J Balzarini

Summary

Affiliation: Katholieke Universiteit Leuven
Country: Belgium

Publications

  1. ncbi request reprint Specific recognition of the bicyclic pyrimidine nucleoside analogs, a new class of highly potent and selective inhibitors of varicella-zoster virus (VZV), by the VZV-encoded thymidine kinase
    Rebecca Sienaert
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 61:249-54. 2002
  2. ncbi request reprint The effect of a methyl or 2-fluoroethyl substituent at the N-3 position of thymidine, 3'-fluoro-3'-deoxythymidine and 1-beta-D-arabinosylthymine on their antiviral and cytostatic activity in cell culture
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Antivir Chem Chemother 17:17-23. 2006
  3. ncbi request reprint Targeting the glycans of glycoproteins: a novel paradigm for antiviral therapy
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Nat Rev Microbiol 5:583-97. 2007
  4. ncbi request reprint The rare HIV-1 gp41 mutations 43T and 50V elevate enfuvirtide resistance levels of common enfuvirtide resistance mutations that did not impact susceptibility to sifuvirtide
    Kris Covens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antiviral Res 86:253-60. 2010
  5. pmc Differences in the mannose oligomer specificities of the closely related lectins from Galanthus nivalis and Zea mays strongly determine their eventual anti-HIV activity
    Bart Hoorelbeke
    Rega Institute for Medical Research, K, U, Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Retrovirology 8:10. 2011
  6. pmc Role of the carbohydrate-binding sites of griffithsin in the prevention of DC-SIGN-mediated capture and transmission of HIV-1
    Bart Hoorelbeke
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    PLoS ONE 8:e64132. 2013
  7. doi request reprint 2-aminothiophene-3-carboxylic acid ester derivatives as novel highly selective cytostatic agents
    J Balzarini
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000, Leuven, Belgium
    Invest New Drugs 32:200-10. 2014
  8. pmc A multi-targeted drug candidate with dual anti-HIV and anti-HSV activity
    Jan Balzarini
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    PLoS Pathog 9:e1003456. 2013
  9. ncbi request reprint Role of cations in the interaction of pradimicins with HIV-1 envelope gp120
    Bart Hoorelbeke
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Top Med Chem 13:1907-15. 2013
  10. pmc A phenyl-thiadiazolylidene-amine derivative ejects zinc from retroviral nucleocapsid zinc fingers and inactivates HIV virions
    Thomas Vercruysse
    Rega Institute for Medical Research, Laboratory for Virology and Chemotherapy, KU Leuven, Minderbroedersstraat 10, Leuven, B 3000, Belgium
    Retrovirology 9:95. 2012

Collaborators

Detail Information

Publications169 found, 100 shown here

  1. ncbi request reprint Specific recognition of the bicyclic pyrimidine nucleoside analogs, a new class of highly potent and selective inhibitors of varicella-zoster virus (VZV), by the VZV-encoded thymidine kinase
    Rebecca Sienaert
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 61:249-54. 2002
    ..Our observations may account for the unprecedented specificity of BCNAs as anti-VZV agents...
  2. ncbi request reprint The effect of a methyl or 2-fluoroethyl substituent at the N-3 position of thymidine, 3'-fluoro-3'-deoxythymidine and 1-beta-D-arabinosylthymine on their antiviral and cytostatic activity in cell culture
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Antivir Chem Chemother 17:17-23. 2006
    ..The decreased biological activity of the N-3-substituted pyrimidine nucleoside analogues coincides with a significantly lower affinity of the modified Thd analogues for the cellular and viral (activating) nucleoside kinases...
  3. ncbi request reprint Targeting the glycans of glycoproteins: a novel paradigm for antiviral therapy
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Nat Rev Microbiol 5:583-97. 2007
    ..This approach may also be extended to other pathogens, including parasites, bacteria and fungi...
  4. ncbi request reprint The rare HIV-1 gp41 mutations 43T and 50V elevate enfuvirtide resistance levels of common enfuvirtide resistance mutations that did not impact susceptibility to sifuvirtide
    Kris Covens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antiviral Res 86:253-60. 2010
    ....
  5. pmc Differences in the mannose oligomer specificities of the closely related lectins from Galanthus nivalis and Zea mays strongly determine their eventual anti-HIV activity
    Bart Hoorelbeke
    Rega Institute for Medical Research, K, U, Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Retrovirology 8:10. 2011
    ..Both lectins are tetrameric proteins sharing 64% sequence similarity...
  6. pmc Role of the carbohydrate-binding sites of griffithsin in the prevention of DC-SIGN-mediated capture and transmission of HIV-1
    Bart Hoorelbeke
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    PLoS ONE 8:e64132. 2013
    ....
