Erik De Clercq

Summary

Affiliation: Katholieke Universiteit Leuven
Country: Belgium

Publications

  1. ncbi request reprint Emerging antiviral drugs
    Erik De Clercq
    Katholieke Universiteit Leuven, Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Expert Opin Emerg Drugs 13:393-416. 2008
  2. ncbi request reprint The acyclic nucleoside phosphonates from inception to clinical use: historical perspective
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 75:1-13. 2007
  3. doi request reprint Antiviral drug discovery: ten more compounds, and ten more stories (part B)
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Med Res Rev 29:571-610. 2009
  4. doi request reprint Antiviral agents acting as DNA or RNA chain terminators
    E De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, Leuven, B 3000, Belgium
    Handb Exp Pharmacol . 2009
  5. ncbi request reprint Curious (Old and New) Antiviral Nucleoside Analogues with Intriguing Therapeutic Potential
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Med Chem 22:3866-80. 2015
  6. doi request reprint Chemotherapy of respiratory syncytial virus infections: the final breakthrough
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Int J Antimicrob Agents 45:234-7. 2015
  7. doi request reprint Ebola virus (EBOV) infection: Therapeutic strategies
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Biochem Pharmacol 93:1-10. 2015
  8. doi request reprint Current race in the development of DAAs (direct-acting antivirals) against HCV
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Biochem Pharmacol 89:441-52. 2014
  9. doi request reprint Selective anti-herpesvirus agents
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Antivir Chem Chemother 23:93-101. 2013
  10. doi request reprint Dancing with chemical formulae of antivirals: A panoramic view (Part 2)
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Biochem Pharmacol 86:1397-410. 2013

Detail Information

Publications123 found, 100 shown here

  1. ncbi request reprint Emerging antiviral drugs
    Erik De Clercq
    Katholieke Universiteit Leuven, Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Expert Opin Emerg Drugs 13:393-416. 2008
    ....
  2. ncbi request reprint The acyclic nucleoside phosphonates from inception to clinical use: historical perspective
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 75:1-13. 2007
    ..between Antonín Holý [Institute of Organic Chemistry and Biochemistry (IOCB, Prague, Czech Republic)] and Erik De Clercq (Rega Institute for Medical Research, K.U. Leuven, Belgium) started exactly 30 years ago...
  3. doi request reprint Antiviral drug discovery: ten more compounds, and ten more stories (part B)
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Med Res Rev 29:571-610. 2009
    ....
  4. doi request reprint Antiviral agents acting as DNA or RNA chain terminators
    E De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, Leuven, B 3000, Belgium
    Handb Exp Pharmacol . 2009
    ..A further discussion of clinical applications in combination therapy can be found in Chap. 12...
  5. ncbi request reprint Curious (Old and New) Antiviral Nucleoside Analogues with Intriguing Therapeutic Potential
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Med Chem 22:3866-80. 2015
    ....
  6. doi request reprint Chemotherapy of respiratory syncytial virus infections: the final breakthrough
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Int J Antimicrob Agents 45:234-7. 2015
    ..A new antiviral, GS-5806, which interferes with virus-cell fusion, has proven efficacious in experimental RSV infections in adults. ..
  7. doi request reprint Ebola virus (EBOV) infection: Therapeutic strategies
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Biochem Pharmacol 93:1-10. 2015
    ....
  8. doi request reprint Current race in the development of DAAs (direct-acting antivirals) against HCV
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Biochem Pharmacol 89:441-52. 2014
    ..e. 12 weeks) of treatment, and (iv) a sustained viral response (SVR) and definite cure of the disease. ..
  9. doi request reprint Selective anti-herpesvirus agents
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Antivir Chem Chemother 23:93-101. 2013
    ....
  10. doi request reprint Dancing with chemical formulae of antivirals: A panoramic view (Part 2)
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium Electronic address
    Biochem Pharmacol 86:1397-410. 2013
    ..Antonín Holý's legacy for its activity against poxviruses and CMV infections, and (x) noroviruses for which the ideal antiviral compounds are still awaited for. ..
  11. doi request reprint Dancing with chemical formulae of antivirals: a personal account
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 86:711-25. 2013
    ..e. GS-9191 and GS-9219); (8) new ANPs: O-DAPy and 5-aza-C phosphonates; (9) non-nucleoside reverse transcriptase inhibitors (NNRTIs): HEPT and TIBO derivatives; and (10) bicyclam derivatives (i.e. AMD3100). ..
