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Publications


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Binding of a potent small-molecule inhibitor of six-helix bundle formation requires interactions with both heptad-repeats of the RSV fusion protein
Author(s): Dirk Roymans, Hendrik L. De Bondt, Eric Arnoult, et al

PNAS January 5, 2010, vol. 107 no. 1 308-313 doi 10.1073/pnas.0910108106:

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The Diarylquinoline TMC207 for Multidrug-Resistant Tuberculosis
Author(s): Andreas H. Diacon, Alexander Pym, Martin Grobusch et al

NEJM 2009 Jun 4; Volume 360; Number 23:2397-2405

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Telaprevir and Peginterferon with or without Ribavirin for Chronic HCV Infection
Author(s): Christophe Hézode, Nicole Forestier, Geoffrey Dusheiko et al

NEJM 2009 Apr 30;Volume 360; Number 18:1839-1850

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Telaprevir with Peginterferon and Ribavirin for Chronic HCV Genotype 1 Infection
Author(s): John G. McHutchison, Gregory T. Everson, Stuart C. Gordon et al

NEJM 2009 Apr 30; Volume 360; Number 18:1827-1838

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Diarylquinolines Are Bactericidal for Dormant Mycobacteria as a Result of Disturbed ATP Homeostasis
Author(s): Anil Koul, Luc Vranckx, Najoua Dendouga, et al

J. Biol. Chem., Vol. 283, Issue 37, 25273-25280, September 12, 2008

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Safety, Tolerability, and Preliminary Efficacy of 48 Weeks of Etravirine Therapy in a Phase IIb Dose-Ranging Study Involving Treatment-Experienced Patients with HIV-1 Infection
Author(s): Julio Montaner, Patrick Yeni, Nathan N. Clumeck, et al

Clinical Infectious Diseases 2008;47:000-000 © 2008 by the Infectious Diseases Society of America. All rights reserved. DOI: 10.1086/591705

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Efficacy and safety of once-daily darunavir/ritonavir versus lopinavir/ritonavir in treatment-naive HIV-1-infected patients at week 48
Author(s): Roberto Ortiz, Edwin DeJesus, Homayoon Khanlou, et al

AIDS: 31 July 2008 - Volume 22 - Issue 12 - p 1389-1397 doi: 10.1097/QAD.0b013e32830285fb Fast Track

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Pharmacokinetic and Pharmacodynamic Study of the Concomitant Administration of Methadone and TMC125 in HIV-Negative Volunteers
Author(s): Monika Schöller-Gyüre, Wim van den Brink, Thomas N. Kakuda, et al

The Journal of New Drugs 2008, doi:10.1177/0091270007310387

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Binding kinetics of darunavir to HIV-1 protease explain the potent antiviral activity and high genetic barrier
Author(s): Inge Dierynck, Mieke De Wit, Emmanuel Gustin, Inge Keuleers, Johan Vandersmissen, Sabine Hallenberger, and Kurt Hertogs

J. Virol. doi:10.1128/JVI.01184-07Manuscript

In vitro Anti-mycobacterial Spectrum of a Diarylquinoline ATP Synthase Inhibitor
Author(s): Emma Huitric, Peter Verhasselt, Koen Andries, and Sven E. Hoffner

Antimicrob. Agents Chemother. doi:10.1128/AAC.00181-07

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Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial
Author(s): Lazzarin A, Campbell T, Clotet B et al

Lancet 2007 Jul 7;370(9581):39-48.

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Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial
Author(s): Madruga JV, Cahn P, Grinsztejn B, Haubrich R, Lalezari J, Mills A, Pialoux G, Wilkin T, Peeters M, Vingerhoets J, de Smedt G, Leopold L, Trefiglio R, Woodfall B, on behalf of the DUET-1 study group

The Lancet - Vol. 370, Issue 9581, 07 July 2007, Pages 29-38

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Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial
Author(s): José Valdez Madruga, Daniel Berger, Marilyn McMurchie et al

The Lancet 2007; 370:49-58



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Diarylquinolines target subunit c of mycobacterial ATP synthase
Author(s): Anil Koul, Najoua Dendouga, Karen Vergauwen et al

Nature Chemical Biology 3, 323 - 324 (2007):

