Yearly International Publication list
(in reviewed Journals)
2008
Reumers V, Deroose CM, Krylyshkina O, Nuyts J, Geraerts M, Mortelmans L, Gijsbers R, Van Den Haute C, Debyser Z, Baekelandt V. Non-invasive and Quantitative Monitoring of Adult Neuronal Stem Cell Migration in Mouse Brain using Bioluminescence Imaging. Stem Cells. 2008 Jul 3 [Epub ahead of print]. [abstract] [pdf]
Brandt I, Gérard M, Sergeant K, Devreese B, Baekelandt V, Augustyns K, Scharpé S, Engelborghs Y, Lambeir AM. Prolyl oligopeptidase stimulates the aggregation of alpha-synuclein. Peptides May 15 [Epub ahead of print]. [abstract] [pdf]
Greggio E, Zambrano I, Kaganovich A, Beilina A, Taymans JM, Daniëls V, Lewis P, Jain S, Ding J, Syed A, Thomas KJ, Baekelandt V, Cookson MR. The Parkinson disease-associated leucine-rich repeat kinase 2 (LRRK2) is a dimer that undergoes intramolecular autophosphorylation. J Biol Chem 283(24):16906-14. [abstract] [pdf]
Hombrouck A, Van Remoortel B, Michiels M, Noppe W, Christ F, Eneroth A, Sahlberg BL, Benkestock K, Vrang L, Johansson NG, Barreca ML, De Luca L, Ferro S, Chimirri A, Debyser Z, Witvrouw M. Preclinical Evaluation of 1H-Benzylindole Derivatives as Novel Human Immunodeficiency Virus Integrase Stran Transfer Inhibitors. Antimicrob Agents Chemother 52(8). [abstract] [pdf]
Hombrouck A, Voet A, Van Remoortel B, Desadeleer C, De Maeyer M, Debyser Z, Witvrouw M. Mutations in HIV-1 Integrase Confer Resistance to the Naphthyridine L-870,810 and Cross Resistance to the Clinical Trial drug GS-9137. Antimicrob Agents Chemother. 52(6):2069-78. [abstract] [pdf]
Gerard M, Debyser Z, Desender L, Baert J, Brandt I, Baekelandt V, Engelborghs Y. FK506 binding protein 12 differentially accelerates fibril formation of wild type alpha-synuclein and its clinical mutants A30P or A53T. J Neurochem. 2008 Apr 14 [Epub ahead of print]. [abstract] [pdf]
Dubois M, Bailly F, Mbemba G, Mouscadet JF, Debyser Z, Witvrouw M, Cotelle P. Reaction of Rosmarinic Acid with Nitrite Ions in Acidic Conditions: Discovery of Nitro- and Dinitrorosmarinic Acids as New Anti-HIV-1 Agents. J Med Chem 51(8):2575-9. [abstract] [no pdf]
De Luca L, Barreca ML, Ferro S, Iraci N, Michiels M, Christ F, Debyser Z, Witvrouw M, Chimirri A. A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series. Bioorg Med Chem Lett. 18(9):2891-5. [abstract] [pdf]
Al-Mawsawi LQ, Christ F, Dayam R, Debyser Z, Neamati N. Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: Insight into integrase-DNA complex formation and catalysis. FEBS Lett. 582(10):1425-30. [abstract] [pdf]
Dayam R, Al-Mawsawi LQ, Zawahir Z, Witvrouw M, Debyser Z, Neamati N. Quinolone 3-carboxylic acid pharmacophore: design of second generation HIV-1 integrase inhibitors. J Med Chem 51(5):1136-44. [abstract] [no pdf]
Gielen E, Smisdom N, De Clercq B, Vandeven M, Gijsbers R, Debyser Z, Rigo JM, Hofkens J, Engelborghs Y, Ameloot M. Diffusion of Myelin Oligodendrocyte Glycoprotein in Living OLN-93 Cells Investigated by Raster-Scanning Image Correlation Spectroscopy (RICS). J Fluoresc. 2008 Jan 18 [Epub ahead of print]. [abstract] [pdf]
Celen S, Deroose C, de Groot T, Chitneni SK, Gijsbers R, Debyser Z, Mortelmans L, Verbruggen A, Bormans G. Synthesis and evaluation of 18F- and 11C-labelled phenyl-galactopyranosides as potential probes for in vivo visualization of lacZ gene expression using positron emission tomography. Bioconj. Chem. 19(2):441-9. [abstract] [no pdf]
Chitneni SK, Serdons K, Evens N, Fonge H, Celen S, Deroose CM, Debyser Z, Mortelmans L, Verbruggen AM, Bormans GM. Efficient purification and metabolite analysis of radiotracers using high-performance liquid chromatography and on-line solid-phase extraction. J Chromatogr A. 1189(1-2):323-31. [abstract] [pdf]
Casteels C, Lauwers E, Bormans G, Baekelandt V, Van Laere K. Metabolic-dopaminergic mapping of the 6-hydroxydopamine rat model of Parkinson’s disease. Eur J Nucl Med Mol Imaging (1):124-34. [abstract] [pdf]
Lin Y, Liu X, Yan R, Li J, Pannecouque C, Witvrouw M, De Clercq E. Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs). Bioorg Med Chem. 16(1):157-63. [abstract] [pdf]
Queffélec C, Bailly F, Mbemba G, Mouscadet JF, Debyser Z, Witvrouw M, Cotelle P. The total synthesis of fukiic acid, an HIV-1 integrase inhibitor. Eur J Med Chem. 2007 Dec 27 [Epub ahead of print]. [abstract] [pdf]
2007
Toelen J, Gijsbers R, Sbragia L, Deroose C, Debyser Z, Deprest J. Long term pulmonary gene therapy with a lentiviral vector in a fetal rat model. Ultrasound Obstet Gynecol. 30(4):460. [pdf]
Bartholomeeusen K, De Rijck J, Busschots K, Desender L, Gijsbers R, Emiliani S, Benarous R, Debyser Z, Christ F. Differential Interaction of HIV-1 Integrase and JPO2 with the C Terminus of
LEDGF/p75. J Mol Bio 372(2):407-21. [abstract] [pdf]
Chitneni SK, Deroose CM, Balzarini J, Gijsbers R, Celen S, Debyser Z, Mortelmans L, Verbruggen AM, Bormans GM. A p-[(18)F]Fluoroethoxyphenyl Bicyclic Nucleoside Analogue as a Potential Positron Emission Tomography Imaging Agent for Varicella-Zoster Virus Thymidine Kinase Gene Expression. J Med Chem. 50(26):6627-37. [abstract] [no pdf]
Al-Mawsawi LQ, Dayam R, Taheri L, Witvrouw M, Debyser Z, Neamati N. Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors. Bioorg Med Lett 17(23):6472-6472. [abstract] [pdf]
Wu J, Liu X, Cheng X, Cao Y, Wang D, Li Z, Xu W, Pannecouque C, Witvrouw M, De Clercq E. Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1 NNRTIs. Molecules 12(8):2003-16. [abstract] [no pdf]
Maruyama T , Demizu Y, Kozai S, Witvrouw M, Pannecouque C, Balzarini J, Snoecks R, Andrei G, De Clercq E. Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and
HCMV.
Nucleosides Nucleotides Nucleic Acids 26 (10-12):1553-8. [abstract] [no pdf]
Kronenberg G, Wang LP, Geraerts M, Babu H, Synowitz M, Vicens P, Lutsch G, Glass R, Yamaguchi M, Baekelandt V, Debyser Z, Kettenmann H, Kempermann G. Local origin and activity-dependent generation of nestin-expressing protoplasmic
astrocytes in CA1. Brain Struct Funct 212(1):19-35. [abstract] [no pdf]
Hombrouck A, Hantson A, Van Remoortel B, Michiels M, Vercammen J, Rhodes D, Tetz V, Engelborghs Y, Christ F, Debyser Z, Witvrouw M (2007). Selection of human immunodeficiency virus type 1 resistance against the
pyranodipyrimidine V-165 points to a multimodal mechanism of action. J Antimicrob Chemother 59(6):1084-95. [abstract] [pdf]
Mugnaini C, Rajamaki S, Tintori C, Corelli F, Massa S, Witvrouw M, Debyser Z, Veljkovic V, Botta M. Toward novel HIV-1 integrase binding inhibitors: Molecular modeling, synthesis,
and biological studies. Bioorg Med Chem Lett 17(19):5370-3. [abstract] [pdf]
Tintori C, Manetti F, Veljkovic N, Perovic V, Vercammen J, Hayes S, Massa S, Witvrouw M, Debyser Z, Veljkovic V, Botta M. Novel Virtual screening protocol based on the combine use of molecular modelling and electron-ion intereaction potential techniques to design HIV-1 integrase inhibitors. J. Chem. Inf. Model. 2007: 47(4):1536-44. [abstract] [no pdf]
Ferro S, Barreca ML, De Luca L, Rao A, Monforte AM, Debyser Z, Witvrouw M, Chimirri A. New 4-[(1-benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, beta-diketo
acid analogs as HIV-1 integrase inhibitors. Arch Pharm (Weinheim) 340(6):292-8. [abstract] [pdf]
De Rijck J, Vandekerckhove L, Christ F, Debyser Z. Lentiviral nuclear import: a complex interplay between virus and host. Bioessays. 29(5):441-51. [abstract] [pdf]
Chitneni SK, Deroose CM, Fonge H, Gijsbers R, Dyubankova N, Balzarini J, Debyser Z, Mortelmans L, Verbruggen AM, Bormans GM. Synthesis and biological evaluation of an (123)I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging. Bioorg Med Chem Lett.2007. Epub. [abstract] [pdf]
Toelen J, Deroose CM, Gijsbers R, Reumers V, Sbragia LN, Vets S, Chitnei SK, Bormans G, Mortelmans L, Deprest JA, Debyser Z. Fetal gene transfer with lentiviral vectors: long-term in vivo follow-up
evaluation in a rat model. Am J Obstet Gynecol 196(4):352.e1-6. [abstract] [pdf]
Hombrouck A, De Rijck J, Hendrix J, Vandekerckhove L, Voet A, De Maeyer M, Witvrouw M, Engelborghs Y, Christ F, Gijsbers R, Debyser Z (2007). Virus Evolution Reveals an Exclusive Role for LEDGF/p75 in Chromosomal Tethering of HIV. PLoS Pathog 3(3): e47. [abstract] [free full text]
Taymans JM, Vandenberghe LH, Van den Haute C, Thiry I, Deroose CM, Mortelmans L, Wilson JM, Debyser Z, Baekelandt V. Comparative analysis of adeno-associated viral vector serotypes 1, 2, 5, 7, and 8 in mouse brain. Hum Gene Ther 18(3):195-206. [abstract] [pdf]
Chitneni SK, Deroose CM, Balzarini J, Gijsbers R, Celen SJ, de Groot TJ, Debyser Z, Mortelmans L, Verbruggen AM, Bormans GM. Synthesis and preliminary evaluation of 18F- or 11C-labeled bicyclic nucleoside analogues as potential probes for imaging varicella-zoster virus thymidine kinase gene expression using positron emission tomography. J Med Chem 50(5):1041-9. [abstract] [pdf]
Veljkovic V, Mouscadet JF, Veljkovic N, Glisic S, Debyser Z. Simple criterion for selection of flavonoid compounds with anti-HIV activity. Bioorg Med Chem Lett 1;17(5):1226-32.[abstract] [pdf]
Busschots K, Voet A, De Maeyer M, Rain JC, Emiliani S, Benarous R, Desender L, Debyser Z, Christ F. Identification of the LEDGF/p75 binding site in HIV-1 integrase.