  7. doi request reprint 2-aminothiophene-3-carboxylic acid ester derivatives as novel highly selective cytostatic agents
    J Balzarini
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000, Leuven, Belgium
    Invest New Drugs 32:200-10. 2014
    ..Compound 3 was also shown to induce apoptosis in prostate cancer cells. The 2-aminothiophene-3-carboxylic acid ester derivatives represent novel candidate cytostatic agents to be further explored for their tumor-selective potential...
  8. pmc A multi-targeted drug candidate with dual anti-HIV and anti-HSV activity
    Jan Balzarini
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    PLoS Pathog 9:e1003456. 2013
    ..e. the viral polymerases) and HIV transmission prevention through interference with host pathways (i.e. CCR5 receptor down regulation)...
  9. ncbi request reprint Role of cations in the interaction of pradimicins with HIV-1 envelope gp120
    Bart Hoorelbeke
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Top Med Chem 13:1907-15. 2013
    ..Thus, in order to afford antiviral activity, only a few cations can (i) bind to pradimicin to form a dimeric complex and (ii) subsequently coordinate the pradimicin/cation interaction with gp120 glycans. ..
  10. pmc A phenyl-thiadiazolylidene-amine derivative ejects zinc from retroviral nucleocapsid zinc fingers and inactivates HIV virions
    Thomas Vercruysse
    Rega Institute for Medical Research, Laboratory for Virology and Chemotherapy, KU Leuven, Minderbroedersstraat 10, Leuven, B 3000, Belgium
    Retrovirology 9:95. 2012
    ..Therefore, virucidal agents that inactivate HIV virions may be used as a component in topical microbicides...
  11. pmc Introduction of a fluorine atom at C3 of 3-deazauridine shifts its antimetabolic activity from inhibition of CTP synthetase to inhibition of orotidylate decarboxylase, an early event in the de novo pyrimidine nucleotide biosynthesis pathway
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Biol Chem 287:30444-54. 2012
    ..The 3F-3DUrd monophosphate exhibits new inhibitory properties against a different enzyme of the pyrimidine nucleotide metabolism, namely the ODC activity of UMP synthase...
  12. ncbi request reprint Combination of antiretroviral drugs as microbicides
    Jan Balzarini
    Department of Microbiology and Immunology, Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Curr HIV Res 10:53-60. 2012
    ..e. anti-HIV/HSV) activity in different in vitro, ex vivo and animal models. They also deserve special attention for their potential to prevent HIV transmission and to concomitantly suppress co-pathogens of HIV such as herpes viruses...
  13. pmc Structure of vaccinia virus thymidine kinase in complex with dTTP: insights for drug design
    Kamel El Omari
    Division of Structural Biology, The Wellcome Trust Centre for Human Genetics, University of Oxford, Oxford OX3 7BN, UK
    BMC Struct Biol 6:22. 2006
    ..Vaccinia virus TK is a close orthologue of variola TK but also shares a relatively high sequence identity to human type 2 TK (hTK), thus achieving drug selectivity relative to the host enzyme is challenging...
  14. pmc Coexpression and interaction of CXCL10 and CD26 in mesenchymal cells by synergising inflammatory cytokines: CXCL8 and CXCL10 are discriminative markers for autoimmune arthropathies
    Paul Proost
    Laboratory of Molecular Immunology, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Arthritis Res Ther 8:R107. 2006
    ..Synovial concentrations of the neutrophil chemoattractant CXCL8 may therefore be useful to discriminate between autoimmune arthritis types...
  15. pmc Differential activity of candidate microbicides against early steps of HIV-1 infection upon complement virus opsonization
    Mohammad Ali Jenabian
    Université Paris Descartes Paris V, Laboratoire de Virologie, Hopital Europeen Georges Pompidou, Paris, France
    AIDS Res Ther 7:16. 2010
    ..HIV-1 in genital secretions may be opsonized by several molecules including complement components. Opsonized HIV-1 by complement enhances the infection of various mucosal target cells, such as dendritic cells (DC) and epithelial cells...
  16. doi request reprint Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activity
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 75:1127-36. 2009
    ....
  17. pmc Pradimicin S, a highly soluble nonpeptidic small-size carbohydrate-binding antibiotic, is an anti-HIV drug lead for both microbicidal and systemic use
    Jan Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antimicrob Agents Chemother 54:1425-35. 2010
    ..It proved stable at high temperature and low pH. Therefore, PRM-S may qualify as a potential anti-HIV drug candidate for further (pre)clinical studies, including its microbicidal use...
  18. ncbi request reprint Inhibition of HIV entry by carbohydrate-binding proteins
    J Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 71:237-47. 2006
    ....
  19. ncbi request reprint The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 68:49-60. 2005
    ....
  20. ncbi request reprint The alpha(1,2)-mannosidase I inhibitor 1-deoxymannojirimycin potentiates the antiviral activity of carbohydrate-binding agents against wild-type and mutant HIV-1 strains containing glycan deletions in gp120
    Jan Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    FEBS Lett 581:2060-4. 2007
    ..These observations argue for a combined exposure of CBAs and glycosylation inhibitors such as DMJ to HIV to afford a more pronounced suppression of virus replication, prior to, or during, CBA resistance development...
