Tse I Lin

Summary

Affiliation: Johnson and Johnson Pharmaceutical Research and Development
Country: USA

Publications

  1. pmc In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor
    Tse I Lin
    Tibotec BVBA, Gen De Wittelaan L11 B3, Mechelen, Belgium
    Antimicrob Agents Chemother 53:1377-85. 2009
  2. ncbi request reprint Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors
    Pierre Raboisson
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 17:1843-9. 2007
  3. doi request reprint Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350
    Pierre Raboisson
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 18:4853-8. 2008
  4. pmc In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435
    Oliver Lenz
    Tibotec BVBA, Mechelen, Belgium
    Antimicrob Agents Chemother 54:1878-87. 2010
  5. doi request reprint Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors
    Pierre Raboisson
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 18:5095-100. 2008
  6. doi request reprint 2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase
    Tim H M Jonckers
    Tibotec BVBA, A Division of Janssen Pharmaceutical Companies of Johnson and Johnson, Turnhoutseweg 30, 2340 Beerse, Belgium
    J Med Chem 53:8150-60. 2010
  7. doi request reprint Development of a high-content screening assay to identify compounds interfering with the formation of the hepatitis C virus replication complex
    Jan Martin Berke
    Tibotec BVBA, 2800 Mechelen, Belgium
    J Virol Methods 165:268-76. 2010
  8. doi request reprint Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors
    Sandrine Vendeville
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 18:6189-93. 2008
  9. pmc Tracking the evolution of multiple in vitro hepatitis C virus replicon variants under protease inhibitor selection pressure by 454 deep sequencing
    Thierry Verbinnen
    Tibotec BVBA, Turnhoutsebaan, 302340 Beerse, Belgium
    J Virol 84:11124-33. 2010
  10. pmc Antiviral activity and mode of action of TMC647078, a novel nucleoside inhibitor of the hepatitis C virus NS5B polymerase
    Jan Martin Berke
    Tibotec Virco Virology BVBA, Turnhoutseweg 30, 2340 Beerse, Belgium
    Antimicrob Agents Chemother 55:3812-20. 2011

Collaborators

  • Pierre Raboisson
  • Oliver Lenz
  • Maxwell D Cummings
  • Jan Martin Berke
  • Carlo W Boutton
  • Tim H M Jonckers
  • Jean Francois Bonfanti
  • Johan Neyts
  • Matthias Gotte
  • Laurent Leclercq
  • Kenneth Simmen
  • David McGowan
  • Sandrine Vendeville
  • Thierry Verbinnen
  • Gregory Fanning
  • Abdellah Tahri
  • Lili Hu
  • Frederic Delouvroy
  • Ina Vandenbroucke
  • Herwig Van Marck
  • Marijke Claes
  • Leen Vijgen
  • Geert Pille
  • Klara Rombauts
  • Hendrik De Bondt
  • Wendy Mostmans
  • Walter Van den Broeck
  • Liesbet van der Helm
  • Kristof Van Emelen
  • Erna Cleiren
  • Koen Vandyck
  • Katrien Vermeiren
  • Geneviève Vandercruyssen
  • Ludo Quirynen
  • Frederik Pauwels
  • Katie Amssoms
  • Stefaan Last
  • Origene Nyanguile
  • Pedro Lory
  • Kristina Wikstrom
  • Magnus Nilsson
  • Marleen Van Dooren
  • Piet Wigerinck
  • Pia Kahnberg
  • Per Ola Johansson
  • Michael Edlund
  • Asa Rosenquist
  • Wim Van de Vreken
  • Anders Eneroth
  • Bertil Samuelsson
  • Lotta Vrang
  • Stefan Lindström
  • Vladimir Ivanov
  • Herman de Kock
  • Susana Ayesa
  • Björn Classon
  • Dmitry Antonov
  • Dominique Surleraux
  • Natalie Kindermans