J mol biol 365,1480-1492. [abstract] [pdf]
Lauwers E, Beque D, Van Laere K, Nuyts J, Bormans G, Mortelmans L, Casteels C, Vercammen L, Bockstael O, Nuttin B, Debyser Z, Baekelandt V (2007). Non-invasive imaging of neuropathology in a rat model of alpha-synuclein overexpression. Neurobiol Aging. 28:248-257. [abstract] [pdf]
Geraerts M, Krylychkina O, Debyser Z, Baekelandt V. Concise Review: Therapeutic strategies for Parkinson's disease based on the modulation of adult neurogenesis. Stem Cells 25(2):263-270. [abstract] [pdf]
2006
De Rijck J, Vandekerckhove L, Gijsbers R, Hombrouck A, Hendrix J, Vercammen J, Engelborghs Y, Christ F, Debyser Z (2006). Overexpression of the lens epithelium-derived growth factor/p75 Integrase Binding Domain Inhibits HIV Replication. J Virol. 2006 80 (23): 11498-11506. [abstract] [pdf]
Vandekerckhove L, De Rijck J, Christ F, Gijsbers R, Debyser Z. RNAi-based treatment of HIV/AIDS: Current status and perspectives. Drug Discovery Today: Therapeutic Strategies 3(2): 227-235. [abstract] [pdf]
Casteels C, Vermaelen P, Nuyts J, Van Der Linden A, Baekelandt V, Mortelmans L, Bormans G, Van Laere K. Construction and evaluation of Multitracer small-animal PET probabilistic atlases for voxel-based functional mapping of the rat brain. J Nucl Med. 2006 Nov;47(11):1858-66. [abstract] [pdf]
De Rijck J, Debyser Z. The central DNA flap of the human immunodeficiency virus type 1 is important for viral replication. Biochem Biophys Res Commun. 2006;349(3):1100-10. [abstract] [pdf]
Vercammen L, Van der Perren A, Vaudano E, Gijsbers R, Debyser Z, Van den Haute C, Baekelandt V (2006). Parkin Protects against Neurotoxicity in the 6-Hydroxydopamine Rat Model for Parkinson's Disease. Mol Ther. 14:5, 716-723 [abstract] [pdf]
Geraerts M, Willems S, Baekelandt V, Debyser Z, Gijsbers R. Comparison of lentiviral vector titration methods. BMC Biotechnol. 2006 Jul 12;6:34. [abstract] [pdf]
Deroose CM, Reumers V, Gijsbers R, Debyser Z, Bormans G, Mortelmans L, Baekelandt V. Noninvasive Monitoring of Long-Term Lentiviral Vector-Mediated Gene Expression in Rodent Brain with Bioluminescence Imaging. Mol Ther. 14(3):423-31. [abstract] [pdf]
Luk H Vandenberghe, Lili Wang, Suryanarayan Somanathan, Yan Zhi, Joanita Figueredo, Roberto Calcedo, Julio Sanmiguel, Ravi A Desai, Christopher S Chen, Julie Johnston, Rebecca L Grant, Guangping Gao & James M Wilson. Heparin binding directs activation of T cells against adeno-associated virus serotype 2 capsid. Nature Medicine 12, 967 - 971 (2006). [abstract] [pdf]
Geraerts M, Eggermont K, Hernandez-Acosta P, Garcia-Verdugo JM, Baekelandt V, Debyser Z. Lentiviral vectors mediate efficient and stable gene transfer in adult neural stem cells in vivo. Hum Gene Ther. 2006 Jun;17(6):635-50. [abstract] [pdf]
Al-Mawsawi LQ, Fikkert V, Dayam R, Witvrouw M, Burke TR Jr, Borchers CH, Neamati N. Discovery of a small-molecule HIV-1 integrase inhibitor-binding site. PNAS USA 2006. 27;103(26):10080-5. [abstract] [pdf]
Taymans JM, Van den haute C, Baekelandt V. Distribution of PINK1 and LRRK2 in rat and mouse brain. J Neurochem. 2006 Aug;98(3):951-61. [abstract] [pdf]
Gerard M, Debyser Z, Desender L, Kahle PJ, Baert J, Baekelandt V, Engelborghs Y. The aggregation of alpha-synuclein is stimulated by FK506 binding proteins as shown by fluorescence correlation spectroscopy. FASEB J. Mar;20(3):524-6. [abstract] [pdf]
Van Maele B, Busschots K, Vandekerckhove L, Christ F, Debyser Z. Cellular co-factors of HIV-1 integration. Trends Biochem Sci. 80(4):1886-96. [abstract] [pdf]
Vandekerckhove L, Christ F, Van Maele B, De Rijck J, Gijsbers R, Van den Haute C, Witvrouw M, Debyser Z. Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus. J Virol. 2006; 80(4):1886-96. [abstract] [pdf]
Taymans JM, Kia HK, Langlois X. Activator of G protein signaling type 3 mRNA is widely distributed in the rat brain and is particularly abundant in the subventricular zone-olfactory bulb system of neural precursor cell proliferation, migration and differentiation. Neurosci Lett. 2006 Jan 2;391(3):116-21. [abstract] [pdf]
Adams MM, Bats JW, Nikolaus NV, Witvrouw M, Debyser Z, Engels JW. Microwave-assisted synthesis of fluoroquinolones and their nucleosides as inhibitors of HIV integrase. Coll Czech Chem Comm 71 (7): 978-990, 2006. [abstract available on Web of Science] [pdf]
Maruyama T, Kozai S, Demizu Y, Witvrouw M, Pannecouque C, Balzarini J, Snoecks R, Andrei G, De Clercq E. Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives. Chem Pharm Bull (Tokyo). 2006 Mar;54(3):325-33. [abstract] [pdf]
Yan RZ, Liu XY, Xu WF, Pannecouque C, Witvrouw M, De Clercq E. Synthesis and anti-HIV evaluation of the novel 2-(m-chlorobenzyl)-4-substituted-7-methyl-1, 1, 3-trioxo-pyrazolo[4, 5-e] [1, 2, 4]thiadiazines. [abstract] [no-pdf]
2005
Busschots K, Vercammen J, Emiliani S, Benarous R, Engelborghs Y, Christ F, Debyser Z. The interaction of LEDGF/p75 with integrase is lentivirus-specific and promotes DNA binding. J Biol Chem. 2005 May 6;280(18):17841-7. [abstract] [pdf]
De Rijck J, Van Maele B, Debyser Z. Positional effects of the central DNA flap in HIV-1-derived lentiviral vectors. Biochem Biophys Res Commun. 2005 Mar 25;328(4):987-94. [abstract] [pdf]
Hantson A, Fikkert V, Van Remoortel B, Pannecouque C, Cherepanov P, Matthews B, Holan G , De Clercq E , Vandamme AM , Debyser Z , Witvrouw M . Mutations in both env and gag genes are required for HIV-1 resistance to the polysulfonic dendrimer SPL2923, as corroborated by chimeric virus technology. Antivir Chem Chemother. 2005;16(4):253-66. [abstract] [pdf]
Geraerts M, Michiels M, Baekelandt V, Debyser Z, Gijsbers R. Upscaling of lentiviral vector production by tangential flow filtration. J Gene Med. 2005 Oct;7(10):1299-310. [abstract] [pdf]
Maertens G, Vercammen J, Debyser Z, Engelborghs Y. Measuring protein-protein interactions inside living cells using single color fluorescence correlation spectroscopy. Application to human immunodeficiency virus type 1 integrase and LEDGF/p75. FASEB J. 2005 Jun;19(8):1039-41. [abstract] [pdf]
Taymans JM, Kia HK, Groenewegen HJ, Leysen JE, Langlois X. Bilateral control of brain activity by dopamine D1 receptors: evidence from induction patterns of regulator of G protein signaling 2 and c-fos mRNA in D1-challenged hemiparkinsonian rats . Neuroscience. 2005;134(2):643-56. [abstract] [pdf]
van Griensven J, De Clercq E, Debyser Z. Hematopoietic stem cell-based gene therapy against HIV infection: promises and caveats. AIDS Rev. 2005 Jan-Mar;7(1):44-55. [abstract] [pdf]
Van Maele B, Debyser Z. HIV-1 integration: an interplay between HIV-1 integrase, cellular and viral proteins. AIDS Rev. 7(1):26-43. [abstract] [pdf]
Van Maele B, Van Eylen L, Pluymers W, Debyser Z. Evaluation of the activity of HIV-1 integrase over-expressed in eukaryotic cells. Biochem Biophys Res Commun. 4;327(1):261-7. [abstract] [pdf]
Witvrouw M, Fikkert V, Vercammen J, Van Maele B, Engelborghs Y, Debyzer Z (2005). Identification of Authentic Inhibitors of HIV integration. Curr. Med. Chem. Anti-infective agents, 4: 153-165. [no link to pubmed] [pdf]
Witvrouw M, Fikkert V, Hantson A, Pannecouque C, O'keefe BR, McMahon J, Stamatatos L, de Clercq E, Bolmstedt A. Resistance of human immunodeficiency virus type 1 to the high-mannose binding agents cyanovirin N and concanavalin A.
J Virol. 79(12):7777-84. [abstract] [pdf]
Barreca ML, Ferro S, Rao A, De Luca L, Zappala M, Monforte AM, Debyser Z, Witvrouw M, Chimirri A. Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors. J Med Chem. 2005 Nov 3;48(22):7084-8. [abstract] [pdf]
Emiliani S, Mousnier A, Busschots K, Maroun M, Van Maele B, Tempe D, Vandekerckhove L, Moisant F, Ben-Slama L, Witvrouw M, Christ F, Rain JC, Dargemont C, Debyser Z, Benarous R. Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication. J Biol Chem. 2005 Jul 8;280(27):25517-23. [abstract] [pdf]
Moncunill G, Negredo E, Bosch L, Vilarrasa J, Witvrouw M, Llano A, Clotet B, Este JA . Evaluation of the anti-HIV activity of statins. AIDS. 2005 Oct 14;19(15):1697-700. [abstract] [pdf]
Tsotinis A, Vlachou M, Eleutheriades A, Garratt PJ, Ibbett AJ, Ng YF, Pannecouque C, Witvrouw M, De Clercq E.
