Publication list prior to start Project
Prof. Myriam Witvrouw
Witvrouw, M., Fikkert, V., Pluymers, W., Matthews, B., Mardel, K., Schols, D., Raff, J., Debyser, Z., De Clercq, E., Holan, G. & Pannecouque, C. Polyanionic (i.e. polysulfonate) dendrimers can inhibit the replication of human immunodeficiency virus by interfering with both virus adsorption and later steps (reverse transcriptase/integrase) in the virus replicative cycle. Mol. Pharmacol., 58: 1100-1108 (2000).
Pluymers, W., Neamati, N., Pannecouque, C., Fikkert, V., Marchand, C., Burke, T.R., Pommier, Y., Schols, D., De Clercq, E., Debyser, Z. & Witvrouw, M. Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters. Mol. Pharmacol., 58: 641-648 (2000).
Witvrouw, M., Weigold, H., Pannecouque, C., Schols, D., De Clercq E. & Holan, G. Potent anti-HIV (type 1 and type 2) activity of polyoxometalates: Structure-activity-relationship and mechanism of action. J. Med. Chem., 43: 778-783 (2000).
Fikkert V, Cherepanov P, Van Laethem K, Hantson A, Van Remoortel B, Pannecouque C, De Clercq E, Debyser Z, Vandamme AM, Witvrouw M.env Chimeric Virus Technology for Evaluating Human Immunodeficiency Virus Susceptibility to Entry Inhibitors. Antimicrob Agents Chemother. 2002 Dec;46(12):3954-62.
Pannecouque, C., Pluymers, W., Van Maele, B., Tetz, V., Cherepanov, P., De Clercq, E., Witvrouw, M., Debyser Z. New Class of HIV Integrase Inhibitors that Block Viral Replication in Cell Culture. Current Biology. 12, 1169-1177 (2002).
Dr. José A. Esté
Blanco J, Barretina J, Ferri K, Jacotot E, Gutiérrez A, Armand-Ugon M, Cabrera C, Kroemer G, Clotet B and Esté JA. HIV-1 gp41 participates in HIV-1 envelope induced apoptosis in a cell fusion-independent fashion. Virology, 305(2): 318-329, 2003.
Martínez MA, Gutíerrez A, Parera M, Armand-Ugón M, Blanco J, Clotet B and Esté JA. Suppression of chemokine receptor expression by RNA interference (RNAi) allows for inhibition of HIV-1 replication. AIDS, 16(18):2385-2390, 2002.
Castedo M, Roumier T, Blanco J, Larochette N, Ferri K, Barretina J, Andreu K, Perfettini JL, Amendola A, Nardacci R, Leduc P, Ingber DE, Druillence S, Roques B, Esté JA, Modjtahedi N, Piacentini M, Kroemer G. Sequential involvement of Cdk1, mTOR and p53 in apoptosis induced by the human immunodeficiency virus envelope. EMBO Journal, 21(15): 4070-4080, 2002.
Castedo M, Ferri KF, Blanco J, Larochette N, Roumier T, Barretina J, Amedola A, Nardacci R, Esté JA, Piacentini M, and Kroemer G. Human immunodeficiency virus 1 envelope glycoprotein complex-induced apoptosis involves mammalian target of rapamycin/FKBP12-rapamycin-associated protein-mediated p53 phosphorylation. Journal of Experimental Medicine, 194 (8):1097-1110, 2001.
Martinez MA, Clotet B, Esté JA. RNA interference of HIV replication. Trends in Immunology (Immunology Today) , 23(12):559-561, 2002
Prof. Jean-Luc Darlix
Beltz H, Azoulay J, Bernacchi S, Clamme J-P, Ficheux D, Roques B, Darlix J-L,Mély Y. Impact of the Terminal Bulges of HIV-1 cTAR DNA on its Stability and the Destabilizing Activity of the Nucleocapsid Protein NCp7, J Mol Biol 2003. In press
Cristofari G, Darlix JL. The ubiquitous nature of RNA chaperone proteins. Prog Nucleic Acid Res Mol Biol. 72:223-68, 2002. Review.
Cimarelli A, Darlix JL. Assembling the human immunodeficiency virus type 1. Cell Mol Life Sci. 59(7):1166-84, 2002. Review.
Gabus C, Derrington E, Leblanc P, Chnaiderman J, Dormont D, Swietnicki W, Morillas M, Surewicz W, Marck D, Nandi P, Darlix JL. The prion protein has RNA binding and chaperoning properties characteristic of nucleocapsid protein NCp7 of HIV-1. J. Biol. Chem. 276: 19301-19309, 2001.
Theophile Ohlmann, Marcelo Lopez Lastra and Jean-Luc Darlix. 2000. An internal Ribosome Entry Segment (IRES) promotes translation of the SIV genomic RNA. J. Biol. Chem. 275, 11899-11906, 2000.