  21. ncbi request reprint Carbohydrate-binding agents: a potential future cornerstone for the chemotherapy of enveloped viruses?
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Antivir Chem Chemother 18:1-11. 2007
    ..In addition, influenza virus and coronavirus infections may also qualify to be treated by CBAs...
  22. ncbi request reprint Engineering of a single conserved amino acid residue of herpes simplex virus type 1 thymidine kinase allows a predominant shift from pyrimidine to purine nucleoside phosphorylation
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    J Biol Chem 281:19273-9. 2006
    ....
  23. pmc Mutational pathways, resistance profile, and side effects of cyanovirin relative to human immunodeficiency virus type 1 strains with N-glycan deletions in their gp120 envelopes
    Jan Balzarini
    Rega Institute for Medical Research, KU Leuven, Belgium
    J Virol 80:8411-21. 2006
    ....
  24. ncbi request reprint Carbohydrate-binding agents efficiently prevent dendritic cell-specific intercellular adhesion molecule-3-grabbing nonintegrin (DC-SIGN)-directed HIV-1 transmission to T lymphocytes
    Jan Balzarini
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Mol Pharmacol 71:3-11. 2007
    ....
  25. ncbi request reprint Inhibition of feline (FIPV) and human (SARS) coronavirus by semisynthetic derivatives of glycopeptide antibiotics
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 72:20-33. 2006
    ..Some compounds showed inhibitory activity against both, whereas other compounds proved inhibitory to either, FIPV or SARS-CoV. There was no close correlation between the EC(50) values of the glycopeptide derivatives for FIPV or SARS-CoV...
  26. ncbi request reprint Pronounced in vitro and in vivo antiretroviral activity of 5-substituted 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy] pyrimidines
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    J Antimicrob Chemother 59:80-6. 2007
    ..To discover new potent and selective anti-human immunodeficiency virus (HIV) acyclic nucleoside phosphonate (ANP) drugs with in vivo antiretroviral activity...
  27. ncbi request reprint Targeting the glycans of gp120: a novel approach aimed at the Achilles heel of HIV
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Lancet Infect Dis 5:726-31. 2005
    ..Moreover, this approach could be applied to treat other chronic infections by viruses that contain a glycosylated envelope (eg, hepatitis B and C)...
  28. ncbi request reprint Carbohydrate-binding agents cause deletions of highly conserved glycosylation sites in HIV GP120: a new therapeutic concept to hit the achilles heel of HIV
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    J Biol Chem 280:41005-14. 2005
    ..It forces HIV to escape drug pressure by deleting the indispensable glycans on its GP120, thereby obligatorily exposing previously hidden immunogenic epitopes on its envelope...
  29. ncbi request reprint Microbicide drug candidates to prevent HIV infection
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    Lancet 369:787-97. 2007
    ..We review different categories of microbicide drugs and lead compounds, their mechanism of action, current status of development, and progress in phase III trials...
  30. pmc Phosphonylmethoxyethyl purine derivatives, a new class of anti-human immunodeficiency virus agents
    R Pauwels
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 32:1025-30. 1988
    ..Unlike 2',3'-dideoxyadenosine, these compounds were not found to be degraded by deaminases derived from bovine intestine...
  31. ncbi request reprint 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
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    FEBS Lett 410:324-8. 1997
    ..Both Cf 1001 and Cf 1093 were equally efficient as 3TC (lamivudine) in inhibiting HBV replication in hepatocytes, and rank among the most potent HIV and HBV inhibitors reported so far in cell culture...
  32. ncbi request reprint 6-[2-phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines: a new class of acyclic pyrimidine nucleoside phosphonates with antiviral activity
    J Balzarini
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 23:1321-7. 2004
    ..The HPMPO-, PMEO- and PMPO-DAPym derivatives represent a novel well-defined subclass among the acyclic nucleoside phosphonates endowed with potent and selective antiviral activity...
  33. ncbi request reprint Retention of marked sensitivity to (S)-4-isopropoxycarbonyl-6-methoxy-3-(methylthiomethyl)-3,4-di hydroquin oxaline-2(1H)-thione (HBY 097) by an azidothymidine (AZT)-resistant human immunodeficiency virus type 1 (HIV-1) strain subcultured in the combined
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Biochem Pharmacol 55:617-25. 1998
    ..Given the exquisite potency of a concomitant combination of 3TC and HBY 097 in suppressing virus replication, this drug combination should be further pursued in clinical trials in HIV-1-infected individuals...
  34. ncbi request reprint Comparative cytostatic activity of different antiherpetic drugs against herpes simplex virus thymidine kinase gene-transfected tumor cells
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 45:1253-8. 1994
    ..e., resistance to hydrolysis by thymidine phosphorylase)...