Aromatic polycationic molecules with restricted conformations: An alternative approach to antiherpes agents
Lett. Drug Design & Discovery 2 (5): 424-427, Aug 2005. [no Pubmed] [no pdf]
2004
Barreca ML, Rao A, De Luca L, Zappala M, Gurnari C, Monforte P, De Clercq E, Van Maele B, Debyser Z, Witvrouw M, Briggs JM, Chimirri A. Efficient 3D database screening for novel HIV-1 IN inhibitors. J Chem Inf Comput Sci. 2004 Jul-Aug;44(4):1450-1455. [abstract] [pdf] [supp. info.]
Fikkert V, Hombrouck A, Van Remoortel B, De Maeyer M, Pannecouque C, De Clercq E, Debyser Z, Witvrouw M. Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360. AIDS. 2004 Oct 21;18(15):2019-2028. [abstract] [pdf]
Maertens G, Cherepanov P, Debyser Z, Engelborghs Y, Engelman A. Identification and characterization of a functional nuclear localization signal in the HIV-1 integrase (IN) interactor LEDGF/p75. J Biol Chem. 2004;
279(32):33421-9. [abstract] [pdf]
van Griensven J, Zhan X, Van Maele B, Pluymers W, Michiels M, De Clercq E, Cherepanov P, Debyser Z. Expression of HIV-1 integrase in CEM cells inhibits HIV-1 replication. J. Gene Medicine 6:268-277. [abstract] [pdf]
Witvrouw M, Pannecouque C, Switzer WM, Folks TM, De Clercq E, Heneine W. Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis. Antivir Ther. 2004 Feb ;9 (1):57-65. [abstract] [pdf]
Witvrouw M, Van Maele B, Vercammen J, Hantson A, Engelborghs Y, De Clercq E, Pannecouque C, Debyser Z. Novel inhibitors of HIV-1 integration. Curr Drug Metab. 2004 Aug;5(4):291-304. [abstract] [pdf]
Ferro S, Rao A, Zappala M, Chimirri A, Barreca ML, Witvrouw M, Debyser Z, Monforte P.
Synthesis of new potential HIV-1 integrase inhibitors.
HETEROCYCLES 63 (12): 2727-2734 DEC 1 2004. [abstract] [pdf]
Maruyama T, Kozai S, Demizu Y, Witvrouw M, Pannecouque C, Balzarini J, Snoecks R, Andrei G, De Clercq E. Synthesis and antiviral activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil against HIV-1. Nucleic Acids Symp Ser (Oxf). 2004;(48):3-4. [abstract] [pdf]
Taymans JM , Kia HK, Claes R, Cruz C, Leysen J, Langlois X. Dopamine receptor-mediated regulation of RGS2 and RGS4 mRNA differentially depends on ascending dopamine projections and time. Eur J Neurosci. 2004 Apr;19(8):2249-60. [abstract] [pdf]
2003
Debyser Z. Biosafety of lentiviral vectors. Current Gene Therapy 3, 517-525. [abstract] [pdf]
Debyser Z. A short course on virology/vectorology/gene therapy. Current Gene Therapy 3, 495-499. [abstract] [pdf]
Van den Haute C, Eggermont K, Nuttin B, Debyser Z, Baekelandt V. Lentiviral vector-mediated delivery of short hairpin RNA results in persistent knock-down of gene expression in mouse brain. Human Gene Therapy 14, 1799-1807. [abstract] [pdf]
Baekelandt V, Eggermont K, Michiels M, Nuttin B, Debyser Z. Optimized lentiviral vector production and purification procedure prevents immune response after transduction of mouse brain. Gene Therapy 10, 1933-1940. [abstract] [pdf]
Fikkert V, Van Maele B, Vercammen J, Hantson A, Van Remoortel B, Michiels M, Gurnari C, Pannecouque C, De Maeyer M , Engelborghs Y, De Clercq E, Debyser Z, Witvrouw M. Development of resistance against diketo derivatives of human immunodeficiency virus-1 by progressive accumulation of mutations in integrase. J Virology 77(21):11459-70. [abstract] [pdf]
Maertens G, Cherepanov P, Pluymers W, Busschots K, De Clercq E, Debyser Z, Engelborghs Y. LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells. J. Biol. Chem. 278, 33528-39. {6.9} [abstract] [pdf]
Lauwers E, Debyser Z, Van Dorpe J, De Strooper B, Nuttin B, Baekelandt V. Neuropathology and neurodegeneration in rodent brain induced by lentiviral vector-mediated overexpression of a -synuclein. Brain Pathology 13, 364-372 (2003). {5.6} [abstract] [pdf]
Lagoja IM, Pannecouque C, Van Aerschot A, Witvrouw M, Debyser Z, Balzarini J, Herdewijn P, De Clercq E. N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action. J Med Chem, 46(8): 1546-1553. [abstract] [no pdf]
Van Maele B, De Rijck J, De Clercq E, Debyser Z. Impact of the central polypurine tract on the kinetics of HIV-1 vector transduction. J. Virol. 77(8):4685-94. {5.9} [abstract] [pdf]
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, 372-381 (2003). {6.9} [abstract] [pdf]
Witvrouw M, Pannecouque C, Fikkert V, Hantson A, Van Reemortel B, Hezareh M, De Clerck E, Brown SJ. Potent and Selective inhibition of HIV and SIV by prostratin interacting with viral entry. Antivir Chem Chemother 14:321-328. [abstract] [pdf]
Maruyama T, Kozai S, Yamasaki T, Witvrouw M, Pannecouque C, Balzarini J, Snoeck R, Andrei G, De Clercq E. Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV. Antivir Chem Chemother 14(5):271-9. [abstract] [no pdf]
Stamatiou G, Foscolos GB, Fytas G, Kolocouris A, Kolocouris N, Pannecouque C, Witvrouw M, Padalko E, Neyts J, De Clercq E. Heterocyclic rimantadine analogues with antiviral activity.
Bioorg Med Chem. 2003 Dec 1;11(24):5485-92. [abstract] [pdf]
Galtier C, Mavel S, Snoeck R, Andrei G, Pannecouque C, Witvrouw M, Balzarini J, De Clercq E, Gueiffier A. Synthesis and antiviral activities of 3-aralkylthiomethylimidazo[1,2-b]pyridazine derivatives.
Antivir Chem Chemother. 2003 Jul;14(4):177-82. [abstract] [no pdf]
Esquieu D, Peloponese JM, Opi S, Gregoire C, de Mareuil J, Watkins J, Campbell G, Dunot JP, Sturgis J, Witvrouw M, Pannecouque C, de Clercq E, Montembault M, Giang VT, Villieras M, Fargeas V, Lebreton J, Loret EP. Discovery of a Tat HIV-1 inhibitor through computer-aided drug design.
SPECTROSCOPY-AN INTERNATIONAL JOURNAL 17 (4): 639-645 2003. [no abstract, available on web of science] [no pdf]
Anastasi C, Vlieghe P, Hantz O, Hantz O, Schorr O, Pannecouque C, Witvrouw M, De Clercq E, Clayette P, Dereuddre-Bosquete N, Dormont D, Gondois-Rey F, Hirsch I, Kraus JL.
Are 5 '-O-Carbamate-2 ',3 '-dideoxythiacytidine new anti-HIV and anti-HBV nucleoside drugs or prodrugs?
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 13 (15): 2459-2463 AUG 4 2003. [abstract] [pdf]
Okamoto M, Wang X, Debyser Z, De Clercq E, Baba M. Establishment of an in vitro assay system mimicking human immunodeficiency virus type 1-induced neural cell death and evaluation of inhibitors thereof. J Virol Methods. 2003 Mar;108(2):195-203. [abstract] [pdf]
Taymans JM , Leysen JE, Langlois X. Striatal gene expression of RGS2 and RGS4 is specifically mediated by dopamine D1 and D2 receptors: clues for RGS2 and RGS4 functions. J Neurochem. 84(5):1118-27. [abstract] [no pdf]
2002
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. 46, 3954-3962 (2002). {4.6} [abstract] [ pdf]
Debyser Z, Cherepanov P, Van Maele B, De Clercq E, Witvrouw M. In search of authentic inhibitors of HIV-1 integration. Antivir. Chem. Chemother. 13, 1-15. {1.4} [abstract] [pdf]
Pluymers W, Pais G, Van Maele B, Pannecouque C, Fikkert V, Burke TR, De Clercq E, Witvrouw M, Neamati N, Debyser Z. Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives. Antimicrob. Agents Chemother. 46, 3292-3297. {4.6} [abstract] [pdf]
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. {7.5} [abstract] [pdf]
Baekelandt V, Claeys A, Eggermont K, Lauwers E, De Strooper B, Nuttin B, Debyser, Z. Characterization of lentiviral vector mediated gene transfer in adult mouse brain. Human Gene Therapy 13, 841-853 (2002). {6.8} [abstract] [pdf]
Tenenbaum L, Chtarto A, Lehtonen E, Blum D, Baekelandt V, Velu T, Brotchi J, Levivier M. Neuroprotective Gene Therapy for Parkinson’s disease. Current Gene Therapy , 2 (4), 451-483. [abstract] [no pdf]
Vercammen J, Maertens G, Gerard M, De Clercq E, Debyser Z, Engelborghs Y.DNA-induced polymerization of HIV-1 integrase analyzed with fluorescence fluctuation spectroscopy. J Biol Chem. 2002 Oct 11;277(41):38045-52. [abstract] [pdf]
Moukha-chafiq O, Taha ML, Lazrek HB, Vasseur JJ, Pannecouque C, Witvrouw M, De Clercq E.