Philippe-Emmanuel Mangeot, Didier Nègre, Bertrand Dubois, Arend J. Winter, Philippe Leissner, Majid Mehtali, Dominique Kaiserlian, François-Loïc Cosset, and Jean-Luc Darlix. Development of Minimal Lentivirus Vectors Derived from Simian Immunodeficiency Virus (SIVmac251) and Their Use for Gene Transfer into Human Dendritic Cells. J. Virol. 74:8307-8315.
Prof. Dr. Jaume Vilarrasa
Costa AM, Faja M, Farras J, Vilarrasa J. Uracil- and Thymine-Substituted Thymidine and Uridine Derivatives, Tetrahedron Lett. 1998. 39, 1835-1839
Sutton PW, Bradley A, Elsegood MRJ, Farras J, Jackson RFW, Romea P, Urpi F, Vilarrasa J. Design and Synthesis of a Novel Cyclo-ß-tetrapeptide, Tetrahedron Lett. 1999. 40, 2629-2632
Ariza X, Vilarrasa J. High-Yielding Preparation of [3-15N]Cytidine, [4-15NH2]Cytidine, and [3-15N,4-15NH2]Cytidine, J. Org. Chem. 2000. 65, 2827-2829
Gorchs O, Hernandez M, Garriga L, Pedroso E, Grandas A, Farras J. A New Method for the Preparation of Modified Oligonucleotides, Organic Lett. 2002. 4, 1827-1830
Pineda O, Farras J, Vilarrasa J, Botta M, Maccari, Manetti F. In Silico High-Throughput Screening of Laulimalide-Related Anticancer Agents, Angew Chem Int Ed. 2003. 41, ...
Prof. Zeger Debyser
Pannecouque, C., Pluymers, W., Van Maele, B., Tetz, V., Cherepanov, P. De Clercq, E., Witvrouw, M., and Debyser Z. New class of HIV integrase inhibitors that block viral replication in cell culture. Current Biology. 12, 1169-1177 (2002). (8.4)
Cherepanov, P., Maertens, G., Proost, P., Devreese, B., Van Beeumen, J., Engelborghs, Y., De Clercq, E., Debyser, Z. HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells. J. Biol. Chem. 278, 38372-38381 (2003).
Cherepanov, P., Pluymers, W., Claeys, A., De Clercq, E., and Debyser, Z. High level expression of active HIV-1 integrase from a synthetic gene in human cells. FASEB J. 14, 1389-1399 (2000).
Vercammen, J., Maertens, G., Gerard, M., De Clercq, E., Debyser, Z., and Engelborghs, Y., DNA-induced polymerization of HIV-1 integrase analyzed with fluorescence fluctuation spectroscopy. J. Biol. Chem. 277, 38045-38052 (2002).
Van Maele, B., De Rijck, J., De Clercq, E. and Debyser, Z. Impact of the central polypurine tract (cPPT) on the kinetics of HIV-1 vector transduction. J. Virol. In press (2003).
Dr. Richard Benarous
Margottin F., Bour S., Durand H, Selig, L., Benichou S., Richard V., Thomas D., Strebel K. and Benarous R. A novel human WD protein, h-b-TrCP, that interacts with HIV-1 Vpu connects CD4 to the ER degradation pathway through an F-box motif. Mol. Cell, (1998), 1, 565-574.
M. Kroll, F. Margottin, F., A. Kohl, P. Renard P., H. Durand, J.P. Concordet, F. Bachelerie, F., Arenzana-Seisdedos and R. Benarous Inducible degradation of IkBa by the proteasome requires interaction with the F-box protein h-bTrCP. J. Biol. Chem., (1999), 274, 7941-7945
Lassot I, Segeral E, Berlioz-Torrent C, Durand H, Groussin L, Hai T, Benarous R, Margottin-Goguet F. ATF4 degradation relies on a phosphorylation-dependent interaction with the SCF(betaTrCP) ubiquitin ligase.Mol Cell Biol. 2001 Mar;21(6):2192-202.