  35. pmc Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine
    J Balzarini
    Rega Institute of Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 37:332-8. 1993
    ..In addition, upon oral administration to MSV-infected mice, (R)-PMPDAP showed marked antiretroviral efficacy...
  36. ncbi request reprint Intracellular metabolism of CycloSaligenyl 3'-azido-2', 3'-dideoxythymidine monophosphate, a prodrug of 3'-azido-2', 3'-dideoxythymidine (zidovudine)
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 56:1354-61. 1999
    ....
  37. ncbi request reprint Antiretrovirus specificity and intracellular metabolism of 2',3' -didehydro-2',3'-dideoxythymidine (stavudine) and its 5'-monophosphate triester prodrug So324
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 50:1207-13. 1996
    ..Alanyl d4T-MP may be considered to be an intracellular depot form of d4T and/or d4T-MP, which may account for the superior antiretroviral activity of the lipophilic d4T-MP triester So324 compared with d4T...
  38. pmc 9-[(2RS)-3-fluoro-2-phosphonylmethoxypropyl] derivatives of purines: a class of highly selective antiretroviral agents in vitro and in vivo
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Proc Natl Acad Sci U S A 88:4961-5. 1991
    ..The DNA chain-terminating properties of PMEApp and (RS)-FPMPApp seem to be a prerequisite for acyclic nucleoside phosphonates to exhibit antiretrovirus (i.e., anti-HIV) activity...
  39. pmc Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives)
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Proc Natl Acad Sci U S A 92:5470-4. 1995
    ....
  40. ncbi request reprint 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 replication
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 50:394-401. 1996
    ....
  41. pmc SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 41:262-8. 1997
    ..Time-of-addition experiments indicated that SRR-SB3 acts at a late stage of the HIV-1 replicative cycle...
  42. ncbi request reprint Antiviral potential of a new generation of acyclic nucleoside phosphonates, the 6-[2-(phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines
    Erik De Clercq
    Address correspondence to Erik De Clercq, Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, Leuven B 3000, Belgium
    Nucleosides Nucleotides Nucleic Acids 24:331-41. 2005
    ..The 6-[2-(phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines offer substantial potential for the treatment of a broad range of retro-, hepadna-, herpes-, adeno-, and poxvirus infections...
  43. ncbi request reprint Intracellular metabolism of the N7-substituted acyclic nucleoside analog 2-amino-7-(1,3-dihydroxy-2-propoxymethyl)purine, a potent inhibitor of herpesvirus replication
    J Neyts
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 53:157-65. 1998
    ..S2242 was found to be a substrate (K(m) = 90 microM) for purified human deoxyguanosine kinase; the latter enzyme was stimulated 3-4-fold in HCMV-infected cells...
  44. ncbi request reprint Antiviral activity of cyclosaligenyl prodrugs of acyclovir, carbovir and abacavir
    J Balzarini
    Rega Institute for Medical Research, KU Leuven, Belgium
    Antivir Chem Chemother 12:301-6. 2001
    ....
  45. pmc Marked in vivo antiretrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine, a selective anti-human immunodeficiency virus agent
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Proc Natl Acad Sci U S A 86:332-6. 1989
    ....
  46. ncbi request reprint Investigations on the anti-HIV activity of 2',3'-dideoxyadenosine analogues with modifications in either the pentose or purine moiety. Potent and selective anti-HIV activity of 2,6-diaminopurine 2',3'-dideoxyriboside
    R Pauwels
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Biochem Pharmacol 37:1317-25. 1988
    ..e. several pyrrolo[2,3-d]pyrimidine 2',3'-dideoxynucleosides, were investigated for their anti-HIV activity, but none of these derivatives proved as potent or selective as ddDAPR...
  47. ncbi request reprint Potentiating effect of ribavirin on the in vitro and in vivo antiretrovirus activities of 2',3'-dideoxyinosine and 2',3'-dideoxy-2,6-diaminopurine riboside
    J Balzarini
    Rega Institute for Medical Research, Catholic University of Leuven, Belgium
    J Acquir Immune Defic Syndr 3:1140-7. 1990
    ..These observations point to the potential role of ribavirin in potentiating the anti-HIV activity of DDI in AIDS patients...
  48. ncbi request reprint Potentiating effect of ribavirin on the anti-retrovirus activity of 3'-azido-2,6-diaminopurine-2',3'-dideoxyriboside in vitro and in vivo
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antiviral Res 11:161-71. 1989
    ..A slight increase in the in vivo toxicity of AzddDAPR was noted when combined with ribavirin...