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Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains
Author(s): Céline Mordanta, Benoit Schmitta, Elisabeth Pasquiera, et al

European Journal of Medicinal Chemistry Volume 42, Issue 5, May 2007, Pages 567-579

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Efficacy and safety of darunavir-ritonavir at week 48 in treatment-experienced patients with HIV-1 infection in POWER 1 and 2: a pooled subgroup analysis of data from two randomised trials
Author(s): Clotet, Bonaventura; Bellos, Nicholas; Molina, Jean-Michel; et al

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Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1: primary 24-week analysis
Author(s): The TMC125-C223 Writing Group

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Week 24 efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients
Author(s): Haubrich, Richard; Berger, Dan; Chiliade, Philippe et al

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Efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients: 24-week results of POWER 1
Author(s): Katlama, Christine; Esposito, Roberto; Gatell, Jose M et al.

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Dose-Ranging Phase 1 Study of TMC120, a Promising Vaginal Microbicide, in HIV-Negative and HIV-Positive Female Volunteers.
Author(s): Jespers, Vicky; Van Roey, Jens; Beets, Greet; Buve, Anne

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Short-term antiviral activity of TMC278 - a novel NNRTI - in treatment-naive HIV-1-infected subjects
Author(s): Goebel, Frank; Yakovlev, Alexy; Pozniak, Anton L; et al

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Binding kinetics, uptake and intracellular accumulation of F105, an anti-gp120 human IgG1k monoclonal antibody, in HIV-1 infected cells
Author(s): Reginald Clayton, Asa Ohagen, Olivia Goethals, et al

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Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors
Author(s): Pierre Raboisson, Oliver Lenz, Tse-I Lin, Dominique Surleraux, Sarvajit Chakravarty, Annick Scholliers, Katrien Vermeiren, Frederic Delouvroy, Thierry Verbinnen and Kenneth Simmen

Bioorganic & Medicinal Chemistry Letters, Volume 17, Issue 7, 1 April 2007, Pages 1843-1849

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Indolopyridones Inhibit HIV Reverse Transcriptase with a Novel Mechanism of Action
Author(s): Dirk Jochmans, Jerome Deval, Bart Kesteleyn, et al.

Journal of Virology, December 2006, p. 12283-12292, Vol. 80, No. 24. Link: http://jvi.asm.org/cgi/content/abstract/80/24/12283Manuscript

Combinations of R207910 with Drugs Used To Treat Multidrug-Resistant Tuberculosis Have the Potential To Shorten Treatment Duration
Author(s): Nacer Lounis, Nicolas Veziris, Aurelie Chauffour, Chantal Truffot-Pernot, Koen Andries, and Vincent Jarlier

http://aac.asm.org/cgi/content/abstract/50/11/3543?etoc

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TMC125 Displays a High Genetic Barrier to the Development of Resistance: Evidence from in vitro selection experiments
Author(s): Johan Vingerhoets, Hilde Azijn, Els Fransen, Inky De Baere, Liesbet Smeulders, Dirk Jochmans, Koen Andries, Rudi Pauwels, and Marie-Pierre de Bethune

http://jvi.asm.org/cgi/reprint/79/20/12773

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Discovery and Selection of TMC114, a Next Generation HIV-1 Protease Inhibitor
Author(s): D. Surleraux, A Tahri, W Verschueren, G Pille, et al

J Med Chem, Vol 48, No 6, 2005

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TMC114/ritonavir substitution for protease inhibitor(s) in a non-suppressive antiretroviral regimen: a 14-day proof-of-principle trial
Author(s): Keikawus Arasteh, Nathan Clumeck, Anton Pozniak, Adriano Lazzarin, Sandra De Meyer, Heidi Muller, Monika Peeters, Alex Rinehart, Eric Lefebvre for the TMC114-C207 Study Team

http://www.aidsonline.com/pt/re/aids/abstract.00002030-200506100-00011.htm;jsessionid=CobSLbog4zEJIgC2LEe7tdPI2WEEqwIQjkq40HddRjqCd24uvi30!-2006515172!-949856031!9001!-1

