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Items: 1 to 50 of 62

1.

Virological characterization of patients failing darunavir/ritonavir or lopinavir/ritonavir treatment in the ARTEMIS study: 96-week analysis.

Lathouwers E, De Meyer S, Dierynck I, Van de Casteele T, Lavreys L, de Béthune MP, Picchio G.

Antivir Ther. 2011;16(1):99-108. doi: 10.3851/IMP1719.

PMID:
21311113
2.

In vitro susceptibility and virological outcome to darunavir and lopinavir are independent of HIV type-1 subtype in treatment-naive patients.

Dierynck I, De Meyer S, Lathouwers E, Vanden Abeele C, Van De Casteele T, Spinosa-Guzman S, de Béthune MP, Picchio G.

Antivir Ther. 2010;15(8):1161-9. doi: 10.3851/IMP1697.

PMID:
21149923
3.

Characterization of genotypic and phenotypic changes in HIV-1-infected patients with virologic failure on an etravirine-containing regimen in the DUET-1 and DUET-2 clinical studies.

Tambuyzer L, Vingerhoets J, Azijn H, Daems B, Nijs S, de Béthune MP, Picchio G.

AIDS Res Hum Retroviruses. 2010 Nov;26(11):1197-205. doi: 10.1089/aid.2009.0302. Epub 2010 Sep 20.

PMID:
20854144
4.

Short communication: activity of etravirine on different HIV type 1 subtypes: in vitro susceptibility in treatment-naive patients and week 48 pooled DUET study data.

Vingerhoets J, Azijn H, Tambuyzer L, Dierynck I, De Meyer S, Rimsky L, Nijs S, De Smedt G, de Béthune MP, Picchio G.

AIDS Res Hum Retroviruses. 2010 Jun;26(6):621-4. doi: 10.1089/aid.2009.0239.

PMID:
20507207
5.

Resistance profile of etravirine: combined analysis of baseline genotypic and phenotypic data from the randomized, controlled Phase III clinical studies.

Vingerhoets J, Tambuyzer L, Azijn H, Hoogstoel A, Nijs S, Peeters M, de Béthune MP, De Smedt G, Woodfall B, Picchio G.

AIDS. 2010 Feb 20;24(4):503-14. doi: 10.1097/QAD.0b013e32833677ac.

PMID:
20051805
6.

TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.

Azijn H, Tirry I, Vingerhoets J, de Béthune MP, Kraus G, Boven K, Jochmans D, Van Craenenbroeck E, Picchio G, Rimsky LT.

Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. doi: 10.1128/AAC.00986-09. Epub 2009 Nov 23.

7.

Non-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 infection: a review of the last 20 years (1989-2009).

de Béthune MP.

Antiviral Res. 2010 Jan;85(1):75-90. doi: 10.1016/j.antiviral.2009.09.008. Epub 2009 Sep 23. Review.

PMID:
19781578
8.

Short-term randomized proof-of-principle trial of TMC278 in patients with HIV type-1 who have previously failed antiretroviral therapy.

Arastéh K, Rieger A, Yeni P, Pozniak A, Boogaerts G, van Heeswijk R, de Béthune MP, Peeters M, Woodfall B.

Antivir Ther. 2009;14(5):713-22.

PMID:
19704175
9.

Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.

Guillemont J, Benjahad A, Oumouch S, Decrane L, Palandjian P, Vernier D, Queguiner L, Andries K, de Béthune MP, Hertogs K, Grierson DS, Nguyen CH.

J Med Chem. 2009 Dec 10;52(23):7473-87. doi: 10.1021/jm900802y.

PMID:
19645483
10.

The impact of individual human immunodeficiency virus type 1 protease mutations on drug susceptibility is highly influenced by complex interactions with the background protease sequence.

Van Marck H, Dierynck I, Kraus G, Hallenberger S, Pattery T, Muyldermans G, Geeraert L, Borozdina L, Bonesteel R, Aston C, Shaw E, Chen Q, Martinez C, Koka V, Lee J, Chi E, de Béthune MP, Hertogs K.

J Virol. 2009 Sep;83(18):9512-20. doi: 10.1128/JVI.00291-09. Epub 2009 Jul 8.

11.

Characterization of virologic failure patients on darunavir/ritonavir in treatment-experienced patients.