  49. ncbi request reprint Selection and characterisation of murine leukaemia L1210 cells with high-level resistance to the cytostatic activity of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl) adenine (PMEA)
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Biochim Biophys Acta 1402:29-38. 1998
    ..Our observations point to a compromised and highly specific PMEA/PMEDAP uptake as the molecular basis for the pronounced PMEA resistance of the mutant L1210/PMEA-1 cells...
  50. ncbi request reprint Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138
    H Pelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, B-3000, Belgium
    Virology 280:97-106. 2001
    ....
  51. ncbi request reprint The in vitro and in vivo anti-retrovirus activity, and intracellular metabolism of 3'-azido-2',3'-dideoxythymidine and 2',3'-dideoxycytidine are highly dependent on the cell species
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Biochem Pharmacol 37:897-903. 1988
    ..Thus, much higher ddCTP than AzddTTP levels were achieved in human lymphoid cells, an observation that may be particularly relevant from a therapeutic viewpoint...
  52. ncbi request reprint Potent and selective activity of 3'-azido-2,6-diaminopurine-2',3'-dideoxyriboside, 3'-fluoro-2,6-diaminopurine-2',3'-dideoxyriboside, and 3'-fluoro-2',3'-dideoxyguanosine against human immunodeficiency virus
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 33:243-9. 1988
    ..This suggests that ddDAPR and FddDAPR are primarily active as their guanine analogues, whereas AzddDAPR may be potentially active as a 2,6-diaminopurine derivative as well...
  53. ncbi request reprint Kinetic analysis of novel multisubstrate analogue inhibitors of thymidine phosphorylase
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    FEBS Lett 483:181-5. 2000
    ..To our knowledge, the described compounds represent the first type of such multisubstrate analogue inhibitors of TPase; they should be considered as lead compounds for the development of mechanistically novel type of TPase inhibitors...
  54. ncbi request reprint Anti-retrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in vivo increases when it is less frequently administered
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Int J Cancer 46:337-40. 1990
    ..This unique property makes PMEA an attractive candidate for the treatment of retrovirus infections, including AIDS...
  55. ncbi request reprint Differential patterns of intracellular metabolism of 2',3'-didehydro-2',3'-dideoxythymidine and 3'-azido-2',3'-dideoxythymidine, two potent anti-human immunodeficiency virus compounds
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    J Biol Chem 264:6127-33. 1989
    ..The 5'-triphosphates of AZT and D4T are equipotent in their inhibitory effects on the reverse transcriptases from human immunodeficiency virus and Moloney murine leukemia virus...
  56. ncbi request reprint Inactivity of the bicyclic pyrimidine nucleoside analogues against simian varicella virus (SVV) does not correlate with their substrate activity for SVV-encoded thymidine kinase
    R Sienaert
    Rega Institute for Medical Research, Katholieke, Universiteit Leuven, B 3000 Leuven, Belgium
    Biochem Biophys Res Commun 315:877-83. 2004
    ..Our data suggest that the eventual target of the BCNAs against VZV is either absent in SVV or, alternatively, is insensitive for the (phosphorylated) BCNAs...
  57. ncbi request reprint Mutation of Gln125 to Asn selectively abolishes the thymidylate kinase activity of herpes simplex virus type 1 thymidine kinase
    B Degreve
    Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium
    Mol Pharmacol 59:285-93. 2001
    ..e., 1-beta-D-arabinofuranosylthymine and (E)-5-(2-bromovinyl)-1-beta-D-arabinofuranosyluracil]...
  58. pmc Profile of resistance of human immunodeficiency virus to mannose-specific plant lectins
    Jan Balzarini
    Rega Institute for Medical Research, Gent, Belgium
    J Virol 78:10617-27. 2004
    ..The plant lectins represent a well-defined class of anti-HIV (microbicidal) drugs with a novel HIV drug resistance profile different from those of other existing anti-HIV drugs...
  59. ncbi request reprint Prognostic value of positron emission tomography (PET) with fluorine-18 fluorodeoxyglucose ([18F]FDG) after first-line chemotherapy in non-Hodgkin's lymphoma: is [18F]FDG-PET a valid alternative to conventional diagnostic methods?
    K Spaepen
    Department of Nuclear Medicine, University Hospital Gasthuisberg and Catholic University of Leuven, Leuven, Belgium
    J Clin Oncol 19:414-9. 2001
    ..In this study, we evaluated the value of PET in detecting residual disease and, hence, predicting relapse after first-line treatment in patients with non-Hodgkin's lymphoma (NHL)...
  60. ncbi request reprint Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    AIDS Res Hum Retroviruses 16:517-28. 2000
    ..Our data suggest that combinations of GW420867X with 3TC, ABC, and NNRTIs (e.g., efavirenz) would be worth pursuing as therapeutic modalities against HIV-1 infections...
  61. pmc Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine
    L Naesens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium lieve naesens rega kuleuven ac be
    Antimicrob Agents Chemother 40:22-8. 1996
    ..Bis(POM)-PMEA appears to be an efficient oral prodrug of PMEA that deserves further clinical evaluation in human immunodeficiency virus-infected individuals...
