J Balzarini

Summary

Affiliation: Katholieke Universiteit Leuven
Country: Belgium

Publications

  1. pmc Isolation and characterization of a small antiretroviral molecule affecting HIV-1 capsid morphology
    Samir Abdurahman
    Division of Clinical Microbiology, Karolinska Institutet, F68 Karolinska University Hospital Huddinge, SE 141 86 Stockholm, Sweden
    Retrovirology 6:34. 2009
  2. pmc Differential in vitro inhibitory activity against HIV-1 of alpha-(1-3)- and alpha-(1-6)-D-mannose specific plant lectins: implication for microbicide development
    Hela Saidi
    Unité INSERM U743, Equipe Immunité et Biothérapie Muqueuse, Centre de Recherches Biomedicales des Cordeliers, Paris, France
    J Transl Med 5:28. 2007
  3. ncbi request reprint Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    J Antimicrob Chemother 57:472-81. 2006
  4. 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
  5. ncbi request reprint Rapid alternation of drug therapy is highly efficient in suppressing the emergence of mutant drug-resistant HIV strains in cell culture
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    AIDS Res Hum Retroviruses 17:1625-34. 2001
  6. 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
  7. ncbi request reprint 2'-O-Acyl/alkyl-substituted arabinosyl nucleosides as inhibitors of human mitochondrial thymidine kinase
    J Balzarinia
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000, Leuven, Belgium
    Biochem Pharmacol 61:727-32. 2001
  8. ncbi request reprint Lack of susceptibility of bicyclic nucleoside analogs, highly potent inhibitors of varicella-zoster virus, to the catabolic action of thymidine phosphorylase and dihydropyrimidine dehydrogenase
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 61:1140-5. 2002
  9. 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
  10. 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

