtiaux N, Changeux JP, Marks MJ, Clementi F and Zoli M (2005) Heterogeneity and selective targeting of neuronal nAChR subtypes expressed on retinal afferents of the superior colliculus and lateral geniculate nucleus: identification of a new nAChR subtype a3b2(a5/b3) enriched in retinocollicular afferents. Mol Pharmacol 68:1162-1171.
    4. Gotti C Moretti M, Clementi F, Riganti L, McIntosh JM, Collins AC, Marks MJ and Whiteaker P (2005) Expression of nigrostriatal alpha6-containing nAChRs is selectively reduced, but not eliminated, by beta3 subunit gene deletion. Mol Pharmacol 67:2007-2015
    5. Gotti C Zoli M and Clementi F (2006) Brain nicotinic acetylcholine receptors: native subtypes and their relevance. Trends Pharmacol Sci 27(9):482-491.

    Partner 14: Hellenic Pasteur Institute (HPI), Athens, Greece

    Prof. Socrates Tzartos

    1. Avramopoulou, V., Mamalaki, A., Tzartos, S.J. (2004) Soluble, oligomeric and ligand-binding extra­cellular domain of human alpha7 nAChR expressed in yeast. Replacement of the hydrophobic cys-loop by the hydrophilic loop of AChBP enhances protein solubility. J. Biol. Chem. 279: 38287-93.
    2. Psaridi-Linardaki, L., Mamalaki, A., Trakas, N. and Tzartos, S.J. (2005) Specific immunoadsorption of the antibodies from myasthenic patients using the extracellular domain of human nAChR alpha-subunit. Development of an antigen-specific therapeutic strategy. J. Neuroimmunol. 159:183-91
    3. Kostelidou, K., Trakas,N., Zouridakis, M., Bitzopoulou, K., Sotiriadis,A., Gavra, H., and Tzartos, S.J.Expression and characterization of soluble forms of the extracellular domains of the β, γ and ε subunits of the human muscle nAChR. FEBS J. 273: 3557-3568 (2006)
    4. Konstantakaki, M., Tzartos, S.J., Poulas, K., and Eliopoulos, E. (2007) Molecular modeling of complex between nAChR and anti-MIR Fab. Biochem. Biophys. Res. Commun. 356:569-75.
    5. Kalamida, D., Poulas, K., Avramopoulou, V, Fostieri, E., Lagoumintzis, G., Lazaridis, K., Sideri A., M. Zouridakis and Tzartos, S.J. (2007). Muscle and Neuronal nAChRs: Structure, Function and Pathogenicity. FEBS J. In press.

    Partner 15: University of Patras (UPAT), Department of Pharmacy

    Assist Prof. Georgios A. Spyroulias

    1. Spyroulias GA, Nikolakopoulou P, Tzakos A, Gerothanassis IP, Magafa V, Manessi-Zoupa E, Cordopatis P. (2003) Comparison of the solution structures of angiotensin I & II. Implication for structure-function relationship. Eur J Biochem. 270:2163-73.
    2. Banci L, Bertini I, Ciofi-Baffoni S, Kandias NG, Robinson NJ, Spyroulias GA,, Su XC, Tottey S, Vanarotti M. (2006) The delivery of copper for thylakoid import observed by NMR. Proc Natl Acad Sci U S A. 103:8320-5.
    3. Bertini I, Felli IC, Gonnelli L, Pierattelli R, Spyranti Z, Spyroulias GA, (2006) Mapping protein-protein interaction by 13C’-detected heteronuclear NMR spectroscopy. J Biomol NMR. 36:111-22.
    4. Bertini I., Calderone V, Fragai M, Giachetti A, Loconte M, Luchinat C, Maletta M, Nativi C, Yeo KJ. (2007) Exploring the subtleties of drug-receptor interactions: the case of matrix metalloproteinases. J Am Chem Soc. 129:2466-75.
    5. A. Papakyriakou, Spyroulias GA, E. Sturrock, E. Manessi-Zoupa, P. Cordopatis. (2007) Simulated Interactions between Angiotensin-Converting Enzyme and Substrate Gonadotropin-Releasing Hormone: Novel Insights into Domain-Selectivity. Biochemistry (revision pending).