Wyss S, Berlioz-Torrent C, Boge M, Blot G, Honing S, Benarous R, Thali M. The highly conserved C-terminal dileucine motif in the cytosolic domain of the human immunodeficiency virus type 1 envelope glycoprotein is critical for its association with the AP-1 clathrin adapter. J Virol. 2001 Mar;75(6):2982-92
Blot, G., Janvier, K., Benarous, R. and C. Berlioz-Torrent. Targetting of the HIV-1 envelope to the trans-Golgi network through binding to TIP47 is required for Env incorporation into virions and infectivity.J. Virol., (2003). In press
Prof. Alba Chimirri
Barreca ML, Chimirri A, De Luca L, Monforte AM, Monforte P, Rao A, Zappalà M, Balzarini J, De Clercq E, Pannecouque C, Witrouw M. Discovery of 2,3-Diaryl-1,3-thiazolidin-4-ones as Potent Anti-HIV-1 Agents, Bioorg Med. Chem 2001, 11, 1793-1796
Barreca ML, Balzarini J, Chimirri A, De Clercq E, De Luca L, Holtje HD, Holtje M, Monforte AM, Monforte P, Pannecouque C, Rao A, Zappalà M. Design, Synthesis, Structure-Activity Relationships and Molecular Modeling Studies of 2,3-Diaryl-1,3-thiazolidin-4-ones Potent Anti-HIV-1 Agents, J. Med. Chem. 2002, 45, 5410-5413
Barreca M, Lee KW, Chimirri A, Briggs JM. Molecular dynamics studies of the wild-type and double mutant HIV-1 integrase complexed with the 5CITEP inhibitor: mechanism for inhibition and drug resistance, Bioph. J. 2003, 84, 1450-1463
Barreca ML, Gitto R, Quartarone S, De Luca L, De Sarro G, Chimirri A. Pharmacophore modeling as an efficient tool in the discovery of novel noncompetitive AMPA receptor antagonists, J. Chem. Inf. Comp. Sci, in press (web release date: January 30, 2003)
Dr. Ursula Dietrich
Königs C, Merrill JR, Thompson P, Myers MA, Scealy M, Davies JM, Wu L, Dietrich U, Mackay CR, Mackay IR. Monoclonal antibody screening of a phage displayed random peptide library reveals mimotopes of chemokine receptor CCR5: implications for the tertiary structure of the receptor and an N-terminal HIV-1 gp120 binding site. Europ. J. Immunol. 2000. 30, 1162-1171.
Ruppach H, Nara P, Raudonat I, Elanjikal Z, Rübsamen-Waigmann H, Dietrich U. HIV-positive sera taken shortly after seroconversion neutralize the autologous HIV-1 isolates on primary macrophages, but not on lymphocytes. J Virol 2000. 74, 5403-5411.
Oudin S, Libyh MT, Goossens D, Dervillez X , Philbert F, Reveil B, Bougy F, Tabary T, Rouger P, Klatzmann D, Cohen JH. A soluble recombinant multimeric anti-Rh(D) single-chain Fv/CR1 molecule restores the immune complex binding ability of CR1-deficient mice. J Immunol 2000. 164 (3), 1505-13.
Pustowka A, Scherr M, Dallmann, I Scherr D, Grez M, Ganser A, Dietrich U, Eder M. Analysis of RNA-protein interaction in vitro using immobolized 5´-biotinylated RNA“ Analytical Biochemistry, submitted
Dietrich U. HIV-1 entry inhibitors, AIDS Reviews 2001. 3, 89-97.
Dr. Gilles Divita
Morris MC, Chaloin L, Mery J, Heitz F, Divita G. A novel potent strategy for gene delivery using single peptide vector as a carrier,Nucleic Acid Research 1999. 27, 3510 – 3517.
Morris MC, Depollier J, Mery J, Heitz F, Divita G. A peptide carrier for the delivery of biologically active proteins into mammalian cells, Nat. Biotechnol. 2001. 19, 1173-1176.
Morris MC, Berducou C, Mery J, Heitz F, Divita G. The thumb domain of the p51 subunit is essential for activation of HIV-1 reverse transcriptase, Biochemistry 1999. 38, 15097 - 15103.
Morris MC, Robert-Hebmann V, Chaloin L, Mery J, Heitz F, Devaux C, Goody RS, Divita G. A new potent HIV-reverse transcriptase inhibitor : a synthetic peptide derived from interface subunit domains. J. Biol. Chem. 1999. 274, 24941 – 24946.