Detail Information

Publications11

  1. pmc In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor
    Tse I Lin
    Tibotec BVBA, Gen De Wittelaan L11 B3, Mechelen, Belgium
    Antimicrob Agents Chemother 53:1377-85. 2009
    ..In conclusion, given the selective and potent in vitro anti-HCV activity, the potential for combination with other anti-HCV agents, and the favorable pharmacokinetic profile, TMC435350 has been selected for clinical development...
  2. ncbi request reprint Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors
    Pierre Raboisson
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 17:1843-9. 2007
    ..Moreover, 36 showed an advantageous PK profile in mice. Experiments performed using different replicon constructs suggest that this series of kinase inhibitors might mediate their effect through the HCV non-structural protein 5A (NS5A)...
  3. doi request reprint Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350
    Pierre Raboisson
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 18:4853-8. 2008
    ..36nM) and viral replication (replicon EC(50)=7.8nM). TMC435350 also displayed low in vitro clearance and high permeability, which were confirmed by in vivo pharmacokinetic studies. TMC435350 is currently being evaluated in the clinics...
  4. pmc In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435
    Oliver Lenz
    Tibotec BVBA, Mechelen, Belgium
    Antimicrob Agents Chemother 54:1878-87. 2010
    ..Finally, combinations of TMC435 with alpha interferon and NS5B polymerase inhibitors prevented the formation of drug-resistant replicon colonies...
  5. doi request reprint Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors
    Pierre Raboisson
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 18:5095-100. 2008
    ..20 nM, EC(50)=3.7 nM), selective, and orally bioavailable dipeptide NS3/4A protease inhibitor, which has features attractive for further preclinical development...
  6. doi request reprint 2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase
    Tim H M Jonckers
    Tibotec BVBA, A Division of Janssen Pharmaceutical Companies of Johnson and Johnson, Turnhoutseweg 30, 2340 Beerse, Belgium
    J Med Chem 53:8150-60. 2010
    ..The oral dosing of 23 led to substantially increased exposure to 5 in both rats and dogs...
  7. doi request reprint Development of a high-content screening assay to identify compounds interfering with the formation of the hepatitis C virus replication complex
    Jan Martin Berke
    Tibotec BVBA, 2800 Mechelen, Belgium
    J Virol Methods 165:268-76. 2010
    ..Finally, the addition of a HCV NS3/4A protease inhibitor resulted in a dose-dependent reduction of "dot-like" structures demonstrating the practicability of the assay...
  8. doi request reprint Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors
    Sandrine Vendeville
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 18:6189-93. 2008
    ..1 nM, EC(50)=4.5 nM) and selective (CC(50) (Huh-7 cells)>50 microM) inhibitor, displaying an excellent PK profile in rats characterized by an oral bioavailability of 54% and a high liver exposure after oral administration...
  9. pmc Tracking the evolution of multiple in vitro hepatitis C virus replicon variants under protease inhibitor selection pressure by 454 deep sequencing
    Thierry Verbinnen
    Tibotec BVBA, Turnhoutsebaan, 302340 Beerse, Belgium
    J Virol 84:11124-33. 2010
    ....
  10. pmc Antiviral activity and mode of action of TMC647078, a novel nucleoside inhibitor of the hepatitis C virus NS5B polymerase
    Jan Martin Berke
    Tibotec Virco Virology BVBA, Turnhoutseweg 30, 2340 Beerse, Belgium
    Antimicrob Agents Chemother 55:3812-20. 2011
    ..TMC647078 is a potent novel nucleoside inhibitor of HCV replication with a promising in vitro virology and biology profile...
  11. doi request reprint 1,5-Benzodiazepine inhibitors of HCV NS5B polymerase
    David McGowan
    Tibotec BVBA, Gen De Wittelaan L11 B3, B 2800 Mechelen, Belgium
    Bioorg Med Chem Lett 19:2492-6. 2009
    ..These data warrant further lead-optimization efforts...