  12. doi request reprint The Holý Trinity: the acyclic nucleoside phosphonates
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Adv Pharmacol 67:293-316. 2013
    ....
  13. doi request reprint The nucleoside reverse transcriptase inhibitors, nonnucleoside reverse transcriptase inhibitors, and protease inhibitors in the treatment of HIV infections (AIDS)
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Adv Pharmacol 67:317-58. 2013
    ....
  14. doi request reprint Antiviral drug development--success and failure: a personal perspective with a Japanese connection
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Antivir Chem Chemother 23:45-55. 2013
    ....
  15. doi request reprint Antivirals: past, present and future
    Erik De Clercq
    Department of Microbiology and Immunology, Rega Institute for Medical Research, KU Leuven, Belgium
    Biochem Pharmacol 85:727-44. 2013
    ....
  16. doi request reprint The race for interferon-free HCV therapies: a snapshot by the spring of 2012
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Rev Med Virol 22:392-411. 2012
    ..The abundance of candidate anti-HCV drugs will, on the one hand, speed up their development but, on the other hand, complicate the choice of the most appropriate drug combination(s)...
  17. doi request reprint Human viral diseases: what is next for antiviral drug discovery?
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Opin Virol 2:572-9. 2012
    ..Yet, new drugs are at the horizon for the treatment of herpes simplex virus (HSV), varicella-zoster virus (VZV), poxvirus, hepatitis B virus (HBV), influenza and enveloped viruses-at-large...
  18. doi request reprint Tenofovir: quo vadis anno 2012 (where is it going in the year 2012)?
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat, 10, B 3000, Leuven, Belgium
    Med Res Rev 32:765-85. 2012
    ..Third, Truvada can be used prophylactically to prevent transmission of HIV infection. And fourth, to prevent sexual HIV transmission, tenofovir could also be used topically (i.e., as a vaginal gel)...
  19. doi request reprint Where rilpivirine meets with tenofovir, the start of a new anti-HIV drug combination era
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 84:241-8. 2012
    ..Exactly twenty-five years later rilpivirine and tenofovir joined each other, together with emtricitabine, in the same "combo" pill, representing a full treatment regimen for AIDS (HIV infection) based on a single once-daily pill...
  20. doi request reprint Ten paths to the discovery of antivirally active nucleoside and nucleotide analogues
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 31:339-52. 2012
    ....
  21. doi request reprint Pre-exposure chemoprophylaxis of HIV infection: quo vadis?
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 83:567-73. 2012
    ..Other PrEP studies are still ongoing. Available data point to the efficacy and safety of TDF with or without FTC in the prophylaxis of HIV infection (AIDS)...
  22. ncbi request reprint Recent highlights in the development of new antiviral drugs
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Opin Microbiol 8:552-60. 2005
    ..e. human papilloma viruses, adenoviruses, human herpesvirus type 6, poxviruses, severe acute respiratory syndrome coronavirus and hemorrhagic fever viruses)...
  23. pmc Antiviral prodrugs - the development of successful prodrug strategies for antiviral chemotherapy
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Br J Pharmacol 147:1-11. 2006
    ..This review will chart the origins and development of the most important of the antiviral prodrugs to date...
  24. ncbi request reprint John Montgomery's legacy: carbocyclic adenosine analogues as SAH hydrolase inhibitors with broad-spectrum antiviral activity
    Erik De Clercq
    Rega Institute for Medical Research, Department of Microbiology and Immunology, K U Letven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 24:1395-415. 2005
    ....
  25. ncbi request reprint Potential antivirals and antiviral strategies against SARS coronavirus infections
    Erik De Clercq
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10B 3000 Leuven, Belgium
    Expert Rev Anti Infect Ther 4:291-302. 2006
    ....
  26. ncbi request reprint Acyclic nucleoside phosphonates: past, present and future. Bridging chemistry to HIV, HBV, HCV, HPV, adeno-, herpes-, and poxvirus infections: the phosphonate bridge
    E De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 73:911-22. 2007
    ..e. PMPO-DAPy, PMEO-DAPy, HPMPO-DAPy) and cyclic nucleoside phosphonates (i.e. PMDTA, PMDTT, GS9148) have been accredited with an antiviral potency and selectivity similar to those of cidofovir, adefovir and/or tenofovir...