PCT/FR01.02638 : Inhibitors of HIV replication and method of treatment of HIV infections ; ( C. Devaux, V. Hebmann, G. Divita, F. Heitz, M.C. Morris, J. Méry et R.S. Goody (2001) application : 342301 D19078
Prof. Dr. Joachim Engels
Klöpffer A, Engels JW. Universal fluorinated nucleobases: Their effect on the catalytic activity of ribozymes, Coll Czech Chem Commun Symp Series 2002.5, 348-351
Parsch J, Engels JW. C-F---H-C hydrogen bonds in RNA, J Amer Chem Soc 2002.124, 5664-5672
Brodin P, Pinskaya M, Buckle M, Parsch U, Romanova E, Engels JW, Gottikh M, Mouscadet JF. Disruption of HIV-1 integrase-DNA-complexes by short 6-Oxocytosine-containing oligonucleotides, Biochemistry 2002.41, 1529-1538
Klebba C, Klein SA, Engels JW. An assay system to detect the selective advantage of anti-HIV ribozyme expressing CD4 T-lymphozytes, Nucleotides, Nucleosides&Nucleic Acids 2001.20, 629-634
Klebba C, Ottmann G, Scherr M, Pape M, Engels JW, Grez M, Hoelzer D, Klein SA, Retrovirally expressed anti-HIV ribozymes confer a selective survival advantage on CD4+ T-cells in vitro, Gene Therapy 2000.7, 408-416
Dr. Marina Gottikh
Gottikh MB, Volkov EM, Romanova EA, Oretskaya TS, Shabarova ZA. Synthesis of oligonucleotide-intercalator conjugates capable to inhibit HIV-1 DNA integration, Nuclesides & Nucleotides 1999.18, 1645-1646
Brodin P, Gottikh MB, Auclair C, Mouscadet J-F. Inhibition of HIV-1 integration by mono- and bi-functionalyzed triple helix forming oligonucleotides, Nuclesides & Nucleotides 1999.18, 1717-1718
Brodin P, Pinskaya MD, Volkov EM, Romanova EA, Leh H, Auclair C, Mouscadet J-F, Gottikh MB. Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase, FEBS Lett 1999.460, 270-274
Pinskaia MD, Brodin P, Romanova EA, Volkov EM, Mouscadet J-F, Gottikh MV. Inhibition of integration of human immunodeficiency virus DNA by modified oligonucleotides, Mol Biol (Moscow) 2000.34, 1039-1045
Brodin P, Pinskaia M D, Buckle M, Parsch U, Romanova E, Engels J, Gottikh M, Mouscadet J-F. Disruption of integrase/DNA complexes by short 6-oxocytosine containing oligonucleotide, Biochemistry 2002.41, 1529-1538
Dr. Nicola M. Howarth
Abraham A, Howarth NM. Synthesis of thymine derivatives of 4-hydroxyvaline, Nucleosides, Nucleotides & Nucleic Acids 2003.in press
Howarth NM, Wakelin LPG, Walker DM. Synthesis of the four diastereoisomers of 3-thymine-1-( tbutoxycarbonyl)aminocyclopentane-1-carboxylic acid, Tetrahedron Lett 2003.44, 695-698.
Vyle JS, Howarth NM. Nucleotides and Nucleic Acids, Organophosphorous Chemistry (RSC Specialist periodical Report) 2001.31, 135-218
Howarth NM, Wakelin LPG. a-PNA: A novel peptide nucleic acid analogue of DNA, J Org Chem 1997.62, 5441-5450.
Searcey M, Martin PN, Howarth NM, Madden B, Wakelin LPG. DNA Threading agents. Effect of sidechain bulk on DNA binding and cytotoxicity of 9-anilinoacridine-4-carboxamides. Bioorg Med Chem Lett, 6, 1996, 1831-1836.
Prof. Robert Kaptein
Eijkelenboom APAM, Puras Lutzke RA, Boelens R, Plasterk RHA, Kaptein R, Hård K. The DNA-binding domain of HIV-1 integrase has an SH3-like fold, Nature Struct. Biol. 1995.2, 807-810
Eijkelenboom APAM, van den Ent FMI, Vos A, Doreleijers JF, Härd K, Tullius TD, Plasterk RHA, Kaptein R, Boelens R. The solution structure of the N-terminal domain of HIV-2 integrase: a novel zinc-binding fold, Current Biology 1997.7, 739-746
Eijkelenboom APAM, Sprangers R, Hård, K, Puras Lutzke RA, Plasterk RHA, Boelens R, Kaptein R. Refined solution structure of the C-terminal DNA-binding domain of Human Immunovirus-1 integrase, Proteins : Structure, Function, and Genetics 1999.36, 556-564
Kalodimos CG, Bonvin AMJJ, Kopke Salinas R, Wechselberger R, Boelens R, Kaptein R. Plasticity in protein-DNA recognition: lac repressor interacts with its natural operator O1 through alternative conformations of its DNA-binding domain, EMBO J. 2002.21, 2866-2876
Dominguez C, Boelens R, Bonvin AMJJ. HADDOCK: A protein-protein docking approach based on biochemical or biophysical information, J.Amer.Chem.Soc. 2003.125, 3731-1737
Dr. Oliver T. Keppler
Keppler OT, Hinderlich S, Langner J, Schwartz-Albiez R, Reutter W, Pawlita M. UDP-GlcNAc 2-epimerase: A regulator of cell surface sialylation. Science 1999.284, 1372–1376
Keppler OT, Yonemoto W, Welte FJ, Patton KS, Iacovides D, Atchison RE, Ngo TA, Hirschberg DL, Speck RF, Goldsmith MA. Susceptibility of rat-derived cells to replication by human immunodeficiency virus type 1, Journal of Virology 2001.75, 8063-8073
Keppler OT, Welte FJ, Ngo T, Chin P, Patton KS, Tsou CL, Abbey NW, Sharkey ME, You Y, Grant R, Scarborough JD, Ellmeier W, Littman DR, Stevenson, M, Charo I, Herndier B, Speck RF, Goldsmith MA. Progress toward a human CD4/CCR5-transgenic rat model for de novo infection by human immunodeficiency virus type 1. Journal of Experimental Medicine 2002.195, 719-736
Jekle A, Keppler OT, De Clercq E, Schols D, Weinstein M, Goldsmith MA. In vivo evolution of HIV-1 towards increased pathogenicity through CXCR4-mediated killing of uninfected CD4 T-cells. Journal of Virology 2003, in press.