Synthesis and biological activity of some 4-substituted 1-[1-(2,3-dihydroxy-1-propoxy)methyl-1,2,3-triazol-(4&5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines
FARMACO 57 (1): 27-32. [abstract] [pdf]
Kritsanida M, Mouroutsou A, Marakos P, Pouli N, Papakonstantinou-Garoufalias S, Pannecouque C, Witvrouw M, De Clercq E. Synthesis and antiviral activity evaluation of some new 6-substituted 3-(1-adamantyl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles FARMACO 57 (3): 253-257. [abstract] [pdf]
Salido S, Altarejos J, Nogueras M, Sanchez A, Pannecouque C, Witvrouw M, De Clercq E. CHemical studies of essential oils of Juniperus oxycedrus ssp badia. J Ethnopharmacology 81 (1): 129-134. [abstract] [pdf]
Cos P, Hermans N, De Bruyne T, Apers S, Sindambiwe JB, Witvrouw M, De Clercq E, Berghe DV, Pieters L, Vlietinck AJ. Antiviral activity of Rwandan medicainal plants against human immounodeficiency virus type-1 (HIV-1). Phytomedicine, 9(1): 62-68. [abstract] [pdf]
Kolocouris A, Dimas K, Pannecouque C, Witvrouw M, Foscolos GB, Stamatiou G,
Fytas G, Zoidis G, Kolocouris N, Andrei G,
Snoeck R,
De Clercq E. New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane
thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and
antimicrobial activity evaluation. Bioorg Med Chem Lett. 2002 Mar 11;12(5):723-7. [abstract] [pdf]
Vlieghe P, Clerc T, Pannecouque C, Witvrouw M,
De Clercq E, Salles JP, Kraus JL. Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved
anti-HIV activities. J Med Chem. 2002 Mar 14;45(6):1275-83. [abstract] [pdf]
Bergstrom DE, Lin X, Wood TD, Witvrouw M, Ikeda S, Andrei G, Snoeck R, Schols D, De Clercq E. Polysulfonates derived from metal thiolate complexes as inhibitors of HIV-1 and
various other enveloped viruses in vitro. Antivir Chem Chemother. 2002 May;13(3):185-95. [abstract] [pdf]
Mishra V, Pandeya SN, Pannecouque C, Witvrouw M, De Clercq E. Anti-HIV activity of thiosemicarbazone and semicarbazone derivatives of
(+/-)-3-menthone. Arch Pharm (Weinheim). 2002 May;335(5):183-6. [abstract] [pdf]
Taymans JM , Wintmolders C, Te Riele P, Jurzak M, Groenewegen HJ, Leysen JE, Langlois X. Detailed localization of regulator of G protein signaling 2 messenger ribonucleic acid and protein in the rat brain. Neuroscience 114(1):39-53. [abstract] [pdf]
2001
Pluymers W, De Clercq E, Debyser Z. HIV-1 integration as a target for antiretroviral therapy: a review. Current Drug Targets-Infectious Disorders 1, 133-149. [abstract] [pdf]
Van de Putte T, Zwijzen A, Lonnoy O, Rybin V, Cozijnsen M, Francis A, Baekelandt V, Kozak CA, Zerial M, Huylebroeck D. Mice with a homozygous gene trap vector insertion in gcRacGAP die during pre-implantation development. Mechanisms of Development, 102 (1-2), 33-44. {4.2} [abstract] [pdf]
Debyser Z, Cherepanov P, Pluymers W, De Clercq E. Assays for the evaluation of HIV-1 integrase inhibitors. Methods in Molecular Biology. Nucleases (Humana Press, Ed. C. H. Schein);160, 139-155. [no abstract] [pdf]
Martinez A, Gil C, Castro A, Perez C, Witvrouw M, Pannecouque C, Balzarini J, De Clercq E. Anti-HIV-1 activity of benzothiadiazine dioxide.
Antivir Chem Chemother. 2001 Nov;12(6):347-51. [abstract] [pdf]
Vlieghe P, Bihel F, Clerc T, Pannecouque C, Witvrouw M, De Clercq E, Salles JP, Chermann JC, Kraus JL. New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs:
synthesis and anti-HIV evaluation. J Med Chem. 2001 Mar 1;44(5):777-86. [abstract] [pdf]
Santhosh KC, Paul GC, De Clercq E, Pannecouque C, Witvrouw M, Loftus TL, Turpin JA, Buckheit RW Jr, Cushman M. Correlation of anti-HIV activity with anion spacing in a series of cosalane
analogues with extended polycarboxylate pharmacophores. J Med Chem. 2001 Mar 1;44(5):703-14. [abstract] [pdf]
Lazrek HB, Taourirte M, Oulih T, Barascut JL, Imbach JL, Pannecouque C, Witrouw M, De Clercq E. Synthesis and anti-HIV activity of new modified 1,2,3-triazole acyclonucleosides. Nucleosides Nucleotides Nucleic Acids. 2001 Dec;20(12):1949-60.
[abstract] [pdf]
Moukha-chafiq O, Taha ML, Lazrek HB, Vasseur JJ, Pannecouque C, Witvrouw M, De Clercq E. Synthesis and biological evaluation of some 4-substituted
1-[1-(4-hydroxybutyl)-1,2,3-triazol-(4 &5)-ylmethyl]-1H-pyrazolo- 13,4-dipyrimidines.
Nucleosides Nucleotides Nucleic Acids. 2001 Oct-Nov;20(10-11):1811-821. [abstract] [no pdf]
Moukha-chafiq O, Taha ML, Lazrek HB, Pannecouque C, Witvrouw M, De Clercq E, Barascut JL, Imbach JL. Synthesis and biological activity of 4-substituted
1-[1-(2-hydroxyethoxy)-methyl-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.
Nucleosides Nucleotides Nucleic Acids. 2001 Oct-Nov;20(10-11):1797-810. [abstract] [pdf]
Redwane N, Lazrek HB, Barascut JL, Imbach JL, Balzarini J, Witvrouw M, De Clercq E. Synthesis and biological activities of (Z) and (E) alpha-ethenyl
acyclonucleosides. Nucleosides Nucleotides Nucleic Acids. 2001 Aug;20(8):1439-47. [abstract] [pdf]
Van Laethem K, Witvrouw M, Pannecouque C, Van Remoortel B, Schmit JC, Esnouf R, Kleim JP, Balzarini J, Desmyter J, De Clercq E, Vandamme AM. Mutations in the non-nucleoside binding-pocket interfere with the
multi-nucleoside resistance phenotype. AIDS. 2001 Mar 30;15(5):553-61. [abstract] [pdf]
Barreca ML, Chimirri A, De Luca L, Monforte AM, Monforte P, Rao A, Zappala M, Balzarini J, De Clercq E, Pannecouque C, Witvrouw M. Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents. Bioorg Med Chem Lett. 2001 Jul 9;11(13):1793-6. [abstract] [pdf]
Chimirri A, Monforte P, Rao A, Zappala M, Monforte AM, De Sarro G, Pannecouque C, Witvrouw M, Balzarini J, De Clercq E. Synthesis, biological activity, pharmakinetic properties and molecular modelling of novel 1H,3H-oxazolo[3,4-a]benzimidazoles: non-nucleoside HIV-1 reverse transcriptase inhinitors. Antiviral Chem. Chemotherapy. 2001 12:169-174. [no abstract] [pdf]
Casimiro-Garcia A, De Clercq E, Pannecouque C, Witvrouw M, Loftus TL, Turpin JA, Buckheit RW Jr, Fanwick PE, Cushman M. Synthesis and anti-HIV activity of cosalane analogues incorporating two dichlorodisalicylmethane pharmacophore fragments. Bioorg Med Chem. 2001 Nov;9(11):2827-41. [abstract] [pdf]
Goebel FD, Hemmer R, Schmit JC, Bogner JR, de Clercq E, Witvrouw M, Pannecouque C, Valeyev R, Vandevelde M, Margery H, Tassignon JP. Phase I/II dose escalation and randomized withdrawal study with add-on azodicarbonamide in patients failing on current antiretroviral therapy. AIDS. 2001 Jan 5;15(1):33-45. [abstract] [pdf]
Varvaresou A, Iakovou K, Filippatos E, Souli C, Calogeropoulou T, Ioannidou I, Kourounakis AP, Pannecouque C, Witvrouw M, Padalko E, Neyts J, De Clercq E, Tsotinis A. Synthesis, antiretroviral and antioxidant evaluation of a series of new
benzo[b]furan derivatives. Arzneimittelforschung. 2001 Feb;51(2):156-62. [abstract] [pdf]
Selvam P, Chandramohan M, De Clercq E, Witvrouw M, Pannecouque C. Synthesis and anti-HIV activity of 4-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)
amino]-N(4,6-dimethyl-2-pyrimidinyl)-benzene sulfonamide and its derivatives. Eur J Pharm Sci. 2001 Dec;14(4):313-6. [abstract] [pdf]
Kannan A, De Clercq E, Pannecouque C, Witvrouw M, Hartman TL, Turpin JA, Buckheit RW, Cushman M. Synthesis and anti-HIV activity of a bile acid analog of cosalane Tetrahedron 57 (46): 9385-9391. [abstract] [pdf]
Asres K, Bucar F, Kartnig T, Witvrouw M, Pannecouque C, De Clercq E. Antiviral activity against human immunodeficiency virus type 1 (HIV-1) and type
2 (HIV-2) of ethnobotanically selected Ethiopian medicinal plants. Phytother Res. 2001 Feb;15(1):62-9. [abstract] [pdf]
Chaouni-Benabdallah A, Galtier C, Allouchi H, Kherbeche A, Debouzy JC, Teulade JC, Chavignon O, Witvrouw M, Pannecouque C, Balzarini J, de Clercq E, Enguehard C, Gueiffier A. Synthesis of 3-nitrosoimidazo[1,2-a]pyridine derivatives as potential
antiretroviral agents. Arch Pharm (Weinheim). 334(7):224-8. [abstract] [pdf]
Apers S, Baronikova S, Sindambiwe JB, Witvrouw M, De Clercq E, Vanden Berghe D, Van Marck E, Vlietinck A, Pieters L. Antiviral, haemolytic and molluscicidal activities of triterpenoid saponins from
Maesa lanceolata: establishment of structure-activity relationships. Planta Med. 2001 Aug;67(6):528-32. [abstract] [no pdf]
2000
Baekelandt V, De Strooper B, Nuttin B, Debyser Z. Gene therapeutic strategies for neurodegenerative diseases. Current Opinion in Molecular Therapeutics 2, 540-554. [abstract] [pdf]
Baekelandt V, Claeys A, Cherepanov P, De Clercq E, De Strooper B, Nuttin B, Debyser Z. DNA-dependent protein kinase is not required for efficient lentiviral integration. J. Virology 74, 11278-11285. {5.9} [abstract] [pdf]
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. {5.3} [abstract] [pdf]
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. 2000 Mar 9;43(5):778-83. [abstract] [pdf]