  27. ncbi request reprint Antiviral agents active against influenza A viruses
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Nat Rev Drug Discov 5:1015-25. 2006
    ..This article reviews agents that have been shown to have activity against influenza A viruses and discusses their therapeutic potential, and also describes emerging strategies for targeting these viruses...
  28. ncbi request reprint In search of effective anti-HHV-6 agents
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Clin Virol 37:S82-6. 2006
    ....
  29. ncbi request reprint Avian influenza A (H5N1) infection: targets and strategies for chemotherapeutic intervention
    Erik De Clercq
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Trends Pharmacol Sci 28:280-5. 2007
    ..As has been shown for other viral infections, RNA interference could be a powerful means with which to suppress the replication of avian H5N1...
  30. doi request reprint Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV
    Erik De Clercq
    Rega Institute for Medical Research, Department of Microbiology and Immunology, Katholieke Universiteit Leuven, Leuven, Belgium
    Int J Antimicrob Agents 33:307-20. 2009
    ..These compounds should be used in drug combination regimens to achieve the highest possible benefit, tolerability and compliance and to diminish the risk of resistance development...
  31. doi request reprint The AMD3100 story: the path to the discovery of a stem cell mobilizer (Mozobil)
    Erik De Clercq
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 77:1655-64. 2009
    ....
  32. doi request reprint Another ten stories in antiviral drug discovery (part C): "Old" and "new" antivirals, strategies, and perspectives
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Med Res Rev 29:611-45. 2009
    ....
  33. doi request reprint Yet another ten stories on antiviral drug discovery (part D): paradigms, paradoxes, and paraductions
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Med Res Rev 30:667-707. 2010
    ....
  34. doi request reprint The history of antiretrovirals: key discoveries over the past 25 years
    Erik De Clercq
    Department of Microbiology and Immunology, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Rev Med Virol 19:287-99. 2009
    ..These compounds are used in various drug combination (some at fixed dose) regimens so as to achieve the highest possible benefit and tolerability, and to diminish the risk of virus-drug resistance development...
  35. doi request reprint In search of a selective therapy of viral infections
    Erik De Clercq
    Rega Institute for Medical Research, Department of Microbiology and Immunology, KU Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 85:19-24. 2010
    ..This article forms part of a special issue of Antiviral Research marking the 25th anniversary of antiretroviral drug discovery and development, vol. 85, issue 1, 2010...
  36. doi request reprint A new drug combination therapy for treatment-naive patients with HIV-1 infection, consisting of raltegravir, emtricitabine and tenofovir disoproxil fumarate
    Erik De Clercq
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Expert Opin Pharmacother 10:2935-7. 2009
    ..e. integrase and reverse transcriptase. These multiple (triple or quadruple) drug combinations should be aimed at once daily dosing...
  37. doi request reprint The unabated synthesis of new nucleoside analogues with antiviral potential: a tribute to Morris J. Robins
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 28:586-600. 2009
    ..The furo[2,3-d]pyrimidin-2(3H)-one is the key structural determinant in the exquisitely potent activity of its derivatives (R = 2-deoxyribosyl; R' = p-pentylphenyl) against VZV (varicella-zoster virus) replication. [structure: see text]...
  38. doi request reprint Antiretroviral drugs
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Curr Opin Pharmacol 10:507-15. 2010
    ..Combination of several anti-HIV drugs [often referred to as highly active antiretroviral therapy (HAART)] has drastically altered AIDS from an almost uniformly fatal disease to a chronic manageable one...
  39. doi request reprint A 40-year journey in search of selective antiviral chemotherapy
    Erik De Clercq
    Department of Microbiology and Immunology, Rega Institute for Medical Research, Medical School University of Leuven, Belgium
    Annu Rev Pharmacol Toxicol 51:1-24. 2011
    ..This work, initiated in collaboration with the late Paul A.J. Janssen, eventually led to the identification of rilpivirine as perhaps an "ideal" NNRTI...
  40. doi request reprint Recent advances on the use of the CXCR4 antagonist plerixafor (AMD3100, Mozobil™) and potential of other CXCR4 antagonists as stem cell mobilizers
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Pharmacol Ther 128:509-18. 2010
    ..e. AMD11070, AMD3465, KRH-3955, T-140, and 4F-benzoyl-TN14003), primarily as potential anti-HIV agents. They are all strong CXCR4 antagonists. Their role in stem cell mobilization remains to be assessed...