Co-Inventor of patent U.S. No. 01250297.7 “Transgenic rats and rat cell lines expressing human CD4 and a human chemokine receptor”
Dr. Lajos Kovacs
Kovács L, Herczegh P, Batta G, Farkas I. Thiazole C-nucleosides III. Synthesis of pyranose analogues of tiazofurin, Tetrahedron 1991.47, 5539-5548.
Zahran MA, Kovács L, El Sakka I, Pedersen EB, Nielsen C. The potential of aspirin in prodrug synthesis: a new potential delivery system of AZT and FLT, Arch Pharm 1996.329, 417-420.
Timár Z, Kovács L, Kovács G, Schmél Z. Fmoc/acyl protecting groups in the synthesis of polyamide (peptide) nucleic acid monomers, J Chem Soc, Perkin Trans 1 2000. 19-26.
Kupihár Z, Schmél Z, Kele Z, Penke B, Kovács L. Synthesis and application of a novel, crystalline phosphoramidite with thiol terminus, suitable for the synthesis of DNA conjugates, Bioorg Med Chem 2001.9, 1241-1247.
Kovács G, Timár Z, Kupihár Z, Kele Z, Kovács L. Synthesis and analysis of peptide nucleic acid oligomers on solid phase using Fmoc/acyl-protected monomers, J Chem Soc, Perkin Trans 1 2002. 1266-1270.
Dr. Giovanni Maga
Blanca G, Baldanti F, Paolucci S, Skoblov AY, Victorova L, Hubscher U, Gerna G, Spadari S, Maga G. "Nevirapine resistance mutation at codon 181 of the HIV-1 reverse transcriptase confers Stavudine resistance by increasing nucleotide substrate discrimination and phosphorolytic activity" J Biol Chem. 2003 Feb 24 [epub ahead of print]
Focher F, Spadari S, Maga G. Antivirals at the mirror: the lack of stereospecificity of some viral and human enzymes offers novel opportunities in antiviral drug development. Curr Drug Targets Infect Disord. 2003 Mar;3(1):41-53.
Locatelli GA, Spadari S, Maga G. Hepatitis C virus NS3 ATPase/helicase: an ATP switch regulates the cooperativity among the different substrate binding sites. Biochemistry. 2002 Aug 13;41(32):10332-42.
Maga G, Ramunno A, Nacci V, Locatelli GA, Spadari S, Fiorini I, Baldanti F, Paolucci S, Zavattoni M, Bergamini A, Galletti B, Muck S, Hubscher U, Giorgi G, Guiso G, Caccia S, Campiani G. The stereoselective targeting of a specific enzyme-substrate complex is the molecular mechanism for the synergic inhibition of HIV-1 reverse transcriptase by (R)-(-)-PPO464: a novel generation of nonnucleoside inhibitors. J Biol Chem. 2001 Nov 30;276(48):44653-62.
Maga G, Hubscher U, Pregnolato M, Ubiali D, Gosselin G, Spadari S. Potentiation of inhibition of wild-type and mutant human immunodeficiency virus type 1 reverse transcriptases by combinations of nonnucleoside inhibitors and D- and L-(beta)-dideoxynucleoside triphosphate analogs. Antimicrob Agents Chemother. 2001 Apr;45(4):1192-200.