Detail Information

Publications129 found, 100 shown here

  1. pmc Isolation and characterization of a small antiretroviral molecule affecting HIV-1 capsid morphology
    Samir Abdurahman
    Division of Clinical Microbiology, Karolinska Institutet, F68 Karolinska University Hospital Huddinge, SE 141 86 Stockholm, Sweden
    Retrovirology 6:34. 2009
    ..We have previously described that glycineamide (G-NH2) when added to the culture medium of infected cells induces non-infectious HIV-1 particles with aberrant core structures...
  2. pmc Differential in vitro inhibitory activity against HIV-1 of alpha-(1-3)- and alpha-(1-6)-D-mannose specific plant lectins: implication for microbicide development
    Hela Saidi
    Unité INSERM U743, Equipe Immunité et Biothérapie Muqueuse, Centre de Recherches Biomedicales des Cordeliers, Paris, France
    J Transl Med 5:28. 2007
    ..Plant lectins are candidate for microbicide development...
  3. ncbi request reprint Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    J Antimicrob Chemother 57:472-81. 2006
    ..Evaluation of a wide variety of pyridine N-oxide derivatives on their inhibitory activity against feline coronavirus (FIPV strain) and human SARS-CoV (Frankfurt strain-1) in cell culture...
  4. 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
    ....
  5. ncbi request reprint Rapid alternation of drug therapy is highly efficient in suppressing the emergence of mutant drug-resistant HIV strains in cell culture
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    AIDS Res Hum Retroviruses 17:1625-34. 2001
    ....
  6. 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...
  7. ncbi request reprint 2'-O-Acyl/alkyl-substituted arabinosyl nucleosides as inhibitors of human mitochondrial thymidine kinase
    J Balzarinia
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000, Leuven, Belgium
    Biochem Pharmacol 61:727-32. 2001
    ..This is the first report on such a highly selective arabinosyl nucleoside inhibitor of mitochondrial TK-2, and opens perspectives for the rational design of selective mitochondrial TK-2 inhibitors...
  8. ncbi request reprint Lack of susceptibility of bicyclic nucleoside analogs, highly potent inhibitors of varicella-zoster virus, to the catabolic action of thymidine phosphorylase and dihydropyrimidine dehydrogenase
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 61:1140-5. 2002
    ....
  9. 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...
  10. 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...
  11. 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...
  12. 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
    ....
  13. ncbi request reprint Suppression of resistance to drugs targeted to human immunodeficiency virus reverse transcriptase by combination therapy
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Biochem Pharmacol 58:1-27. 1999
    ....
  14. 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...
  15. pmc Antiretrovirus activity of a novel class of acyclic pyrimidine nucleoside phosphonates
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Antimicrob Agents Chemother 46:2185-93. 2002
    ..e., DNA, RNA, or protein) synthesis. Compounds 1 and 11 should be considered attractive novel pyrimidine nucleotide phosphonate analogues to be further pursued for their potential as antiretroviral agents in the clinical setting...
  16. ncbi request reprint Marked depletion of glycosylation sites in HIV-1 gp120 under selection pressure by the mannose-specific plant lectins of Hippeastrum hybrid and Galanthus nivalis
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 67:1556-65. 2005
    ..The mutant viruses containing the deleted glycosylation sites were markedly more infectious in CEM T-cell cultures than wild-type virus...
  17. ncbi request reprint Pyridine N-oxide derivatives: unusual anti-HIV compounds with multiple mechanisms of antiviral action
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    J Antimicrob Chemother 55:135-8. 2005
    ..Repeated administration of one of the prototype compounds (JPL-32) to DBA/2 and hu-PBMC-SCID mice demonstrated, in the absence of any acute toxicity, protective activity against HIV-induced destruction of CD4 human T lymphocytes...
  18. 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...
  19. 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...
  20. 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...
  21. ncbi request reprint Current status of the non-nucleoside reverse transcriptase inhibitors of human immunodeficiency virus type 1
    J Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Top Med Chem 4:921-44. 2004
    ..NNRTIs have proven beneficial when included in drug combination (triple or quadruple) therapy, preferably in the presence of protease inhibitors and NRTIs...
  22. 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
    ....
  23. ncbi request reprint Non-nucleoside inhibitors of mitochondrial thymidine kinase (TK-2) differentially inhibit the closely related herpes simplex virus type 1 TK and Drosophila melanogaster multifunctional deoxynucleoside kinase
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 63:263-70. 2003
    ..KIN-12, and particularly KIN-52, are the very first non-nucleoside specific inhibitors of TK-2 reported and may be useful for studying the physiological role of the mitochondrial TK-2 enzyme...
  24. ncbi request reprint Metabolic activation of nucleoside and nucleotide reverse transcriptase inhibitors in dendritic and Langerhans cells
    Jan Balzarini
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, B 3000 Leuven, Belgium
    AIDS 16:2159-63. 2002
    ..Metabolism of nucleoside analogues markedly differs in proliferating T lymphocytes and resting monocyte/macrophages, and thus their antiviral efficacy can substantially differ between both cell types...
  25. 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...
  26. ncbi request reprint Chemotherapy of varicella-zoster virus by a novel class of highly specific anti-VZV bicyclic pyrimidine nucleosides
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, Leuven, Belgium
    Biochim Biophys Acta 1587:287-95. 2002
    ..The bicyclic pyrimidine nucleoside analogues represent an entirely new class of highly specific anti-VZV compounds that should be further pursued for clinical development...
  27. 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...
  28. 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...
  29. 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
    ....
  30. 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...
  31. 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...
  32. 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
    ....
  33. 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...
  34. 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...
  35. 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...
  36. 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)...
  37. 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
    ....
  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 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...
  40. 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...
  41. 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...
  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. 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...
  44. 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...
  45. 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...
  46. 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...
  47. 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
    ....
  48. 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...
  49. pmc Concomitant combination therapy for HIV infection preferable over sequential therapy with 3TC and non-nucleoside reverse transcriptase inhibitors
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Proc Natl Acad Sci U S A 93:13152-7. 1996
    ..In contrast with the sequential chemotherapy, concomitant combination treatment of HIV-1-infected cells with 3TC and a variety of NNRTIs resulted in a dramatic delay of virus breakthrough and resistance development...
  50. 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...
  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 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...
  53. 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...
  54. 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...
  55. 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...