  62. ncbi request reprint 9-(2-Phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP): a novel agent with anti-human immunodeficiency virus activity in vitro and potent anti-Moloney murine sarcoma virus activity in vivo
    L Naesens
    Rega Institute for Medical Research, Katholieke Universiteit, Leuven, Belgium
    Eur J Clin Microbiol Infect Dis 8:1043-7. 1989
    ..However, PMEDAP was also more toxic, so that its therapeutic index was equivalent to that of PMEA...
  63. pmc Exploitation of the low fidelity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase and the nucleotide composition bias in the HIV-1 genome to alter the drug resistance development of HIV
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroederstraat 10, B 3000 Leuven, Belgium
    J Virol 75:5772-7. 2001
    ..Forcing the virus to change its inherent nucleotide bias may lead to better control of viral drug resistance development...
  64. pmc 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 NM
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 41:611-6. 1997
    ..Treatment of the NMRI mice with PMEA, (R)-PMPA, and MDL 74,968 at 25 or 50 mg/kg resulted in a high percentage of long-term survivors...
  65. ncbi request reprint Can positron emission tomography with [(18)F]-fluorodeoxyglucose after first-line treatment distinguish Hodgkin's disease patients who need additional therapy from others in whom additional therapy would mean avoidable toxicity?
    K Spaepen
    Department of Nuclear Medicine, University Hospital Gasthuisberg and Catholic University of Leuven, Leuven, Belgium
    Br J Haematol 115:272-8. 2001
    ..Two-year actuarial PFS rate for negative patients was 91% compared with 0% for positive patients. We concluded that [(18)F]-FDG-PET has an important prognostic role in the post-treatment evaluation of HD patients...
  66. ncbi request reprint Efficacy of oral 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the treatment of retrovirus and cytomegalovirus infections in mice
    L Naesens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    J Med Virol 39:167-72. 1993
    ..Oral PMEDAP at doses of 100, 250, or 500 mg/kg resulted in plasma PMEDAP levels of 0.5-2.5 micrograms/ml, which were sustained for 3 or 6 hours after administration and may account for the high antiviral efficacy achieved...
  67. pmc Activity and mechanism of action of HDVD, a novel pyrimidine nucleoside derivative with high levels of selectivity and potency against gammaherpesviruses
    N Coen
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    J Virol 87:3839-51. 2013
    ..In the present study, HDVD emerged as a highly potent antiviral with a unique spectrum of activity against herpesviruses, in particular, gammaherpesviruses, and may be of interest in the treatment of virus-associated diseases...
  68. ncbi request reprint A novel mutation (F227L) arises in the reverse transcriptase of human immunodeficiency virus type 1 on dose-escalating treatment of HIV type 1-infected cell cultures with the nonnucleoside reverse transcriptase inhibitor thiocarboxanilide UC-781
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    AIDS Res Hum Retroviruses 14:255-60. 1998
    ..The F227 amino acid is highly conserved in HIV-1 strains and forms part of the NNRTI-binding pocket. Our model suggests a hydrophobic interaction between F227 and the chloro atom of UC-781...
  69. ncbi request reprint Mutations in the non-nucleoside binding-pocket interfere with the multi-nucleoside resistance phenotype
    K Van Laethem
    Rega Institute for Medical Research and University Hospitals, Katholieke Universiteit Leuven, Belgium
    AIDS 15:553-61. 2001
    ..CONCLUSION: Changes in the non-nucleoside binding pocket must affect the conformation of residues at the dNTP binding site, and can result in a partial phenotypic reversal of the multi-nucleoside resistance phenotype...
  70. ncbi request reprint Cyclosaligenyl-2',3'-didehydro-2',3'-dideoxythymidine monophosphate: efficient intracellular delivery of d4TMP
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 58:928-35. 2000
    ..d4TMP is a poor substrate for the cytosolic 5'(3')-deoxyribonucleotidase (V(max)/K(m) for d4TMP: 0.08 of V(max)/K(m) for dTMP) and is only slowly hydrolyzed to d4T. This contributes to the efficient conversion of the prodrug of d4TTP...
  71. pmc Novel ribofuranosylnucleoside lead compounds for potent and selective inhibitors of mitochondrial thymidine kinase-2
    J Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem J 351:167-71. 2000
    ..It was concluded that the ribonucleosides 5-BV-Urd and 3'-AOD-5-MeUrd represent two new lead compounds for potent and selective inhibitors of mitochondrial TK-2...
  72. pmc Alpha-(1-3)- and alpha-(1-6)-D-mannose-specific plant lectins are markedly inhibitory to human immunodeficiency virus and cytomegalovirus infections in vitro
    J Balzarini
    Laboratory of Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 35:410-6. 1991
    ..Our data suggest that alpha-(1-3)-D- and alpha-(1-6)-D-mannose-specific plant lectins interfere with an event in the HIV replicative cycle that is subsequent to the attachment of the virions to the cells (i.e., the fusion process)...