Prof. Silvio Massa
Costi, R.; Di Santo, R.; Artico, M.; Massa, S. Derivatives of 2,3-dihyrdo-4H-imidazo(1,5,4-ef)(1,2,5)benzothiazepin-6(7H)-thione 1,1-dioxide, a new heterocyclic system related to TIBOJ. Heterocyclic Chem. 2002, 39, 2720-2732
Di Santo, R.; Costi, R.; Artico, M.; Massa, S.; Ragno, R.; Marshall, G.; La Colla, P.Design, synthesis and QSAR studies on N-aryl heteroarylisopropanolamines, a new class of non-peptidic HIV-1 protease inhibitors Bioorg. Med. Chem. 2002 , 10, 2511-2526
Silvestri, R.; Artico, M.; De Martino, G.; Massa, S.; Loddo, R.; Murgioni, C.; Loi, A. G.; La Colla, P.; Pani, A. Synthesis biological evaluation, and binding mode of novel 1-(2-diarylmethoxy)ethyl)-2-methyl-5-nitroimidazoles targeted at the HIV-1 Reverse Transcriptase J. Med. Chem. 2002 , 45, 1567-1576
Sbardella, G.; Mai, A.; Artico, M.; Chimenti, P.; Massa, S.; Loddo, R.; Marongiu, M. E.; La Colla, P.; Pani, A. Structure-activity relationship studies oh new DABOs: effect of substitutions at pyrimidine C-5 and C-6 positions on anti-HIV-1 activity Antiviral. Chem. Chemother. 2001 , 12, 37-50
Mai, A.; Sbardella, G.; Artico, M.; Ragno, G.; Massa, S.; Novellino, E.; Greco, G.; La Vecchia, A.; Musiu, C.; La Colla, M.; Murgioni, C.; La Colla, P.; Loddo, R. Structure-based design, synthesis and biological evaluation of conformationally restricted novel 2-alkylthio-6-(1-(2,6-difluorophenyl)alkyl)-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non nucleoside inhibitors of HIV-1 reverse transcriptase J. Med. Chem. 2001 , 44, 2544-2554
Dr. Yves Mély
Beltz H, Azoulay J, Bernacchi S, Clamme J-P, Ficheux D, Roques B, Darlix J-L,Mély Y. Impact of the Terminal Bulges of HIV-1 cTAR DNA on its Stability and the Destabilizing Activity of the Nucleocapsid Protein NCp7, J Mol Biol 2003. In press
Azoulay J, Clamme JP, Darlix JL, Roques BP,Mely Y. Destabilization of the HIV-1 Complementary Sequence of TAR by the Nucleocapsid Protein Through Activation of Conformational Fluctuations, J Mol Biol 2003.326, 691-700
Bernacchi S, Stoylov S, Piemont E, Ficheux D, Roques BP, Darlix JL,Mely Y. HIV-1 Nucleocapsid Protein Activates Transient Melting of Least Stable Parts of the Secondary Structure of TAR and its Complementary Sequence, J Mol Biol 2002.317, 385-399
Bombarda E, Morellet N, Cherradi H, Spiess B, Bouaziz S, Grell E, Roques BP,Mely Y. Determination of the pK(a) of the four Zn2+-coordinating residues of the distal finger motif of the HIV-1 nucleocapsid protein: consequences on the binding of Zn2+, J Mol Biol 2001.310, 659-672
Bombarda E, Cherradi H, Morellet N, Roques BP,Mely Y. Zn(2+) binding properties of single-point mutants of the C-terminal zinc finger of the HIV-1 nucleocapsid protein: evidence of a critical role of cysteine 49 in Zn(2+) dissociation, Biochemistry 2002.41, 4312-4320
Dr. Jean-François Mouscadet
Bischerour,J., Leh,H., Deprez,E., Brochon,J.C. and Mouscadet,J.F. (2003) Disulfide-linked integrase oligomers involving c280 residues are formed in vitro and in vivo but are not essential for human immunodeficiency virus replication. J.Virol., 77, 135-141.
Jeanson,L. and Mouscadet,J.F. (2002). Ku represses the HIV-1 transcription: identification of a putative Ku binding site homologous to the mouse mammary tumor virus NRE1 sequence in the HIV-1 long terminal repeat. J. Biol. Chem. 277, 4918-4924.
Brodin,P., Pinskaya,M., Buckle,M., Parsch,U., Romanova,E., Engels,J., Gottikh,M., and Mouscadet,J.F. (2002). Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides. Biochemistry 41, 1529-1538.
Deprez,E., Tauc,P., Leh,H., Mouscadet,J.F., Auclair,C., Hawkins,M.E., and Brochon,J.C. (2001). DNA binding induces dissociation of the multimeric form of HIV-1 integrase: a time-resolved fluorescence anisotropy study. Proc. Natl. Acad. Sci. U. S. A 98, 10090-10095.
Polanski,J., Zouhiri,F., Jeanson,L., Desmaele,D., d'Angelo,J., Mouscadet,J.F., Gieleciak,R., Gasteiger,J., and Le Bret,M. (2002). Use of the Kohonen neural network for rapid screening of ex vivo anti-HIV activity of styrylquinolines. J. Med. Chem. 45, 4647-4654.
Dr. Tobias Restle
Jäger, J., Restle, T. and Steitz, T.A., The structure of HIV-1 reverse transcpritase complexed with an RNA pseudoknot inhibitor. EMBO J. (1998), 17, 4535-4542.
Kensch, O., Connolly, B.A., Steinhoff, H.-J., McGregor, A., Goody, R.S. and Restle, T., HIV-1 reverse transcriptase-pseudoknot RNA aptamer interaction has a binding affinity in the low picomolar range coupled with high specificity. J.Biol.Chem. (2000), 275 (24), 18271-18278.