  41. doi request reprint Strategies for the treatment of dengue virus infections: a narrative account
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Future Med Chem 2:601-8. 2010
    ..For other compounds found to be effective against the dengue virus, including geneticin (G418) and FGI-106, the mechanism of action still remains unresolved...
  42. doi request reprint The clinical potential of the acyclic (and cyclic) nucleoside phosphonates: the magic of the phosphonate bond
    Erik De Clercq
    Department of Microbiology and Immunology, K U Leuven, Rega Institute for Medical Research, Minderbroedersstraat, Leuven, Belgium
    Biochem Pharmacol 82:99-109. 2011
    ....
  43. pmc Historical perspectives in the development of antiviral agents against poxviruses
    Erik De Clercq
    Rega Institute for Medical Research, Department of Microbiology and Immunology, Minderbroedersstraat 10, B 3000 Leuven, Belgium E Mail Tel 32 16 337367
    Viruses 2:1322-39. 2010
    ....
  44. ncbi request reprint New developments in anti-HIV chemotherapy
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, Leuven, Belgium
    Biochim Biophys Acta 1587:258-75. 2002
    ....
  45. ncbi request reprint Strategies in the design of antiviral drugs
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Nat Rev Drug Discov 1:13-25. 2002
    ..Here, I describe the rationale behind current and future drug-based strategies for combating viral infections...
  46. 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...
  47. doi request reprint Substituted imidazopyridines as potent inhibitors of HCV replication
    Inge Vliegen
    Rega Institute for Medical Research, KU Leuven, Minderbroedesstraat 10, 3000 Leuven, Belgium
    J Hepatol 50:999-1009. 2009
    ..The particular characteristics of one of the most potent compounds in this series (5-[[3-(4-chlorophenyl)-5-isoxazolyl]methyl]-2-(2,3-difluorophenyl)-5H-imidazo[4,5-c]pyridine or GS-327073), were studied...
  48. ncbi request reprint New anti-HIV agents and targets
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Med Res Rev 22:531-65. 2002
    ..e., azapeptidic (atazanavir)) or non-peptidic scaffold (i.e., cyclic urea (mozenavir), 4-hydroxy-2-pyrone (tipranavir)). Non-peptidic PIs may be expected to inhibit HIV mutant strains that have become resistant to peptidomimetic PIs...
  49. 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...
  50. 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...
  51. ncbi request reprint Antivirals and antiviral strategies
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Nat Rev Microbiol 2:704-20. 2004
    ..Here, the virus infections for which antiviral therapy is needed and the compounds that are available, or are being developed, for the treatment of these infections are described...
  52. 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
    ....
  53. ncbi request reprint DNA polymerase mutations in drug-resistant herpes simplex virus mutants determine in vivo neurovirulence and drug-enzyme interactions
    Graciela Andrei
    Laboratory of Virology, Rega Institute for Medical Research, K U Leuven, Belgium
    Antivir Ther 12:719-32. 2007
    ..It appears that drug-resistant mutants arising under the pressure of HPMP derivatives have the lowest levels of neurovirulence...
  54. 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
    ....
  55. 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
    ....
  56. ncbi request reprint Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis
    Myriam Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antivir Ther 9:57-65. 2004
    ..Co-receptor antagonists such as AMD3100 show promising anti-HIV-2 therapeutic modalities. Both AMD3100 and enfuvirtide could be used for prophylaxis against SHIV89.6...
  57. 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...
  58. pmc A novel, highly selective inhibitor of pestivirus replication that targets the viral RNA-dependent RNA polymerase
    Jan Paeshuyse
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 80:149-60. 2006
    ..The potential of BPIP for the treatment of pestivirus and hepacivirus infections is discussed...
  59. ncbi request reprint In vitro evaluation of the anti-orf virus activity of alkoxyalkyl esters of CDV, cCDV and (S)-HPMPA
    Fabiana Dal Pozzo
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 75:52-7. 2007
    ..Our results support the development of alkoxyalkyl esters of ANPs as antivirals not only for the treatment of complicated human orf lesions, but also in the therapy and prophylaxis of contagious ecthyma in sheep and goats...
  60. pmc Inhibitory activities of three classes of acyclic nucleoside phosphonates against murine polyomavirus and primate simian virus 40 strains
    Ilya Lebeau
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, Leuven, Belgium
    Antimicrob Agents Chemother 51:2268-73. 2007
    ..The last class showed the highest activities and selectivities against both polyomaviruses...