Witvrouw M, Pannecouque C, Desmyter J, De Clercq E, Andries K. In vitro evaluation of the effect of temporary removal of HIV drug pressure. Antiviral Res. 2000 Jun;46(3):215-21.[abstract] [pdf]
Cherepanov P, Pluymers W, Claeys A, De Clercq E, Debyser Z. High level expression of active HIV-1 integrase from a synthetic gene in human cells. FASEB J. 14, 1389-1399. {14.6} [abstract] [pdf]
Van Laethem K, Witvrouw M, Balzarini J, Schmit JC, Sprecher S, Hermans P, Leal M, Harrer T, Ruiz L, Clotet B, Van Ranst M, Desmyter J, De Clercq E, Vandamme AM. Patient HIV-1 strains carrying the multiple nucleoside resistance mutations are cross-resistant to abacavir. AIDS. 2000 Mar 10;14(4):469-71. [no abstract] [no pdf]
Van Laethem K, Schmit JC, Pelemans H, Balzarini J, Witvrouw M, Perez-Perez MJ, Camarasa MJ, Esnouf RM, Aquaro S, Cenci A, Perno CF, Hermans P, Sprecher S, Ruiz L, Clotet B, Van Wijngaerden E, Van Ranst M, Desmyter J, De Clercq E, Vandamme AM. Presence of 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxath iole-2",2"-dioxide) (TSAO)-resistant virus strains in TSAO-inexperienced HIV patients. AIDS Res Hum Retroviruses. 2000 Jun 10;16(9):825-33. [abstract] [pdf]
Van Vaerenbergh K, Van Laethem K, Albert J, Boucher CA, Clotet B, Floridia M, Gerstoft J, Hejdeman B, Nielsen C, Pannecouque C, Perrin L, Pirillo MF, Ruiz L, Schmit JC, Schneider F, Schoolmeester A, Schuurman R, Stellbrink HJ, Stuyver L, Van Lunzen J, Van Remoortel B, Van Wijngaerden E, Vella S, Witvrouw M, Yerly S, De Clercq E, Destmyer J, Vandamme AM. Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues. Antimicrob Agents Chemother. 2000 Aug;44(8):2109-17. [abstract] [pdf]
Paul GC, De Clercq E, Pannecouque C, Witvrouw M, Loftus TL, Turpin JA, Buckheit RW Jr, Cushman M. Identification of optimal anion spacing for anti-HIV activity in a series of cosalane tetracarboxylates. Bioorg Med Chem Lett. 2000 Sep 18;10(18):2149-52. [abstract] [pdf]
Casimiro-Garcia A, De Clercq E, Pannecouque C, Witvrouw M, Stup TL, Turpin JA, Buckheit RW Jr, Cushman M. Synthesis and anti-HIV activity of cosalane analogues incorporating nitrogen in the linker chain. Bioorg Med Chem. 2000 Jan;8(1):191-200. [abstract] [pdf]
Daelemans D, Schols D, Witvrouw M, Pannecouque C, Hatse S, van Dooren S, Hamy F, Klimkait T, de Clercq E, VanDamme AM. A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry. Mol Pharmacol. 2000 Jan;57(1):116-24. [abstract] [pdf]
Santhosh KC, De Clercq E, Pannecouque C, Witvrouw M, Loftus TL, Turpin JA, Buckheit RW, Cushman M. Anti-HIV activity of a series of cosalane amino acid conjugates. Bioorg Med Chem Lett. 2000 Nov 20;10(22):2505-8. [abstract] [pdf]
Péloponèse JM Jr, Grégoire C, Opi S, Esquieu D, Sturgis J, Lebrun E, Meurs E, Collette Y, Olive D, Aubertin AM, Witvrouw M, Pannecouque C, De Clercq E, Bailly C, Lebreton J, Loret EP.1H-13C nuclear magnetic resonance assignment and structural characterization of HIV-1 Tat protein. C R Acad Sci III. 2000 Oct;323(10):883-94. [abstract] [pdf]
Pluymers W, Neamati N, Pannecouque C, Fikkert V, Marchand C, Burke TR Jr, 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. 2000 Sep;58(3):641-8. [abstract] [pdf]
Kavimani S, Jaykar B, De Clercq E, Pannecoucque C, Witvrouw M. Studies on anti-HIV activity of Indigofera tinctoria. Hamdard XLIII:5-7. [no abstract] [pdf]
1999
Oelrichs RB, Vandamme AM, Van Laethem K, Debyser Z, McCutchan FE, Deacon NJ. Full-length genomic sequence of an HIV type 1 subtype G from Kinshasa. AIDS Research and Human Retroviruses 15, 585-589. {3} [PubMed] [pdf]
Pluymers W, Cherepanov P, Schols D, De Clercq E, Debyser Z. Nuclear localization of human immunodeficiency virus type 1 integrase expressed as a fusion protein with green fluorescent protein. Virology 258, 327-332. {3.5} [abstract] [pdf]
Cherepanov P, Surratt D, Toelen J, Pluymers W, Griffith J, Desmyter J, De Clercq E, Debyser Z. Activity of recombinant HIV-1 integrase on mini-HIV DNA. Nucleic Acids Research 27, 2202-2210 (1999). {4.2} [abstract] [pdf]
Lin Z, Neamati N, Zhao H, Kiryu Y, Turpin JA, Aberham C, Strebel K, Kohn K, Witvrouw M, Pannecouque C, Debyser Z, De Clercq E, Rice WG, Pommier Y, Burke TR. Chicoric acid analogues as HIV-1 integrase inhibitors. J. Medicinal Chemistry 42, 1401-1414. {3.6} [abstract] [pdf]
Vandamme AM, Van Laethem K, Schmit JC, Van Wijngaerden E, Reynders M, Debyser Z, Witvrouw, M, Van Ranst M, De Clercq E, Desmyter J. Long-term stability of HIV viral load and infectivity in whole blood. Eur. J. of Clinical Investigation 29, 445-452. {1.7} [abstract] [pdf]
Moechars D, Dewachter I, Lorent K, Reversé D, Baekelandt V, Tesseur I, Spittaels K, Naidu A, Van Den Haute C, Checler F, Godaux E, Cordell B, Van Leuven F. (1999) Early phenotypic changes in transgenic mice that overexpress different mutants of amyloid precursor protein in brain. J. Biol. Chem. 274: 6483-6492. {7.4} [abstract] [pdf]
Herreman A, Hartmann D, Annaert W, Saftig P, Craessaerts K, Serneels L, Umans L, Schrijvers V, Checler F, Vanderstichele H, Baekelandt V, Dressel R, Cupers P, Huylebroeck D, Zwijsen A, Van Leuven F, De Strooper B (1999). Presenilin 2 deficiency causes a mild pulmonary phenotype and no changes in amyloid precursor protein processing but enhances the embryonic lethal phenotype of presenilin 1 deficiency. PNAS, 96, 11872-7. {10.8} [abstract] [pdf]
Baekelandt V, Moechars D, Laenen I, Lorent K, Van Leuven F (1999). Disturbance of the glutamatergic system in mice transgenic for the amyloid precursor protein. Alzheimer’s Reports , 2, 359-368. {0.8} [no PubMed] [no pdf]
Van Gelder J, Witvrouw M, Pannecouque C, Henson G, Bridger G, Naesens L, De Clercq E, Annaert P, Shafiee M, Van den Mooter G, Kinget R, Augustijns P. Evaluation of the potential of ion pair formation to improve the oral absorption of two potent antiviral compounds, AMD3100 and PMPA. Int J Pharm. 1999 Sep 20;186(2):127-36 [abstract] [pdf]
Chimirri A, Grasso S, Monforte P, Rao A, Zappala M, Monforte AM, Pannecouque C, Witvrouw M, Balzarini J, De Clercq E. Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. Antivir Chem Chemother. 1999 Jul;10(4):211-7. [abstract] [pdf]
Van Laethem K, Van Vaerenbergh K, Schmit JC, Sprecher S, Hermans P, De Vroey V, Schuurman R, Harrer T, Witvrouw M, Van Wijngaerden E, Stuyver L, Van Ranst M, Desmyter J, De Clercq E, Vandamme AM. Phenotypic assays and sequencing are less sensitive than point mutation assays for detection of resistance in mixed HIV-1 genotypic populations. J Acquir Immune Defic Syndr. 1999 Oct 1;22(2):107-18. [abstract] [pdf]
Witvrouw M, Pannecouque C, Van Laethem K, Desmyter J, De Clercq E, Vandamme AM. Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV. AIDS. 1999 Aug 20;13(12):1477-83. [abstract] [pdf]
Witvrouw M, Pannecouque C, De Clercq E, Fernandez-Alvarez E, Marco JL. Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV. AIDS. 1999 Aug 20;13(12):1477-83. [abstract] [pdf]
Thormar H, Bergsson G, Gunnarsson E, Georgsson G, Witvrouw M, Steingrimsson O, De Clercq E, Kristmundsdottir T. Hydrogels containing monocaprin have potent microbicidal activities against sexually transmitted viruses and bacteria in vitro. Sex Transm Infect. 1999 Jun;75(3):181-5. [abstract] [pdf]
Pandeya SN, Yogeeswari P, Sriram D, de Clercq E, Pannecouque C, Witvrouw M. Synthesis and screening for anti-HIV activity of some N-Mannich bases of isatin derivatives. Chemotherapy. 1999 May-Jun;45(3):192-6. [abstract] [pdf]
Arranz ME, Diaz JA, Ingate ST, Witvrouw M, Pannecouque C, Balzarini J, De Clercq E, Vega S. Synthesis and anti-HIV activity of 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazines (TTDs): a new family of HIV-1 specific non-nucleoside reverse transcriptase inhibitors. Bioorg Med Chem. 1999 Dec;7(12):2811-22. [abstract] [pdf]
Cushman M, Insaf S, Paul G, Ruell JA, De Clercq E, Schols D, Pannecouque C, Witvrouw M, Schaeffer CA, Turpin JA, Williamson K, Rice WG. Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency. J Med Chem. 1999 May 20;42(10):1767-77. [abstract] [pdf]
Ruell JA, De Clercq E, Pannecouque C, Witvrouw M, Stup TL, Turpin JA, Buckheit RW Jr, Cushman M. Synthesis and anti-HIV activity of cosalane analogues with substituted benzoic acid rings attached to the pharmacophore through methlylene amide linkers. J Org Chem 1999, 64, 5858-5866. [no abstract] [pdf]
Swart PJ, Harmsen MC, Kuipers ME, Van Dijk AA, Van Der Strate BW, Van Berkel PH, Nuijens JH, Smit C, Witvrouw M, De Clercq E, de Bethune MP, Pauwels R, Meijer DK. Charge modification of plasma and milk proteins results in antiviral active compounds. J Pept Sci. 1999 Dec;5(12):563-76. [abstract] [pdf]
Cabrera C, Witvrouw M, Gutierrez A, Clotet B, Kuipers ME, Swart PJ, Meijer DK, Desmyter J, De Clercq E, Este JA. Resistance of the human immunodeficiency virus to the inhibitory action of negatively charged albumins on virus binding to CD4. AIDS Res Hum Retroviruses. 1999 Nov 20;15(17):1535-43. [abstract] [pdf]