  73. ncbi request reprint Models which explain the inhibition of reverse transcriptase by HIV-1-specific (thio)carboxanilide derivatives
    R M Esnouf
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Biochem Biophys Res Commun 234:458-64. 1997
    ..They further predict that mutations to Phe227, Trp229, or Leu234 might confer resistance. Since these are not observed, some constraining structural or functional role for these residues in the active enzyme is suggested...
  74. doi request reprint Identification of aspartic acid-203 in human thymidine phosphorylase as an important residue for both catalysis and non-competitive inhibition by the small molecule "crystallization chaperone" 5'-O-tritylinosine (KIN59)
    A Bronckaers
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 78:231-40. 2009
    ..Our findings reveal the existence of a previously unrecognized site in TP that can be targeted by small molecules to inhibit the catalytic activity of TP...
  75. pmc 1,1,3-Trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine (TTD) derivatives: a new class of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors with anti-HIV-1 activity
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 42:618-23. 1998
    ..Modelling studies suggest that in contrast to most other NNRTIs, but akin to nevirapine, QM96521 does not act as a hydrogen bond donor in the RT-drug complex...
  76. ncbi request reprint Activity of various thiocarboxanilide derivatives against wild-type and several mutant human immunodeficiency virus type 1 strains
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antiviral Res 27:219-36. 1995
    ..One of the most potent HIV-1 inhibitors among the thiocarboxanilide derivatives, namely UC38, selected for a mutant virus strain in which Lys at position 101 and Gly at position 190 of the reverse transcriptase was replaced by Glu...
  77. ncbi request reprint Single-dose administration of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the prophylaxis of retrovirus infection in vivo
    L Naesens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antiviral Res 16:53-64. 1991
    ..Thus, single doses of PMEA or PMEDAP, when administered shortly before or after MSV infection, appear to be effective in preventing the manifestations of the retroviral disease...
  78. ncbi request reprint Characterization of the catalytic subunit of the human herpesvirus 6 (HHV-6) DNA polymerase expressed in an in vitro transcription/translation assay
    L De Bolle
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 22:999-1001. 2003
  79. ncbi request reprint Inhibitory effects of 9-(2-phosphonylmethoxyethyl)adenine and 3'-azido-2',3'-dideoxythymidine on tumor development in mice inoculated intracerebrally with Moloney murine sarcoma virus
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Int J Cancer 45:486-9. 1990
    ....
  80. pmc Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus
    Jan Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 81:362-73. 2007
    ....
  81. ncbi request reprint Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Med Chem 46:2755-64. 2003
    ..The mode of anti-HIV action of the antibiotic aglycon derivatives could be ascribed to inhibition of the viral entry process...
  82. pmc Actinohivin, a broadly neutralizing prokaryotic lectin, inhibits HIV-1 infection by specifically targeting high-mannose-type glycans on the gp120 envelope
    Bart Hoorelbeke
    Rega Institute for Medical Research, Minderbroedersstraat 10, Leuven B 3000, Belgium
    Antimicrob Agents Chemother 54:3287-301. 2010
    ....
  83. ncbi request reprint The A167Y mutation converts the herpes simplex virus type 1 thymidine kinase into a guanosine analogue kinase
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochemistry 41:6517-24. 2002
    ..Therefore, the single A167Y mutation converts the wild-type HSV-1 TK from a predominantly pyrimidine nucleos(t)ide kinase into a virtually exclusive purine (guanine) nucleoside analogue kinase...
  84. ncbi request reprint The nucleoside derivative 5'-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action
    Sandra Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Biol Chem 279:29598-605. 2004
    ..Identification of these site(s) is important to obtain a better insight into the molecular role of TPase in the progression of cancer and angiogenic diseases...
  85. doi request reprint Simian immunodeficiency virus is susceptible to inhibition by carbohydrate-binding agents in a manner similar to that of HIV: implications for further preclinical drug development
    Katrien O François
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Mol Pharmacol 74:330-7. 2008
    ..Therefore, SIV(mac251)-infected monkeys might represent a relevant animal model to study the efficacy of CBAs in vivo...
  86. pmc Microvirin, a novel alpha(1,2)-mannose-specific lectin isolated from Microcystis aeruginosa, has anti-HIV-1 activity comparable with that of cyanovirin-N but a much higher safety profile
    Dana Huskens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Biol Chem 285:24845-54. 2010
    ..Therefore, MVN may qualify as a useful lectin for potential microbicidal use based on its broad and potent antiviral activity and virtual lack of any stimulatory properties and cellular toxicity...