  61. pmc Activities of several classes of acyclic nucleoside phosphonates against camelpox virus replication in different cell culture models
    Sophie Duraffour
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, Leuven, Belgium
    Antimicrob Agents Chemother 51:4410-9. 2007
    ..Our results demonstrate that compounds belonging to the newly synthesized ANPs, in addition to cidofovir, represent promising candidates for the treatment of poxvirus infections...
  62. pmc The thiazolobenzimidazole TBZE-029 inhibits enterovirus replication by targeting a short region immediately downstream from motif C in the nonstructural protein 2C
    Armando M De Palma
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 82:4720-30. 2008
    ..The ATPase activity of 2C, however, remained unaltered in the presence of TBZE-029...
  63. doi request reprint The discovery of antiviral agents: ten different compounds, ten different stories
    Erik De Clercq
    Katholieke Universiteit Leuven, Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Med Res Rev 28:929-53. 2008
    ....
  64. pmc Clinical potential of the acyclic nucleoside phosphonates cidofovir, adefovir, and tenofovir in treatment of DNA virus and retrovirus infections
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Clin Microbiol Rev 16:569-96. 2003
    ....
  65. 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
    ....
  66. ncbi request reprint HIV-chemotherapy and -prophylaxis: new drugs, leads and approaches
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Int J Biochem Cell Biol 36:1800-22. 2004
    ..Taken together, it is obvious that the approaches for the treatment of HIV infections in recent years have become both more diverse and more efficient...
  67. ncbi request reprint Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360
    Valery Fikkert
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    AIDS 18:2019-28. 2004
    ..Study of HIV-1 resistance development to the diketo analogue S-1360, the first HIV-1 integrase strand transfer inhibitor that has entered clinical development...
  68. ncbi request reprint New approaches toward anti-HIV chemotherapy
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Med Chem 48:1297-313. 2005
  69. ncbi request reprint The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro
    Jan Paeshuyse
    Rega Institute for Medical Research, Leuven, Belgium
    Hepatology 43:761-70. 2006
    ....
  70. ncbi request reprint Ribavirin and mycophenolic acid markedly potentiate the anti-hepatitis B virus activity of entecavir
    Chunxiao Ying
    Rega Institute for Medical Research, Faculty of Medicine, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 73:192-6. 2007
    ....
  71. pmc The imidazopyrrolopyridine analogue AG110 is a novel, highly selective inhibitor of pestiviruses that targets the viral RNA-dependent RNA polymerase at a hot spot for inhibition of viral replication
    Jan Paeshuyse
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 81:11046-53. 2007
    ..It is concluded that a single drug-binding pocket exists within the finger domain region of the BVDV RdRp that consists of two separate but potentially overlapping binding sites rather than two distinct drug-binding pockets...
  72. doi request reprint Looking back in 2009 at the dawning of antiviral therapy now 50 years ago an historical perspective
    Erik De Clercq
    Rega Institute for Medical Research, Department of Microbiology and Immunology, K U Leuven, Leuven, Belgium
    Adv Virus Res 73:1-53. 2009
    ....
  73. ncbi request reprint New class of HIV integrase inhibitors that block viral replication in cell culture
    Christophe Pannecouque
    Rega Institute for Medical Research, KULeuven, Minderbroedersstraat 10, Belgium
    Curr Biol 12:1169-77. 2002
    ....
  74. ncbi request reprint Acyclic nucleoside phosphonates: a key class of antiviral drugs
    Erik De Clercq
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Nat Rev Drug Discov 4:928-40. 2005
    ....
  75. ncbi request reprint In search of authentic inhibitors of HIV-1 integration
    Zeger Debyser
    Rega Institute for Medical Research, KU Leuven, Flanders, Belgium
    Antivir Chem Chemother 13:1-15. 2002
    ..We point to potential pitfalls in defining an inhibitor as an authentic integrase inhibitor, and propose new strategies and technologies for the discovery of authentic HIV integration inhibitors...
  76. 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
    ....
  77. 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...
  78. pmc Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations
    Valery Fikkert
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Virol 77:11459-70. 2003
    ..As to the replication kinetics of the selected strains, the replication fitness for all strains was lower than that of the wild-type HIV-1 strain...