Kuipers ME, Swart PJ, Witvrouw M, Este JA, Reymen D, De Clercq E, Meijer DK. Anti-HIV-1 activity of combinations and covalent conjugates of negatively charged human serum albumins (NCAs) and AZT. J Drug Target. 1999;6(5):323-35. [abstract] [pdf]
Bridger GJ, Skerlj RT, Padmanabhan S, Martellucci SA, Henson GW, Struyf S, Witvrouw M, Schols D, De Clercq E. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4. J Med Chem. 1999 Sep 23;42(19):3971-81. [abstract] [pdf]
De Bruyne T, Pieters L, Witvrouw M, De Clercq E, Vanden Berghe D, Vlietinck AJ. Biological evaluation of proanthocyanidin dimers and related polyphenols. J Nat Prod. 1999 Jul;62(7):954-8. [abstract] [no pdf]
Niyonzima G, Laekeman G, Witvrouw M, Van Poel B, Pieters L, Paper D, De Clercq E, Franz G, Vlietinck AJ. Hypoglycemic, anticomplement and anti-HIV activities of Spathodea campanulata stem bark. Phytomedicine. 1999 Mar;6(1):45-9. [abstract]
[no pdf]
1998
Park K, Debyser Z, Tabor S, Richardson CC, Griffith JD. Formation of a DNA loop at the replication fork generated by bacteriophage T7 replication proteinscteriophage proteins. J. Biol. Chem. 273, 5260-5270. {6.9} [abstract] [pdf]
Debyser Z, Van Wijngaerden E, Van Laethem K, Beuselinck K, Reynders M, De Clercq E, Desmyter J, Vandamme AM. Failure to quantify viral load with two of the three commercial methods in a pregnant woman harboring an HIV type 1 subtype G strain. AIDS Research and Human Retroviruses, 14, 453-459. {3} [abstract] [no pdf]
Esté JA, Cabrera C, Schols D, Cherepanov P, Gutierrez A, Witvrouw M, Pannecouque C, Debyser Z, Rando RF, Clotet B, Desmyter J, De Clercq E. Human immunodeficiency virus glycoprotein gp120 as the primary target for the antiviral action of AR177 (zintevir). Mol. Pharmacol., 53, 340-345. {4.9} [abstract] [pdf]
Moechars D, Lorent K, Dewachter I, Baekelandt V, De Strooper B, Van Leuven F (1998). Transgenic mice expressing an a -secretion mutant of the amyloid precursor protein in the brain develop a progressive CNS disorder. Behavioural Brain Research, 95, 55-64. {2.3} [abstract] [pdf]
Arranz ME, Diaz JA, Ingate ST, Witvrouw M, Pannecouque C, Balzarini J, De Clercq E, Vega S. Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives: as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication. J. Med. Chem., 41 : 4109-4117 (1998). {4.1} [abstract] [pdf]
Borges JE, Fernandez F, Garcia X, Hergueta AR, Lopez C, Andrei G, Snoeck R, Witvrouw M, Balzarini J, De Clercq E. Novel carbocyclic nucleosides containing a cyclobutyl ring. Guanosine and adenosine analogues. Nucleosides & Nucleotides, 17 : 1237-1253 (1998). {0.6} [abstract] [pdf]
Chimirri A, Grasso S, Monforte AM, Monforte P, Rao A, Zappala M, Bruno G, Scopelliti R, Pannecouque C, Witvrouw M, De Clercq E. Synthesis, structure and in vitro anti-HIV activity of novel 3-methyl-1H,3H-thiazolo[3,4-a]benzimidazoles. Antiviral Chem. Chemother., 9 : 431-438. {2.4} [abstract] [no pdf]
Gueiffier A, Mavel S, Lhassani M, Elhakmaoui A, Snoeck R, Andrei G, Chavignon O, Teulade JC, Witvrouw M, Balzarini J, De Clercq E, Chapat JP. Synthesis of imidazo[1,2-a]pyridines as antiviral agents. J. Med. Chem., 41 : 5108-5112. {4.1} [abstract] [no pdf]
Jonckheere H, Witvrouw M, De Clercq E, Anné J. Lamivudine resistance of HIV type 1 does not delay development of resistance to nonnucleoside HIV type 1-specific reverse transcriptase inhibitors as compared with wild-type HIV type 1. AIDS Res. Hum. Retroviruses, 14 : 249-253. {3.0} [abstract] [no pdf]
Lazrek HB, Rochdi A, Khaider H, Barascut JL, Imbach JL, Balzarini J, Witvrouw M, De Clercq E. Synthesis of (Z) and (E) a-alkenyl phosphonic acid derivatives of purines and pyrimidines. Tetrahedron, 54 : 3807-3816. {2.6} [no abstract] [pdf]
Leydet A, Moullet C, Roque JP, Witvrouw M, Pannecouque C, Andrei G, Snoeck R, Neyts J, Schols D, De Clercq E. Polyanion inhibitors of human immunodeficiency virus and others viruses. Part VII. Polyanionic compounds and polyzwitterrionic compounds derived from cyclodextrins as inhibitors of HIV transmission. J. Med. Chem., 41 : 4927-4932. {4.1} [abstract] [no pdf]
Mishra V, Pandeya SN, De Clercq E, Pannecouque C, Witvrouw M. Synthesis of aryl semicarbazone of 4-aminoacetophenone and their anti-HIV activity. Pharm. Acta. Helv., 73 : 215-218. [abstract] [no pdf]
Pandeya SN, Sriram D, De Clercq E, Pannecouque C Witvrouw M. Anti-HIV activity of some mannich bases of isatin derivatives. Indian J. Pharm. Sci., 60 : 207-212. [no Pubmed] [no pdf]
Schmit JC, Martinez-Picado J, Ruiz L, Tural C, Van Laethem K, Cabrera C, Ibanez A, Puig T, Witvrouw M, De Clercq E, Clotet B, Vandamme AM. Evolution of HIV drug resistance in zidovudine/zalcitabine - and zidovudine/didanosine - experienced patients receiving lamivudine - containing combination therapy. Antiviral Therapy, 3 : 81-88. {4.5} [no abstract] [no pdf]
Schmit JC, Van Laethem K, Ruiz L, Hermans P, Sprecher S, Sönnerborg A, Leal M, Harrer T, Clotet B, Arendt V, Lissen E, Witvrouw M, Desmyter J, De Clercq E, Vandamme AM. Multiple dideoxynucleoside analogue-resistant (MddNR) HIV-1 strains isolated from patients from different European countries. AIDS, 12 : 2007-2015 (1998). {8.0} [abstract] [pdf]
Witvrouw M, Arranz ME, Pannecouque C, Declercq R, Jonckheere H, Schmit JC, Vandamme AM, Diaz JA, Desmyter J, Esnouf R, Van Meervelt L, Vega S, Balzarini J, De Clercq E. 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives : a new class non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs) with anti-HIV-1 activity. Antimicrob Agents Chemother 42:618-623. {4.0} [abstract] [pdf]
Witvrouw M, Daelemans D, Pannecouque C, Neyts J, Andrei G, Snoeck R, Vandamme AM, Balzarini J, Desmyter J, Baba M, De Clercq E. Broad-spectrum antiviral activity of the piperazinylquinolone derivative K-12 and its mechanism of action. Antiviral. Chem. Chemother 9:403-411. {2.4} [abstract] [pdf]
1997
Debyser Z, Reynders M, Goubau P, Desmyter J. Comparison of three ELISA techniques and an indirect immunofluorescense assay for the serological diagnosis of Epstein-Barr virus infection. Clinical and Diagnostic Virology 8 : 71-81 (1997). [abstract] [pdf]
Cherepanov P, Este JA, Rando RF, Ojwang JO, Reekmans G, Steinfeld R, David G, De Clercq E, Debyser Z. Mode of interaction of G-quartets with the integrase of human immunodeficiency virus type 1. Mol Pharmacol. 52(5):771-80. [abstract] [pdf]
Irwin N, Baekelandt V, Goritchenko L, Benowitz LI. Identification of two proteins that bind to a pyrimidine-rich sequence in the 3’-untranslated region of GAP-43 mRNA. Nucleic Acids Research 25(6):1281-1288. [abstract] [pdf]
Balzarini J, Kruining J, Wedgwood O, Pannecouque C, Aquaro S, Perno CF, Naesens L, Witvrouw M, Heijtink R, De Clercq E, McGuigan C. Conversion of 2’,3’-dideoxyadenosine (ddA) and 2’,3’-didehydro-2’,3’-dideoxyadenosine (d4A) to their corresponding aryloxyphosphoramidate derivatives markedly potentiates their activity against human immunodeficiency virus and hepatitis B virus. FEBS Letters, 410 : 324-328 (1997). [abstract] [pdf]
Balzarini J, Vahlenkamp T, Egberink H, Hartmann K, Witvrouw M, Pannecouque C, Casara P, Navé JF, De Clercq E. Antiretroviral activities of acyclic nucleoside phosphonates [9-(2-phosphonylmethoxyethyl)adenine, 9-(2-phosphonylmethoxyethyl) guanine, (R)-9-(2-phosphonylmethoxypropyl)adenine, and MDL 74,968] in cell cultures and murine sarcoma virus-infected newborn NMRI mice. Antimicrob. Agents Chemother., 41, 611-616 (1997). [abstract] [pdf]
Chimirri A, Grasso S, Molica C, Monforte AM, Monforte P, Zappala M, Bruno G, Nicolo F, Witvrouw M, Jonckheere H, Balzarini J, De Clercq E. Structural features and anti-HIV activity of the isomers of 1-(2’,6’-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole, a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Antiviral. Chem. Chemother., 8 : 363-370 (1997). [no abstract] [pdf]
Daelemans D, Esté JA, Witvrouw M, Pannecouque C, Jonckheere H, Perno CF, De Clercq E, Vandamme AM. S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of Tat transactivation. Mol. Pharmacol., 52 : 1157-1163 (1997). [abstract] [pdf]
Fytas G, Stamatiou G, Foscolos GB, Kolocouris A, Kolocouris N, Witvrouw M, Pannecouque C, De Clercq E. Synthesis and anti-HIV activity of some new aminoadamantane heterocycles. Bioorg.Med. Chem. Letters, 7 : 1887-1890 (1997). [abstract] [pdf]
Kren V, Piskala A, Sedmera P, Havlicek V, Prikrylova V, Witvrouw M, De Clercq E. Synthesis and antiviral evaluation of N-b-D-ribosides of ergot alkaloids. Nucleosides & Nucleotides, 16 : 97-106 (1997). [no abstract - available on Web of Science] [pdf]
Ingate ST, Marco JL, Witvrouw M, Pannecouque C, De Clercq E. Studies into the synthesis of derivatives of 4-amino-2,3-dihydroisothiazole 1,1-dioxides and 4-amino-1,2-oxathiole 2,2-dioxides: The search for linked π-system containing analogues as potential inhibitors of HIV-1 reverse transcriptase.