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TMC 114, a Novel HIV-1 Protease Inhibitor active against Protease Inhibitor-Resistant Viruses, including a broad range of clinical isolates
Author(s): Sandra De Meyer, Hilde Azijn, Dominique Surleraux, Dirk Jochmans, Abdellah Rahri, Rudi Pauwels, Piet Wigerinck, and Marie-Pierre de Bethune

http://aac.asm.org/cgi/content/abstract/49/6/2314?etoc

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A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis
Author(s): K.Andries,P.Verhasselt,J.Guillemont,H.W.H.Gohlmann,JM.Neefs,H.Winkler,J.VanGestel,P.Timmerman,Min Zhu,E. Lee,P.Williams,D.deChaffoy,E.Huitric,S.Hoffner,E.Cambau,C.Truffot-Pernot,N.Lounis,V.Jarlier

http://www.sciencemag.org/cgi/content/short/307/5707/223

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TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant HIV type 1
Author(s): Koen Andries, Hilde Azijn, Theo Thielemans, ...

Antimicrobial Agents and Chemotherapy, Dec 2004, p 4680-4686

Abstract
Structural and thermodynamic basis for the binding of TMC114, a next generation...
Author(s): Nancy M. King, Moses Prabu-Jeyabalan, Ellen A. Nalivaika, Piet Wigerinck, ...

Journal of Virology, Nov 2004, p. 12012-12021

Abstract
Roles on conformational and positional adaptability in structure-based design of TMC125-R165335 ...
Author(s): Kalyan Das, Arthur D. Clark Jr, Paul. J. Lewi, ...

J. Med. Chem 2004, 47, 2550-2560

Abstract
TMC125, a novel next generation non-nucleoside reverse transcriptase inhibitor active against non-nucleoside reverse transcriptase inhibitor-resistant HIV-1
Author(s): K. Andries, H. Azijn, T. Thielemans et al

Antimicrobial Agents and Chemotherapy, December 2004, p. 4680-4686, Vol. 48, No. 12

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Comparative Efficacy of Topical Therapy with a Slow-Release Mucoadhesive Buccal Tablet Containing Miconazole Nitrate Versus Systemic Therapy With Ketoconazole in HIV-Positive Patients With Oropharyngeal Candidiasis
Author(s): J. Van Roey, M. Haxaire, M. Kamya, I. Lwanga, E. Katabira

J Acquir Immune Defic Syndr, Vol 35, No 2, February 1 2004

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An open-label assessment of TMC125 - a new, next generation NNRTI, for 7 days in HIV-1 infected individuals with NNRTI resistance
Author(s): B. Gazzard, A. Pozniak, W. Rosenbaum et al

AIDS 2003, Vol 17, No 18, p. 49-54

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Novel bis-Tetrahydrofuranylurethane - containing Nonpeptidic Protease Inhibitor UIC-94017 with Potent Activity against Multi-PI-resistant HIV in vitro
Author(s): Yasuhiro Koh, Hiromoto Nakata et al

Antimicrobial Agents and Chemotherapy, Oct. 2003, p. 3123-3129

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Encoding microcarriers by spatial selective photobleaching
Author(s): K. Braeckmans, S. De Smedt, C. Roelant, M. Leblans, R. Pauwels, J. Demeester

Nature, Materials, Aug 2003

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TMC125 exerts similar initial antiviral potency as a five-drug, triple class antiretroviral regimen
Author(s): S. Sankatsing, G. Weverling, M. Peeters et al

AIDS 2003, Vol 17, No 18, p. 2623-2627

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A randomized, double-blind, placebo-controlled trial of TMC125 as 7-day monotherapy in antiretroviral naive, HIV-1 infected subjects
Author(s): B. Gruzdev, A. Rakhmanova, E. Doubovskaya et al

AIDS 2003, Vol 17, No 17, p. 2487-2494

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Inhibition of vaginal transmission of HIV-1 in hu-SCID mice by the non-nucleoside reverse transcriptase inhibitor TMC120 in a gel formulation
Author(s): S. Di Fabio, J. Van Roey, G. Giannini et al

AIDS 2003, Vol 17, No 11, p. 1597-1604

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Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives.
Author(s): Rudi Pauwels, Koen Andries, Jan Desmyter, Dominique Schols, ...

Nature. Pages: 470-4; Volume(Issue): 343 (6257)

Abstract
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