    Partner 16: Universität Konstanz (Unikon), Konstanz, Germany

    Prof. Wolfram Welte

    1. Ferguson AD, Hofmann E, Coulton JW, Diederichs K, Welte W. (1998) Siderophore-mediated iron transport: crystal structure of FhuA with bound lipopolysaccharide. Science. 282:2215-20.
    2. Freigang J, Proba K, Leder L, Diederichs K, Sonderegger P, Welte W. (2000) The crystal structure of the ligand binding module of axonin-1/TAG-1 suggests a zipper mechanism for neural cell adhesion.Cell. 101:425-33.
    3. Meier T, Polzer P, Diederichs K, Welte W. Dimroth P. (2005) Structure of the rotor ring of F-Type Na+-ATPase from Ilyobacter tartaricus. Science 308:659-62.
    4. Kodding J, Killig F, Polzer P, Howard SP, Diederichs K, Welte W. (2005) Crystal structure of a 92-residue C-terminal fragment of TonB from Escherichia coli reveals significant conformational changes compared to structures of smaller TonB fragments. J Biol Chem. 280:3022-8.
    5. Krug M, Lee SJ, Diederichs K, Boos W, Welte W. (2006) Crystal structure of the sugar binding domain of the archaeal transcriptional regulator TrmB. J Biol Chem. 281:10976-82.

    Partner 17: VU University Amsterdam, Amsterdam (VUA), The Netherlands

    Dr. Iwan de Esch

    1. De Esch, I.J.P., Mills, J.E., Perkins, T.D., Romeo, G., Hoffmann, M., Wieland, K., Leurs, R., Menge, W.M., Nederkoorn, P.H., Dean, P.M., Timmerman, H. (2001) Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE. J Med Chem. 44:1666-74.
    2. Hulshof, J.W., Casarosa, P., Menge, W.M., Kuusisto, L.M., van der Goot, H., Smit, M.J., de Esch, I.J.P.,  Leurs, R. (2005) Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human CMV encoded chemokine receptor US28. J Med Chem. 48:6461-71.
    3. De Esch, I.J.P., Thurmond, R.L., Jongejan, A., Leurs, R. (2005) The histamine H4 receptor as a new therapeutic target for inflammation. Trends Pharmacol Sci. 26:462-9.
    4. Hough, L.B., de Esch, I.J.P., Janssen, E., Phillips, J., Svokos, K., Kern, B., Trachler, J., Abood, M.E., Leurs, R., Nalwalk, J.W. (2006) Antinociceptive activity of chemical congeners of improgan: optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic. Neuropharmacology. 51 :447-56.
    5. Govoni, M., Lim, H.D., El-Atmioui, D., Menge, W.M., Timmerman, H., Bakker, R.A., Leurs R., de Esch, I.J.P. (2006) A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function. J Med Chem. 49: 2549-57.

    Partner 18: ProteoSys AG (PSY), Mainz, Germany

    Prof. dr. André Schrattenholz

    1. Schillo S, Pejović V, Hunzinger C, Hansen T, Poznanović S, Kriegsmann J, Schmidt WJ and Schrattenholz A. (2005) Integrative Proteomics: functional and molecular characterization of a particular glutamate-related neuregulin isoform. Journal of Proteome Research 4 (3), 900-908.
    2. Šoškić V, Schwall G, Nyakatura E, Poznanovic S, Stegmann W and Schrattenholz A. (2006) HDA-Sepharose 4B: A new tool for preparation of albumin depleted plasma. Journal of Proteome Research, 5(12), 3453-3458.
    3. Hunzinger C, Wozny W, Schwall GP, Poznanović S, Stegmann W, Schoepf R, Groebe K, Cahill MA, Osiewacz HD, Jägemann N, Bloch M, Dencher NA, Krause, Schrattenholz A.(2006) Comparative profiling of the mammalian mitochondrial proteome: multiple aconitase-2 isoforms including N-formylkynurenine modifications as part of a protein biomarker signature for reactive oxidative species. Journal of Proteome Research 5(3), 625-633.
    4. Reineke J, Tenzer S, Rupnik M, Hasselmayer O, Schrattenholz A., Schild H, von Eichel-Streiber C (2007) Cleavage of Clostridium difficile Toxin B is Autocatalytic and Requires Cellular Inositolphosphates. Nature, 446, 415-419.
    5. Wozny W, Schroer K, Schwall GP, Poznanović S, Stegmann W, Dietz K, Rogatsch H, Schaefer G, Huebl H, Klocker H, Schrattenholz A., Cahill MA (2007) Differential radioactive quantification of protein abundance ratios between benign and malignant prostate tissues: cancer association of annexin A3.Proteomics, 7(2), 313-322.