Tetrahedron, 53 : 17795-17814 (1997). [abstract] [pdf]
Kren V, Olsovsky P, Havlicek V, Sedmera P, Witvrouw M, De Clercq E. Synthesis and biological activity of N-deoxyribosides of ergot alkaloides. Tetrahedron, 53 : 4503-4510 (1997). [abstract] [pdf]
Leydet A, Barragan V, Boyer B, Lamaty G, Roque J P, Witvrouw M, Este J, Snoeck R, Andrei G, De Clercq E. Polyanion inhibitors of human immunodeficiency virus and other viruses. Part V. Telomerized anionic surfactants derived from amino acids. J. Med. Chem., 40 : 342-349 (1997). [abstract] [no pdf]
Leydet A, Jeantet-Segonds C, Bouchité C, Moullet C, Boyer B, Roque JP, Witvrouw M, Esté J, Snoeck R, Andrei G, De Clercq E. Polyanion inhibitors of human immunodeficiency virus and other virusus. Part VI.-Micelle-like anti-HIV polyanionic compounds based on a carbohydrate core. J Med Chem, 40 : 350-356 (1997). [abstract] [no pdf]
Song R, Witvrouw M, Schols D, Robert A, Balzarini J, De Clercq E, Bernadou J, Meunier B. Anti-HIV activities of anionic metalloporphyrins and related compounds. Antiviral. Chem. Chemother., 8 : 85-97 (1997). [no abstract - available on Web of Science] [pdf]
Witvrouw M, Balzarini J, Pannecouque C, Jhaumeer-Laulloo S, Esté J, Schols, D, Cherepanov P, Schmit JC, Debyser Z, Vandamme AM, Desmyter J, Ramadas R, De Cercq E. SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus. Antimicrob. Agents Chemother., 41 : 262-268 (1997). [abstract] [pdf]
Witvrouw M, De Clercq E. Review: Sulfated polysaccharides extracted from sea algae as potential antiviral drugs. Gen Pharmac, 29 : 497-511 (1997). [abstract] [pdf]
Witvrouw M, Schmit JC, Van Remoortel B, Daelemans D, Esté J, Vandamme AM, Desmyter J, De Clercq E. Cell type-dependent effect of sodium valproate on human immunodeficiency virus (HIV) type 1 replication in vitro. AIDS Res. Hum. Retroviruses, 13 : 187-192 (1997). [abstract] [pdf]
1996
Debyser Z, De Clercq E. Antiviral therapy for HIV infection. EOS, Journal of Immunology and Immunopharmacology, 2 : vol. XVI (1996). [no abstract or pdf]
Jonckheere H, De Vreese K, Debyser Z, Vandekerckhove J, Balzarini J, Desmyter J, De Clercq E, Anne J. A two plasmid co-expression system in Escherichia coli for the production of virion-like reverse transcriptase of the human immunodeficiency virus type 1. J Virol Methods. 1996 Sep;61(1-2):113-25. [abstract] [pdf]
Debyser Z, De Clercq E. Chemical crosslinking of the subunits of HIV-1 reverse transcriptase. Protein Science. 5 : 278-286 (1996). [abstract] [pdf]
Baekelandt V, Eysel UT, Orban GA, Vandesande F. (1996) Long-term effects of retinal lesions on growth-associated protein 43 (GAP-43) expression in the visual system of adult cats. Neurosci. Lett., 208, 113-116. [abstract] [pdf]
Balzarini J, Aquaro S, Perno CF, Witvrouw M, Holy A, De Clercq E. Activity of the (R)-enantiomers of 9-(2-phosphonylmethoxypropyl)-adenine ((R)-PMPA) and 9-(2-phosphonylmethoxypropyl)- 2,6-diaminopurine((R)-PMPDAP) against human immuno-deficiency virus in different human cell systems. Biochem. Biophys. Res. Commun., 219: 337-341 (1996). [abstract] [pdf]
Balzarini J, Pelemans H, Aquaro S, Perno CF, Witvrouw M, Schols D, De Clercq E, Karlsson A. Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 (HIV-1) replication. Mol. Pharmacol., 50 : 394-401 (1996). [abstract] [pdf]
Bellarosa D, Antonelli G, Bambacioni F, Giannotti D, Viti G, Nannicini R, Giachetti A, Dianzani F, Witvrouw M, Pauwels R, Desmyter J, De Clercq E. New arylpyrido diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase. Antiviral Res., 30 : 109-124 (1996). [abstract] [pdf]
Bridger GJ, Skerlj RT, Padmanabhan S, Martellucci SA, Henson GW, Abrams MJ, Joao HC, Witvrouw M, De Vreese K, Pauwels R, De Clercq E. Synthesis and structure activity relationships of phenylenebis(methylene) linked bis-tetraazamacrocycles that inhibit HIV replication 2. Effect of heteroaromatic linkers on the activity of bicyclams. J. Med. Chem., 39 : 109-119 (1996). [abstract] [pdf]
Esté JA, De Vreese K, Witvrouw M, Schmit JC, Vandamme AM, Anné J, Desmyter J, Henson G, Bridger G, De Clercq E. Antiviral activity of the bicyclam derivative SID791 (JM3100) against drug-resistant strains of human immunodeficiency virus type 1. Antiviral Res., 29 : 297-307 (1996). [abstract] [no pdf]
Groziak MP, Lin R, Stevens WC, Wotring LL, Balzarini J, Witvrouw M, De Clercq E. Definitive solution structures for the 6-formylated versions of 1-beta-D-ribofuranosyl-,1-(2’-deoxy beta-D-ribofuranosyl)-, and 1-beta-D-arabinofurano
syluracil. Nucleosides & Nucleotides, 15 : 1041-1057 (1996). [abstract on Web of Science] [no pdf]
Gueiffier A, Lhassani M, Elhakmaoui A, Snoeck R, Andrei G, Chavignon O, Teulade JC, Kerbal A, Essassi EM, Debouzy JC, Witvrouw M, Blache Y, Balzarini J, De Clercq E, Chapat JP. Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents. J. Med. Chem., 39 : 2856-2859 (1996). [abstract] [pdf]
Leydet A, Barthélémy P, Boyer B, Lamaty G, Roque JP, Witvrouw M, De Clercq E. Polyanion inhibitors of human immunodeficiency virus. Part IV.-Polymerized anionic surfactants : influence of the density and distribution of anionic groups on the antiviral activity. Bioorg. Med.Chem. Letters, 6 : 397-402 (1996). [abstract on Web of Science] [no pdf]
Leydet A, El Hachemi H, Boyer B, Lamaty G, Roque JP, Schols D, Snoeck R, Andrei G, Ikeda S, Neyts J, Reymen D, Este J, Witvrouw M, De Clercq E. Polyanion inhibitors of human immunodeficiency virus and other viruses. Part II. Polymerized anionic surfactants derived from amino acids and dipeptides. J. Med. Chem., 39 : 1626-1634 (1996). [abstract] [no pdf]
Locher CP, Witvrouw M, de Béthune MP, Burch MT, Mower HF, Davis H, Lasure A, Pauwels R, De Clercq E, Vlietinck AJ. Antiviral activity of Hawaiian medicinal plants against human immunodeficiency virus type-1 (HIV-1). J. Phytomedicine, 2: 259-264 (1996). [abstract on Web of Science] [pdf]
Maruyama T, Sato Y, Oto Y, Takahashi Y, Snoeck R, Andrei G, Witvrouw M, De Clercq E. Synthesis and antiviral activity of 6-chloropurine arabinoside and its 2'-deoxy-2'-fluoro derivative. Chem Pharm Bull (Tokyo). 1996 Dec;44(12):2331-4. [abstract] [no pdf]
Reymen D, Witvrouw M, Esté JA, Neyts J, Cushman M, De Clercq E. Mechanism of the antiviral activity of new aurintricarboxylic acid analogues. Antiviral Chem. Chemother., 7 : 142-152 (1996). [abstract on Web of Science] [no pdf]
Schmit, J.-C., Cogniaux, J.,Hermans, P., Van Vaeck, C., Sprecher, S., Van Remoortel, B., Witvrouw, M., Balzarini, J., Desmyter, J., De Clercq, E. & Vandamme A.-M. Multiple drug resistance to nucleoside analogues and non-nucleoside reverse transcriptase inhibitors in an efficiently replicating HIV-1 patient strain. J. Infect. Dis., 174 : 962-968 (1996). [abstract] [no pdf]
Vandamme AM, Schmit J, Van Dooren S, Van Laethem K, Gobbers E, Kok W, Goubau P, Witvrouw M, Peetermans W, De Clercq E, Desmyter J. Quantification of HIV-1 RNA in plasma: Comparable results with the NASBA® HIV-1 RNA QT and the AMPLICOR® HIV monitor test. J. Acquir. Immune Defic. Syndr. Hum. Retrovirol., 13 : 127-139 (1996). [abstract] [no pdf]
Vandevelde M, Witvrouw M, Schmit JC, Sprecher S, De Clercq E, Tassignon JP. ADA, a potential anti-HIV drug. AIDS Res. Hum. Retroviruses, 12 : 567-568 (1996). [no abstract] [no pdf]
Witvrouw M, Seifert JM, Henson GW, Martellucci SA, Desmyter J, De Clercq E. Pharmacokinetics of the anti-HIV bicyclam SID791 (JM3100) in rabbits, as determined by both analytical and bioassay methods. Antiviral. Chem. Chemother., 7 : 27-30 (1996). [no abstract] [pdf]
1995
Debyser Z. Novel DNA substrates for studying replication mechanisms. Synthetic replication forks. Methods in Enzymology, 262 : 457-466 (1995). [no abstract or pdf]
Thormar H, Balzarini J, Debyser Z, Witvrouw M, Desmyter J, De Clercq E. Inhibition of visna virus replication in sheep choroid plexus cell cultures by selected anti-HIV agents. Antiviral Research, 27 : 49-57 (1995). [abstract] [pdf]
Cushman M, Wang P, Reymen D, Esté J, Witvrouw M, Neyts J, De Clercq E. Anti-HIV and anti-HCMV activities of new aurintricarboxylic acid analogues. Antiviral Chem. Chemother., 6 : 179-186 (1995). [abstract on Web of Science] [pdf]
Esté J, Witvrouw, M, Tu J, Desmyter J, De Clercq E, Vandamme AM. Inhibition of HIV-1 Tat mediated transactivation by oncostatin M in HL-tat cells. AIDS Res. Hum. Retroviruses, 11 : 1355-1358 (1995). [abstract] [no pdf]
Neyts J, Reymen D, Letourneur D, Jozefonvicz J, Este J, Andrei G, McKenna P, Witvrouw M, Ikeda S, Clement J, De Clercq E. Differential activity of derivatized dextrans. Biochem. Pharmacol., 50 : 743-751 (1995). [abstract] [pdf]
1994
Pauwels R, Andries K, Debyser Z, Kukla MJ , Schols D, Breslin HJ, Woestenborghs R, Desmyter J, Janssen MAC, De Clercq E, Janssen PAJ. New tetrahydroimidazo[4,5,1-jk] [1,4]-benzodiazepin-2(1H)-one and -thione derivatives are potent inhibitors of HIV-1 replication and are synergistic with 2',3'-dideoxynucleoside analogues. Antimicrob. Agents Chemother., 38 : 2863-2870 (1994). [abstract] [pdf]