  87. ncbi request reprint The N137 and P140 amino acids in the p51 and the P95 amino acid in the p66 subunit of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase are instrumental to maintain catalytic activity and to design new classes of anti-HIV-1 drugs
    Joeri Auwerx
    Rega Institute for Medical Research, K U Leuven, Belgium
    FEBS Lett 579:2294-300. 2005
    ....
  88. pmc Sugar-binding proteins potently inhibit dendritic cell human immunodeficiency virus type 1 (HIV-1) infection and dendritic-cell-directed HIV-1 transfer
    Stuart G Turville
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 79:13519-27. 2005
    ..Thus, our findings indicate that I-SPT may be more elusive to targeting by antiviral drugs and stress the need for drugs affecting the pronounced inhibition of the infection of DCs by HIV-1...
  89. ncbi request reprint N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action
    Irene M Lagoja
    Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, Belgium
    J Med Chem 46:1546-53. 2003
    ....
  90. doi request reprint Antiviral activity of carbohydrate-binding agents and the role of DC-SIGN in dengue virus infection
    Marijke M F Alen
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Virology 387:67-75. 2009
    ..However, the CBAs were devoid of antiviral activity in DENV-susceptible Vero-B (DC-SIGN(-)) cells, demonstrating cell type-dependent differences in viral entry mechanisms...
  91. ncbi request reprint Bicyclic pyrimidine nucleoside analogues (BCNAs) as highly selective and potent inhibitors of varicella-zoster virus replication
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    J Antimicrob Chemother 50:5-9. 2002
    ..Given the above-mentioned favourable properties, BCNAs may represent a promising novel class of highly selective anti-VZV drugs that should be further pursued for clinical application...
  92. ncbi request reprint Capture and transmission of HIV-1 by the C-type lectin L-SIGN (DC-SIGNR) is inhibited by carbohydrate-binding agents and polyanions
    Joeri Auwerx
    Virology and Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antiviral Res 83:61-70. 2009
    ..The excess value of CBAs and polyanions to prevent HIV-1 capture and transmission by DC-SIGN and L-SIGN-expressing cells to susceptible T-lymphocytes could be of interest for the development of new drug leads targeting HIV entry/fusion...
  93. doi request reprint Glycan deletions in the HIV-1 gp120 V1/V2 domain compromise viral infectivity, sensitize the mutant virus strains to carbohydrate-binding agents and represent a specific target for therapeutic intervention
    Joeri Auwerx
    Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Virology 382:10-9. 2008
    ..The gp120 V1/V2 loop glycans of HIV-1 should therefore be considered as a hot spot and novel target for specific therapeutic drug intervention...
  94. pmc Novel human immunodeficiency virus (HIV) inhibitors that have a dual mode of anti-HIV action
    Miguel Stevens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Antimicrob Agents Chemother 47:3109-16. 2003
    ....
  95. ncbi request reprint Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors
    Joeri Auwerx
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 65:244-51. 2004
    ....
  96. ncbi request reprint Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Eur J Med Chem 42:993-1003. 2007
    ..Furthermore, it was found that the (+)-22 isomer was predominantly responsible for the potent anti-HIV-1 activity (EC(50) value of 0.178 microM), while the levo isomer was more than 60-fold less active...
  97. pmc The phenylmethylthiazolylthiourea nonnucleoside reverse transcriptase (RT) inhibitor MSK-076 selects for a resistance mutation in the active site of human immunodeficiency virus type 2 RT
    Joeri Auwerx
    Rega Institute for Medical Research, B 3000 Leuven, Belgium
    J Virol 78:7427-37. 2004
    ..Our findings have important implications for the development of new NNRTIs with pronounced activity against a wider range of lentiviruses...
  98. pmc Mannose-specific plant lectins from the Amaryllidaceae family qualify as efficient microbicides for prevention of human immunodeficiency virus infection
    Jan Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antimicrob Agents Chemother 48:3858-70. 2004
    ..0) for prolonged time periods and can be easily formulated in gel preparations for microbicidal use; they did not agglutinate human erythrocytes and were not toxic to mice when administered intravenously...
  99. pmc The phthalocyanine prototype derivative Alcian Blue is the first synthetic agent with selective anti-human immunodeficiency virus activity due to its gp120 glycan-binding potential
    Katrien O François
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antimicrob Agents Chemother 53:4852-9. 2009
    ....
  100. ncbi request reprint Obligatory involvement of CD26/dipeptidyl peptidase IV in the activation of the antiretroviral tripeptide glycylprolylglycinamide (GPG-NH(2))
    Jan Balzarini
    Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Int J Biochem Cell Biol 36:1848-59. 2004
    ..e. CD26) that plays a direct regulatory and indispensable role in the eventual antiretroviral activity of small synthetic molecules such as the antiretroviral (pro)drug GPG-NH2...
  101. ncbi request reprint Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compounds
    S Liekens
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 25:975-80. 2006
    ..Our observations indicate that allosteric sites in TPase may regulate its biological activity...