    Partner 19: REGULON A.E.(REG), Athens, Greece

    Dr. Michael Roberts (Director, Gene Therapy)
    CEO of Regulon: Teni Boulikas, Alimos, Athens, Greece

    1. Lundstrom, K. (2003) Semliki Forest virus vectors for rapid and high-level expression of integral membrane proteins. Biochimica Biophysica Acta 1610, 90-96.
    2. Lundstrom, K. (2005) Structural Genomics of GPCRs. Trends in Biotechnology 23, 103-108.
    3. Hassaine, G., Wagner, R., Kempf, J., Cherouati, N., Hassaine, N., Prual, C., André, N., Reinhart, C., Pattus, F. & and Lundstrom, K. (2006) Semliki Forest Virus vectors for overexpression of 101 G Protein-coupled receptors in mammalian host cells. Protein Expression & Purification, 45(2):343-51.
    4. Related Patent: WO 2005/056805: Viral particles containing an alpha virus derived vector and method for preparing said viral particle. Inventor: J.C. Pages
    5. Related Patent: Application: Liposomally encapsulated hybrid Adenovirus-Semliki Forest Virus (SFV) vectors carrying RNAi constructs and therapeutic genes for use against cancer targets and other diseases. Inventor: M. L. Roberts

    Partner 20: Beactica AB (Beactica), Uppsala, Sweden.

    Prof. Helena Danielson, Ph.D.

    1. Källblad, P., Mancera, R.L. and Todorov, N.P. (2004) Assessment of multiple binding modes in ligand-protein docking., J. Med. Chem. 47:3334-7.
    2. Shuman, C.F., Vrang, L. and Danielson, U.H. (2004) Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. J. Med. Chem. 47:5953-61.
    3. Cimitan, S., Lindgren, M., Bertucci, C. and Danielson, U.H. (2005) Early ADME analysis of anti-tumour and anti-AIDS drugs: Lipid membrane and plasma protein interactions. J. Med. Chem.48:3536-46.
    4. Geitmann, M., Unge, T. and Danielson, U.H. (2006) Kinetic characterization of the interaction between HIV-1 reverse transcriptase and non-nucleoside inhibitors. J. Med. Chem.49:2367-74.
    5. Gutierrez, O.A. and Danielson, U.H. (2006) Detection of enzyme inhibition with end point progress curve data. Anal. Biochem. 358:11-19.

    Partner 22: Università di Modena e Reggio Emilia (UNIMORE), Modena Italy

    Dr. Michele Zoli

    1. Zoli M., Moretti M., Zanardi A., McIntosh M.J., Clementi F., Gotti C. (2002) Identification of the nicotinic receptor subtypes expressed on dopaminergic terminals in the rat striatum. J. Neurosci. 22:8785-8789.
    2. Picciotto M.R., Zoli M., Rimondini R., Léna C., Marubio L., Merlo Pich E., Fuxe K., Changeux J.-P. (1998) Acetylcholine receptors containing beta2 subunits are involved in the reinforcing properties of nicotine. Nature, 391:173-177.
    3. Zoli M., Léna C., Picciotto M.R., Changeux J.P. (1998) Identification of four classes of brain nicotinic receptors using beta2-mutant mice. J. Neurosci. 18:4461-4472.
    4. Zanetti L, de Kerchove D’Exaerde A, Zanardi A, Changeux JP, Picciotto MR, Zoli M.(2006) Inhibition of both alpha7* and beta2* nicotinic acetylcholine receptors is necessary to prevent development of sensitization to cocaine-elicited increases in extracellular dopamine levels in the ventral striatum. Psychopharmacology (Berl) 187: 181-188.
    5. Zanetti L, Picciotto MR, Zoli M. (2007) Differential effects of nicotinic antagonists perfused into the nucleus accumbens or the ventral tegmental area on cocaine-induced dopamine release in the nucleus accumbens of mice. Psychopharmacology (Berl) 190(2):189-199.

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