  79. ncbi request reprint Potent, selective and cell-mediated inhibition of human herpesvirus 6 at an early stage of viral replication by the non-nucleoside compound CMV423
    Leen De Bolle
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, 3000, Leuven, Belgium
    Biochem Pharmacol 67:325-36. 2004
    ..We, therefore, conclude that CMV423 exerts its activity against HHV-6 through inhibition of a cellular process that is critical at early stages of viral replication and that may affect protein tyrosine kinase activity...
  80. pmc Establishment of a novel CCR5 and CXCR4 expressing CD4+ cell line which is highly sensitive to HIV and suitable for high-throughput evaluation of CCR5 and CXCR4 antagonists
    Katrien Princen
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Retrovirology 1:2. 2004
    ..Here, we describe the establishment of a novel CD4+ cell line, U87.CD4.CCR5.CXCR4, stably expressing both CCR5 and CXCR4 at the cell surface...
  81. pmc Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist
    Katrien Princen
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 78:12996-3006. 2004
    ..AMD3451 is the first low-molecular-weight anti-HIV agent with selective HIV coreceptor, CCR5 and CXCR4, interaction...
  82. ncbi request reprint CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro
    Kurt Vermeire
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    AIDS 18:2115-25. 2004
    ..To evaluate the anti-HIV-1 activity of the cyclotriazadisulfonamide CADA against primary isolates in vitro and the combination of CADA with approved anti-HIV drugs for potential synergy...
  83. ncbi request reprint Deoxythreosyl phosphonate nucleosides as selective anti-HIV agents
    Tongfei Wu
    Laboratories of Medicinal Chemistry and Virology, Rega Institute for Medical Research, Minderbroedersstraat 10, Leuven, Belgium
    J Am Chem Soc 127:5056-65. 2005
    ..The incorporated PMDTA fits very well in the active site pocket of HIV-1 reverse transcriptase...
  84. 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...
  85. pmc Ribavirin antagonizes the in vitro anti-hepatitis C virus activity of 2'-C-methylcytidine, the active component of valopicitabine
    Lotte Coelmont
    Rega Institute for Medical Research, KULeuven, Leuven, Belgium
    Antimicrob Agents Chemother 50:3444-6. 2006
    ..These findings may have implications when planning clinical studies with valopicitabine...
  86. ncbi request reprint Antiviral treatment of chronic hepatitis B virus infections: the past, the present and the future
    Geoffrey Férir
    Rega Institute for Medical Research, KULeuven, Leuven, Belgium
    Rev Med Virol 18:19-34. 2008
    ..Foremost among these newer compounds are adefovir dipivoxil, entecavir and telbivudine...
  87. ncbi request reprint The design of drugs for HIV and HCV
    Erik De Clercq
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    Nat Rev Drug Discov 6:1001-18. 2007
    ....
  88. ncbi request reprint Drug targets in cytomegalovirus infection
    Graciella Andrei
    Laboratory of Virology and Chemotherapy, Department of Microbiology and Immunology, Rega Institute for Medical Research, K U Leuven, Belgium
    Infect Disord Drug Targets 9:201-22. 2009
    ..This review will focus on new compounds that inhibit a specific viral process (viral targets) and on cell-based approaches (cellular targets) that result in selective inhibition of virus replication...
  89. ncbi request reprint Sugar-modified conjugated diene analogues of adenosine and uridine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects
    Stanislaw F Wnuk
    Department of Chemistry, Florida International University, Miami, FL 33199, USA
    J Med Chem 45:2651-8. 2002
    ..7 microM and cytostatic at > or =11 microM, while dienoic esters 16a,b showed activity against both varicella-zoster virus (at 10 microM, 16a) and cytomegalovirus (at 10 microM, 16a; 18 microM, 16b)...
  90. ncbi request reprint Bone marrow transplantation in a child with Wiskott-Aldrich syndrome latently infected with acyclovir-resistant (ACV(r)) herpes simplex virus type 1: emergence of foscarnet-resistant virus originating from the ACV(r) virus
    Masayuki Saijo
    Special Pathogens Laboratory, Department of Virology 1, National Institute of Infectious Diseases, Tokyo, Japan
    J Med Virol 68:99-104. 2002
    ..This is the first report on the clinical course of a BMT-associated ACV(r) HSV-1 infection that subsequently developed resistance to foscarnet as well...