Debyser Z, Tabor S, Richardson CC. Coordination of leading and lagging strand synthesis at the replication fork of bacteriophage T7. Cell, 77, 157-166 (1994). [abstract] [no pdf]
De Clercq E, Yamamoto N, Pauwels R, Balzarini J, Witvrouw M, De Vreese K, Debyser Z, Rosenwirth B, Datema R, Thornton D, Skerlj R, Bridger G, Henson G, Abrams M. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob. Agents Chemother., 38, 668-674 (1994). [abstract] [pdf]
Vandamme AM, Debyser Z, Pauwels R, De Vreese K, Goubau P, Youle M, Gazzard B, Stoffels PA, Cauwenbergh GF, Anné J, Andries K, Janssen PAJ, Desmyter J, De Clercq E. Characterization of HIV-1 strains isolated from patients treated with TIBO R82913. AIDS Res. Human Retrovir., 10 : 39-46 (1994). [abstract] [no pdf]
Baekelandt V, Arckens L, Annaert W, Eysel UT, Orban GA, Vandesande F. (1994) Alterations in GAP-43 and synapsin immunoreactivity provide evidence for synaptic reorganization in adult cat dorsal lateral geniculate nucleus following retinal lesions. Eur. J. Neurosci., 6,754-765. [abstract] [no pdf]
Damonte E, Neyts J, Pujol CA, Snoeck R, Andrei G, Ikeda S, Witvrouw M, Reymen D, Haines H, Matulewicz MC, Cerezo A, Coto CE, De Clercq E. Antiviral activity of a sulfated polysaccharide from the red seaweed Nothogenia fastigiata. Biochem. Pharmacol., 47 : 2187-2192 (1994). [abstract] [no pdf]
Witvrouw M, Desmyter J, De Clercq E. Antiviral portrait series: 4. Polysulfates as inhibitors of HIV and other enveloped viruses. Antiviral Chem. Chemother., 5 : 345-359 (1994). [abstract on Web of Science] [pdf]
Witvrouw M, Este JA, Mateu MQ, Reymen D, Andrei G, Snoeck R, Ikeda S, Pauwels R, Bianchini NV, Desmyter J, De Clercq E. Activity of a sulfated polysaccharide extracted from the red seaweed Aghardhiella tenera against human immunodeficiency virus and other enveloped viruses. Antiviral Chem. Chemother., 5: 297-303 (1994). [abstract on Web of Science] [pdf]
Otake T, Schols D, Witvrouw M, Neasens L, Nakashima H, Moriya T, Kurita H, Matsumoto K, Ueba N, De Clercq E. Modified Cyclodextrion sulfates (MCDS11) have potent inhibitory activity against HIV and high oral bioavailability. Antiviral Chem. Chemother., 5 : 155-161. [abstract on Web of Science] [no pdf]
1993
Thormar H, Balzarini J, Holy A, Jindrich J, Dvorakova H, Debyser Z, Desmyter J, De Clercq, E. Inhibition of visna virus replication by 2',3'-dideoxynucleosides and acyclic nucleoside phosphonate analogues. Antimicrob. Agents Chemother., 37 : 2540-2544 (1993). [abstract] [pdf]
Debyser Z, De Vreese K, Knops-Gerrits PP, Baekelandt V, Bhikhabhai R, Strandberg B, Pauwels R, Anné J, Desmyter J, De Clercq E. Kinetics of different human immunodeficiency virus type 1 reverse transcriptases resistant to human immunodeficiency virus type 1-specific reverse transcriptase inhibitors. Mol. Pharmacol., 43: 521-526 (1993). [abstract] [pdf]
Pauwels R, Andries K, Debyser Z, Van Daele P, Schols D, Stoffels P, De Vreese K, Woestenborghs R, Vandamme AM, Janssen CGM, Anné J, Cauwenbergh G, Desmyter J, Heykants J, Janssen MAC, De Clercq E, Janssen PAJ. Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of alfa-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase. Proc. Natl. Acad. Sci. USA, 90: 1711-1715 (1993). [abstract] [pdf]
Bârzu T, Level M, Petitou M, Lormeau JC, Choay J, Schols D, Baba M, Pauwels R, Witvrouw M, De Clercq E. Preparation and anti-HIV activity of O-acylated heparin and dermatan sulfate derivatives with low anticoagulant effect. J. Med. Chem., 36 : 3546-3555 (1993). [abstract] [no pdf]
1992
Pauwels R, Andries K, Debyser Z, Kukla M, Schols D, Desmyter J & De Clercq E, Janssen PAJ . TIBO derivatives : a new class of highly potent and specific inhibitors of HIV-1 replication. Biochem. Soc. Trans., 20: 509-512 (1992). [no abstract] [no pdf]
Yamamoto N, Schols D, De Clercq E, Debyser Z, Pauwels R, Balzarini J, Nakashima H, Baba M, Hosoya M, Snoeck R, Neyts J, Andrei G, Murrer BA, Theobald B, Bossard G, Henson G, Abrams M, Picker D. Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents. Mol. Pharmacol 42: 1109-1117 (1992). [abstract] [pdf]
Baba M, Debyser Z, Shigeta S, De Clercq E. Highly potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by the HIV-1-specific reverse transcriptase inhibitors. Drugs of the Future, 17(10): 891-897 (1992). [no abstract] [no pdf]
Debyser Z, Vandamme A, Pauwels R, Baba M, Desmyter J, De Clercq E. Kinetics of inhibition of endogenous human immunodeficiency virus type 1 reverse transcription by 2',3'-dideoxynucleoside 5'-triphosphate, tetrahydroimidazo-[4,5,1-jk][1,4]-benzodiaze-pin-2(1H)-thione, and 1-[(2-hydroxyethoxy)methyl]-6-(phenyl-thio)thymine derivatives. J Biol Chem 267: 11769-11776 (1992). [abstract] [pdf]
De Clercq E, Yamamoto N, Pauwels R, Baba M, Schols D, Nakashima H, Balzarini J, Debyser Z, Murrer BA, Schwartz D, Thornton D, Bridger G, Fricker S, Henson G, Abrams M, Picker D. Potent and selective inhibition of human immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event. Proc. Natl. Acad. Sci. USA, 89: 5286-5290 (1992). [abstract] [pdf]
Debyser Z, De Vreese K, Pauwels R, Yamamoto N, Anné J, De Clercq E, Desmyter J. Differential inhibitory effects of TIBO derivatives on different strains of simian immunodeficiency virus. J. Gen. Virol., 73: 1799-1804 (1992). [abstract] [no pdf]
Debyser Z, Pauwels R, Baba M, Desmyter J, De Clercq E. Common features in the interaction of tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione and 1-[(2-hydroxyethoxy)methyl]-6(phenylthio)thymine derivatives with the human immunodeficiency virus type 1 reverse transcriptase. Mol. Pharmacol 41: 963-969 (1992). [abstract] [pdf]
Debyser Z, Pauwels R, Andries K, De Clercq E. Specific HIV-1 reverse transcriptase inhibitors. J. Enzyme Inhibition, 6: 47-53 (1992). [no abstract] [no pdf]
de Vreese K, Debyser Z, Vandamme AM, Pauwels R, Desmyter J, De Clercq E, Anné J. Resistance of human immunodeficiency virus type 1 reverse transcriptase to TIBO derivatives induced by site-directed mutagenesis. Virology, 188: 900-904 (1992). [abstract] [no pdf]
Debyser Z, Pauwels R, Andries K, Desmyter J, Engelborghs Y, Janssen PAJ, De Clercq E. Allosteric inhibition of HIV-1 reverse transcriptase by tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione compounds. Mol. Pharmacol., 41: 203-208 (1992). [abstract] [pdf]
Schols D, Pauwels R, Witvrouw M, Desmyter J, De Clercq E. Differential activity of polyanionic compounds and castanospermine against HIV replication and HIV-induced syncytium formation depending on virus strain and cell type. Antiviral Chem. Chemother., 3 : 23-29 (1992). [abstract on Web of Science] [no pdf]
Witvrouw M, Pauwels R, Vandamme AM, Schols D, Reymen D, Yamamoto N, Desmyter J, De Clercq E. Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactivation inhibitor Ro5-3335. Antimicrob. Agents Chemother., 36 : 2628-2633 (1992). [abstract] [pdf]
Witvrouw M, Schols D, Andrei G, Snoeck R, Ikeda S, Pauwels R, Van Schepdael A, Arnout J, Claes P, Desmyter J, De Clercq E. New polyacetal polysulphate active against human immunodeficiency virus and other enveloped viruses. Antiviral Chem. Chemother 3 : 351-360 (1992). [abstract on Web of Science] [pdf]
1991
Debyser Z, Pauwels R, Andries K, Desmyter J, Kukla M, Janssen PAJ, De Clercq E. An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione derivatives. Proc. Natl. Acad. Sci. USA, 88: 1451-1455 (1991). [abstract] [pdf]
Peters M, Witvrouw M, De Clercq E, Ruf B. Pharmacokinetics of intravenous pentosan polysulphate (HOE/BAY 946) in HIV positive patients. AIDS 5: 1534-1535 (1991). [no abstract] [pdf]
Schols D, De Clercq E, Witvrouw M, Nakashima H, Snoeck R, Pauwels R, Van Schepdael A, Claes P. Sulphated cyclodextrins are potent anti-HIV agents acting synergistically with 2',3'-dideoxy-nucleoside analogues. Antiviral Chem. Chemother, 2 : 45-53 (1991). [no abstract] [pdf]
Witvrouw M, Schols D, Andrei G, Snoeck R, Hosoya M, Pauwels R, Balzarini J, De Clercq E. Antiviral activity of low-MW dextran sulphate (derived from dextran MW 1000) compared to dextran sulphate samples of higher MW. Antiviral Chem. Chemother., 2 : 171-179 (1991). [no abstract] [pdf]
1990
Schols D, De Clercq E, Balzarini J, Baba M, Witvrouw M, Hosoya M, Andrei G, Snoeck R, Neyts J, Pauwels R, Nagy M, Györgyi-Edelényi J, Machovich R, Horváth I, Löw M, Görög S. Sulphated polymers are potent and selective inhibitors of various enveloped viruses, including herpes simplex virus, cytomegalovirus, vesicular stomatitis virus, respiratory syncytial virus, and toga-, arena- and retroviruses. Antiviral Chem. Chemother., 1 : 233-240 (1990). [no abstract] [pdf]
Witvrouw M, Baba M, Balzarini J, Pauwels R, De Clercq E. Establishment of a bioassay to determine serum levels of dextran sulfate and pentosan polysulfate, two potent inhibitors of human immunodeficiency virus. J. Acquir. Immun. Defic. Syndr., 3 : 343-347 (1990). [abstract] [pdf]
1989
Pauwels R, Debyser Z, Balzarini J, Baba M, Desmyter J, Rayner B, Morvan F, Imbach Jl, Declercq E. Alpha-oligodeoxynucleotides as inhibitors of hiv reverse-transcriptase. Nucleosides & nucleotides 8(5-6): 995-1000. [abstract in lirias] [no pdf]