Chaloin, L., Lehmann, M. J., Sczakiel, G. and Restle, T., Endogenous expression of a high-affinity pseudoknot RNA aptamer suppresses replication of HIV-1. NAR (2002), 30 (18), 4001-4008.
Restle, T., Müller, B. and Goody, R.S., Dimerization of human immunodeficiency virus type 1 reverse transcriptase. A target for chemotherapeutic intervention. J.Biol.Chem. (1990), 265, 8986-8988.
Rothwell, P., Berger, S., Kensch, O., Felekyan, S., Antonik, M., Wöhrl, B.M., Restle, T., Goody, R.S. and Seidel, C.A.M., Multiparameter single-molecule fluorescence spectroscopy reveals heterogeneity of HIV-1 reverse transcriptase:primer/template complexes . PNAS (2003), 100 (4), 1655-1660.
Prof. Inmaculada Robina
Moreno-Vargas AJ, Fernández-Bolaños JG, Fuentes J, Robina I. Solution and Solid Phase Synthesis of Hetarylene-Carbopeptoids. A New Type of Peptidomimetics, Tetrahedron Lett., 2001, 42, 1283-1285.
Moreno-Vargas AJ, Jiménez-Barbero J, Robina I. Hetarylene-aminopolyols and Hetarylene-carbopeptoids. A new type of glyco- and peptidomimetics. Syntheses and studies on solution conformation and dynamics, J. Org. Chem., in press.
Carmona AT, Fuentes J, Robina I.A convenient stereoselective route to novel tetrahydroxyindolizidines, Tetrahedron Lett., 2002, 43, 8543-8546.
Carmona AT, Fuentes J, Robina I, Rodríguez-García E, Demange R, Vogel P, Winters AL Stereoselective of 1,4-Dideoxy-1,4-Iminooctitols and Novel Tetrahydroxyindolizidines, J. Org. Chem., in press.
Vera-Ayoso Y, Borrachero P, Cabrera-Escribano F, Diánez MJ, Estrada MD, Gómez-Guillén M, López Castro A, Pérez Garrido S. Towards cyclic, conformationally constrained fluorine-containing a-aminoacids derivatives from D-glucose. Tetrahedron:asymmetry, 2001, 12, 2031-2041.
Borrachero P, Cabrera-Escribano F, Diánez MJ, Estrada MD, López Castro A, Gómez-Guillén M, Pérez Garrido S, Torres I. Tetrahedron:Asymmetry, 2002, 13, 2025-2038.
Khiar N, Alcudia F, Espartero JL, Rodríguez L,Fernández I.Dynamic kinetic resolution of bis-sulfinyl chlorides:A general enantiodivergent synthesis of C2-symmetric bis-sulfinate esters and bis-sulfoxides, J. Am. Chem. Soc., 2000,122, 7598-7599.
Dr. Veljko Veljkovic
Prljic J, Veljkovic N, Doliana R, Colombatti A, Johnson E, Metlas R, Veljkovic V. Identification of the Chi recombinational hot spot within the HIV-1 gp120 gene: possible implications for the AIDS vaccine development, Vaccine 1999. 17, 1462-1467
Metlas R, Trajkovic D, Srdic T, Veljkovic V, Colombatti A. Human immunodeficiency virus V3 peptide-reactive antibodies are present in normal HIV-negative sera, AIDS Res. Hum. Retrovir. 1999. 15, 671-677
Metlas R, Trajkovic D, Srdic T, Veljkovic V, Colombatti A. Anti-V3 and anti-IgG antibodies of healthy individuals share complementarity structures, J. Acquir. Immune. Defic. Syndr. 1999. 21, 266-270
Veljkovic V, Metlas R, Kohler H, Urnovitz H, Prljic J, Veljkovic N, Johnson E, Muller S. AIDS epidemic at the beginning of the third millennium: time for a new AIDS vaccine strategy, Vaccine 2001. 19, 1855-1862.
Veljkovic V, Metlas R, Jevtovic Dj, Stringer WW. The Role of Passive. Immunization in HIV+ Patients: A Case Report, Chest 2001. 120, 662-666.
Dr. José Villalaín
M. Giudici, R. Pascual, L. de la Canal, K. Pfüller, U. Pfüller y J. Villalaín. Interaction of viscotoxins A3 and B with membrane model systems. implications to their mechanism of action. BIOPHYS. J. (in press, 2003).