  56. 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]...
  57. 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...
  58. 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...
  59. 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)...
  60. 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...
  61. 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...
  62. 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...
  63. ncbi request reprint Metabolic and pharmacological characteristics of the bicyclic nucleoside analogues (BCNAs) as highly selective inhibitors of varicella-zoster virus (VZV)
    R Sienaert
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 22:995-7. 2003
  64. 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...
  65. 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...
  66. 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...
  67. 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...
  68. 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
    ....
  69. 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...
  70. 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...
  71. 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...
  72. doi 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
    ....
  73. 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
    ....
  74. 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
    ....
  75. 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...
  76. ncbi request reprint Synthesis and antiviral activity of some 5'-N-phthaloyl-3'-azido-2',3'-dideoxythymidine analogues
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antivir Chem Chemother 14:139-44. 2003
    ..They did not inhibit recombinant HIV-1 reverse transcriptase. All compounds were inactive against HIV in thymidine kinase-deficient cells, pointing to the compounds' requirement to release free AZT to afford antiviral efficacy...
  77. 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
    ....
  78. ncbi request reprint Plant lectins are potent inhibitors of coronaviruses by interfering with two targets in the viral replication cycle
    Els Keyaerts
    Laboratory of Clinical and Epidemiological Virology, Department of Microbiology and Immunology, Rega Institute for Medical Research, University of Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium
    Antiviral Res 75:179-87. 2007
    ..The first target is located early in the replication cycle, most probably viral attachment, and the second target is located at the end of the infectious virus cycle...
  79. 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...
  80. 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...
  81. ncbi request reprint Pronounced cytostatic activity and bystander effect of a novel series of fluorescent tricyclic acyclovir and ganciclovir derivatives in herpes simplex virus thymidine kinase gene-transduced tumor cell lines
    J Balzarini
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Gene Ther 9:1173-82. 2002
    ..Also, the lipophilicity of the tricyclic purine derivatives is much higher than that of ACV and GCV, and this may allow better uptake of these derivatives from the blood into the central nervous system...
  82. 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
    ....
  83. pmc Identification of novel thiocarboxanilide derivatives that suppress a variety of drug-resistant mutant human immunodeficiency virus type 1 strains at a potency similar to that for wild-type virus
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 40:1454-66. 1996
    ..UC-781 and UC-82 should be considered potential candidate drugs for the treatment of HIV-1-infected individuals...
  84. 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...
  85. 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
    ....
  86. ncbi request reprint 5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis
    Sandra Liekens
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Mol Pharmacol 70:501-9. 2006
    ..Thus, 5'-O-trityl nucleoside derivatives combine antiangiogenic and vascular-targeting activities, which opens perspectives for their potential use as anticancer agents...
  87. 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...
  88. 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
    ....
  89. 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
    ....
  90. pmc Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives
    Miguel Stevens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Antimicrob Agents Chemother 47:2951-7. 2003
    ....
  91. 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...
  92. 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
    ....
  93. ncbi request reprint Anti-angiogenic activity of a novel multi-substrate analogue inhibitor of thymidine phosphorylase
    Sandra Liekens
    Rega Institute for Medical Research, Minderbroedersstraat 10, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    FEBS Lett 510:83-8. 2002
    ....
  94. ncbi request reprint Chimeric human immunodeficiency virus type 1 and feline immunodeficiency virus reverse transcriptases: role of the subunits in resistance/sensitivity to non-nucleoside reverse transcriptase inhibitors
    Joeri Auwerx
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 61:400-6. 2002
    ..This decreased catalytic efficacy of the RT chimeras may suggest suboptimal interactions between p66 and p51 in the chimeric enzymes. Our results point to a minor role of the p51 subunit in the sensitivity to RT inhibitors...
  95. ncbi request reprint Early restaging positron emission tomography with ( 18)F-fluorodeoxyglucose predicts outcome in patients with aggressive non-Hodgkin's lymphoma
    K Spaepen
    Departments of Nuclear Medicine, University Hospital Gasthuisberg and Catholic University of Leuven, Leuven, Belgium
    Ann Oncol 13:1356-63. 2002
    ..This study was intended to assess the value of a midtreatment fluorine-18 fluorodeoxyglucose positron emission tomography ([(18)F]FDG-PET) scan to predict clinical outcome in patients with aggressive NHL...
  96. ncbi request reprint Mutations at amino acid positions 63, 189, and 396 of human immunodeficiency virus type 1 reverse transcriptase (RT) partially restore the DNA polymerase activity of a Trp229Tyr mutant RT
    H Pelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, B-3000, Belgium
    Virology 287:143-50. 2001
    ..Therefore, amino acid position 229 may be regarded as an excellent amino acid target within the NNRTI pocket for rational drug design...
  97. ncbi request reprint Intestinal absorption characteristics of the low solubility thiocarboxanilide UC-781
    S Deferme
    Laboratory of Pharmacotechnology and Biopharmacy, Katholieke Universiteit Leuven, O and N, Gasthuisberg, 3000 Leuven, Belgium
    Int J Pharm 234:113-9. 2002
    ..The inclusion of the solubility/dissolution rate-enhancing agent VitE-TPGS did not result in absorption enhancement in the intestinal perfusion technique...
  98. 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
  99. ncbi request reprint Effect of antimetabolite drugs of nucleotide metabolism on the anti-human immunodeficiency virus activity of nucleoside reverse transcriptase inhibitors
    J Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000, Leuven, Belgium
    Pharmacol Ther 87:175-87. 2000
    ..A profound evaluation of this relatively new concept in the clinical setting will reveal whether this approach will establish a place in future treatment modalities of HIV infections...
  100. ncbi request reprint The multifunctional deoxynucleoside kinase of insect cells is a target for the development of new insecticides
    J Balzarini
    Rega Institute for Medical Research, Leuven, Belgium
    Mol Pharmacol 57:811-9. 2000
    ..Our data indicate that insect multifunctional deoxyribonucleoside kinase should be considered an entirely novel and attractive target in the development of new nucleoside types of highly selective insecticidal drugs...
  101. ncbi request reprint 9-(2-phosphonylmethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine: a novel prodrug of 9-(2-phosphonylmethoxyethyl)guanine with improved antitumor efficacy and selectivity in choriocarcinoma-bearing rats
    L Naesens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Oncol Res 11:195-203. 1999
    ..Based on its efficacy and therapeutic safety, cPr-PMEDAP can be regarded as a promising antitumor agent, which merits further in vivo evaluation in additional tumor models for human neoplasms...