  91. ncbi request reprint Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents
    Maria L Barreca
    Dipartimento Farmaco Chimico, Universita di Messina, Viale Annunziata, 98168 Messina, Italy
    J Med Chem 45:5410-3. 2002
    ..Computational studies were used to delineate the ligand-RT interactions and to probe the binding of the ligands to HIV-1 RT...
  92. ncbi request reprint Database searching for thymidine and thymidylate kinase inhibitors using three-dimensional structure-based methods
    David T Manallack
    Celltech R and D Ltd, Great Abington, Cambridge, UK
    J Enzyme Inhib Med Chem 17:167-74. 2002
    ..The best of these compounds was only 4.6-fold less potent than 3'-azido-3'-deoxythymidine-5'-monophosphate (AZTMP). This study demonstrates the utility of structure-based drug design methods in the search for novel enzyme inhibitors...
  93. ncbi request reprint Synthesis and antiviral activities of 3-aralkylthiomethylimidazo[1,2-b]pyridazine derivatives
    Christophe Galtier
    Laboratoire de Chimie Therapeutique, Faculte de Pharmacie, Tours, France
    Antivir Chem Chemother 14:177-82. 2003
    ..The results presented here suggest that compound 10 should be considered as a new lead in the development of antiviral agents...
  94. ncbi request reprint Design and synthesis of phosphonoacetic acid (PPA) ester and amide bioisosters of ribofuranosylnucleoside diphosphates as potential ribonucleotide reductase inhibitors and evaluation of their enzyme inhibitory, cytostatic and antiviral activity
    Stefano Manfredini
    Department of Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy
    Antivir Chem Chemother 14:183-94. 2003
    ....
  95. ncbi request reprint 5-Substituted-2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidines-acyclic nucleoside phosphonate analogues with antiviral activity
    Dana Hocková
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Flemingovo nam 2, CZ 166 10, Prague 6, Czech Republic
    J Med Chem 46:5064-73. 2003
    ..0023-0.0110 mumol/mL), comparable to that of the reference drugs adefovir and tenofovir, but were devoid of measurable toxicity at 0.3 mumol/mL...
  96. ncbi request reprint Structure-activity relationship studies on a novel family of specific HIV-1 reverse transcriptase inhibitors
    Maria Cruz Bonache
    Instituto de Quimica Medica CSIC, Madrid, Spain
    Antivir Chem Chemother 14:249-62. 2003
    ..Our studies demonstrate that both the carboxymethyl moiety at the nucleobase and tert-butyldimethylsilyl groups at the sugar are important structural components since deletion of either of them is detrimental to the antiviral activity...
  97. ncbi request reprint Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV
    Tokumi Maruyama
    Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan
    Antivir Chem Chemother 14:271-9. 2003
    ..We found that 1-benzyl-3-(3,5-dimethylbenzyl)uracil and 1-cyanomethyl-3-(3,5-dimethylbenzyl)-4-thiouracil showed powerful inhibition against HCMV and HIV-1, respectively...
  98. ncbi request reprint Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents
    Angela Rao
    Dipartimento Farmaco Chimico, Universita di Messina, Viale Annunziata, 98168, Messina, Italy
    Farmaco 59:33-9. 2004
    ....
  99. ncbi request reprint Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors
    Maximilian A Silvestri
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    J Med Chem 47:3149-62. 2004
    ..8 microM level. At the same time, the bis(thioester) modification was less cytotoxic to uninfected MT-4 cells, with a CC(50) of >224 microM versus 160 microM for the parent compound...
  100. ncbi request reprint Hybrids of [TSAO-T]-[foscarnet]: The first conjugate of foscarnet with a non-nucleoside reverse transcriptase inhibitor through a labile covalent ester bond
    Sonsoles Velazquez
    Instituto de Química Médica C S I C, Juan de la Cierva 3, E 28006 Madrid, Spain
    J Med Chem 47:3418-26. 2004
    ..Moreover, stability studies of the [TSAO-T]-[PFA] conjugates demonstrated that the compounds were stable in PBS whereas some of the conjugates regenerated the parent inhibitors in extracts from CEM cells...
  101. ncbi request reprint Efficient 3D database screening for novel HIV-1 IN inhibitors
    Maria Letizia Barreca
    Dipartimento Farmaco Chimico, Universita di Messina, Viale Annunziata, 98168 Messina, Italy
    J Chem Inf Comput Sci 44:1450-5. 2004
    ..Biological testing shows that our strategy was successful in searching for new structural leads as HIV-1 IN inhibitors...