Bernabeu, A., Shapiro, S y J. Villalaín. A MAS-NMR study of the location of (+)-totarol, a diterpenoid bioactive molecule, in phospholipid model membranes. CHEM. PHYS. LIPIDS 119, 33-39 (2002)
J. Villalaín, C. R. Mateo, F. J. Aranda, S. Shapiro y V. Micol. Membranotropic effects of the antibacterial agent triclosan. ARCHIVES BIOCHEM. BIOPHYS 390, 128-36 (2001)
Contreras, L.M., Aranda, F.J., Gavilanes, F., González-Ros, José M., Villalaín, J. Structure and interaction with membrane model systems of a peptide derived from the major epitope region of HIV protein gp41. Implications on viral fusion mechanism. BIOCHEMISTRY 40, 3196-3207 (2001)
Micol, V., C.R. Mateo, Shapiro, S., Aranda, F.J. y J. Villalaín. Effects of (+)-totarol, a diterpenoid antibacterial agent, on phospholipid model membranes. BIOCHIM. BIOPHYS. ACTA. 1511, 281-290 (2001)
Prof. Dr. Pierre Vogel
Moreno-Vargas AJ, Demange R, Fuentes J, Robina I, Vogel P. Synthesis of [(2S, 3S, 4R)-3,4-dihydroxypyrrolidin-2-yl]-5-methylfuran-4-carboxylic acid derivatives: New Leads as Selective b -Galactosidase Inhibitors, Bioorg Med Chem Lett 2002.12, 2335-2339
Gerber-Lemaire S, Popowycz F, Rodriguez-Garcia E, Carmona Asenjo AT, Robina I, Vogel P. An Efficient combinatorial method for the discovery of glycosidase inhibitors, ChemBioChem 2002.3, 466-470
Navarro I, Vogel P. Synthesis of a new C(1 ® 2)-linked iminodisaccharide starting from levoglucosenone, Helv Chim Acta 2002.85, 152-160
Popowycz F, Gerber-Lemaire S, Demange R, Rodriguez-Garcia E, Carmona Asenjo AT, Robina I, Vogel P. Derivatives of (2S, 3R, 4S)-2-Aminomethylpyrrolidine-3,4-diol are selective a -Mannosidase inhibitors, Bioorg Med Chem Lett 2001.11, 2489-2493
Barbero Jimenez J, Demange R, Schenk K, Vogel P. Synthesis and Solution Conformation Analysis of 2,3-anhydro-3-C [ (IR)-2,6-anhydro-1-deoxy-1-fluoro-D-glycero-D-guloheptitol-1-C-yl ] - b -D-gulo-furanose: First example of a monofluoromethlylene-linked C-disaccharide, J Org Chem 2001.66, 5132-5138
Dr. Nils Johansson (MEDIVIR)
Högberg M, Sahlberg S, Engelhardt P, Noréen R et al. Urea-PETT compounds as a New Class of HIV-1 Reverse Transcriptase Inhibitors, J. Med. Chem. 1999.42, 4150-4160
Sahlberg C, Noréen R, Engelhardt P, Högberg M et al. Synthesis and Anti-HIV Activities of Urea-PETT Analogs. Bioorg. & Med. Chem. Letters 1998.8, 1511-16
Lourdes Odén, Lotta Naeslund . WO 02/70516 Published 12.09.2002, Stefan Lindström, Christer Sahlberg, Hans Wallberg, Genaidy KalyanovNon-Nucleoside Reverse Transcriptase Inhibitors
Xiao-Xiong Zhou, Nils-Gunnar Johansson, Horst Wähling, Christain Sund, Lourdes Salvador, Stefan LindströmWO 00/47561 Published 17.08.2000. Non-Nucleoside Reverse Transcriptase Inhibitors
Chrsiter Sahlberg, Rolf Noréen, Marita Högberg, Per Engelhardt. WO 99/36406 Published 22.07.1999. Antivirals
Dr. Donny Strosberg (HYBRIGENICS)
Rain JC, Selig L, De Reuse H, Battaglia V, Reverdy C, Simon S, Lenzen G, Petel F, Wojcik J, Schachter V, Chemama Y, Labigne A, Legrain P. The protein-protein interaction map of Helicobacter pylori. Nature. 2001, 409, 211-215.
Legrain P, Wojcik J, Gauthier JM. Protein--protein interaction maps: a lead towards cellular functions.Trends Genet. 2001, 6, 346-352.
Fromont-Racine M, Rain JC, Legrain P. Building protein-protein networks by two-hybrid mating strategy. Methods Enzymol. 2002, 350, 513-524.
Wojcik J, Boneca IG, Legrain P. Prediction, assessment and validation of protein interaction maps in bacteria. J Mol Biol. 2002, 323, 763-770.
Legrain P., Rain J.C., Benarous R., Blot G., Emiliani S. Berlioz-Torrent C. inventeurs. Brevet « Protein-protein interactions in Human Immunodeficiency Virus » Déposants Hybrigenics, INSERM. N° de priorité : US 60/333,346, le 26 Nov 2001, extension : le 26 Nov 2002, N° en cours.
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20-02-2006
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