De Meyer S, Lathouwers E, Dierynck I, De Paepe E, Van Baelen B, Vangeneugden T, Spinosa-Guzman S, Lefebvre E, Picchio G, de Béthune MP.

AIDS. 2009 Sep 10;23(14):1829-40. doi: 10.1097/QAD.0b013e32832cbcec.

PMID:
19474650
12.

Compilation and prevalence of mutations associated with resistance to non-nucleoside reverse transcriptase inhibitors.

Tambuyzer L, Azijn H, Rimsky LT, Vingerhoets J, Lecocq P, Kraus G, Picchio G, de Béthune MP.

Antivir Ther. 2009;14(1):103-9.

PMID:
19320243
13.

Influence of baseline protease inhibitor resistance on the efficacy of darunavir/ritonavir or lopinavir/ritonavir in the TITAN trial.

De Meyer S, Hill A, Picchio G, DeMasi R, De Paepe E, de Béthune MP.

J Acquir Immune Defic Syndr. 2008 Dec 15;49(5):563-4. doi: 10.1097/QAI.0b013e318183ac9c. No abstract available.

PMID:
19202459
14.

Efficacy and safety of etravirine (TMC125) in treatment-experienced HIV-1-infected patients: 48-week results of a phase IIb trial.

Cohen CJ, Berger DS, Blick G, Grossman HA, Jayaweera DT, Shalit P, Thompson M, Peeters M, de Béthune MP, Voorspoels E, Mack R, Woodfall B.

AIDS. 2009 Jan 28;23(3):423-6. doi: 10.1097/QAD.0b013e32831c5040.

PMID:
19114852
15.

Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.

Fletcher P, Harman S, Azijn H, Armanasco N, Manlow P, Perumal D, de Bethune MP, Nuttall J, Romano J, Shattock R.

Antimicrob Agents Chemother. 2009 Feb;53(2):487-95. doi: 10.1128/AAC.01156-08. Epub 2008 Nov 24.

16.

Effect of baseline viral susceptibility on response to darunavir/ritonavir versus control protease inhibitors in treatment-experienced HIV type 1-infected patients: POWER 1 and 2.

Pozniak A, Opravil M, Beatty G, Hill A, de Béthune MP, Lefebvre E.

AIDS Res Hum Retroviruses. 2008 Oct;24(10):1275-80. doi: 10.1089/aid.2007.0275.

PMID:
18844462
17.

Efficacy of once-daily darunavir/ritonavir 800/100 mg in HIV-infected, treatment-experienced patients with no baseline resistance-associated mutations to darunavir.

De Meyer SM, Spinosa-Guzman S, Vangeneugden TJ, de Béthune MP, Miralles GD.

J Acquir Immune Defic Syndr. 2008 Oct 1;49(2):179-82. doi: 10.1097/QAI.0b013e318183a959.

PMID:
18769351
18.

Resistance profile of darunavir: combined 24-week results from the POWER trials.

de Meyer S, Vangeneugden T, van Baelen B, de Paepe E, van Marck H, Picchio G, Lefebvre E, de Béthune MP.

AIDS Res Hum Retroviruses. 2008 Mar;24(3):379-88. doi: 10.1089/aid.2007.0173.

PMID:
18327986
19.

Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent.

Ptak RG, Gallay PA, Jochmans D, Halestrap AP, Ruegg UT, Pallansch LA, Bobardt MD, de Béthune MP, Neyts J, De Clercq E, Dumont JM, Scalfaro P, Besseghir K, Wenger RM, Rosenwirth B.

Antimicrob Agents Chemother. 2008 Apr;52(4):1302-17. doi: 10.1128/AAC.01324-07. Epub 2008 Jan 22.

20.

Response to "key amprenavir resistance mutations counteract dramatic efficacy of darunavir in highly experienced patients".

Picchio G, De Meyer S, de Béthune MP.

AIDS. 2008 Jan 2;22(1):165-7. Review. No abstract available.

PMID:
18090413
21.

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.

Madruga JV, Berger D, McMurchie M, Suter F, Banhegyi D, Ruxrungtham K, Norris D, Lefebvre E, de Béthune MP, Tomaka F, De Pauw M, Vangeneugden T, Spinosa-Guzman S; TITAN study group.

Lancet. 2007 Jul 7;370(9581):49-58.

PMID:
17617272
22.

Screening and selecting for optimized antiretroviral drugs: rising to the challenge of drug resistance.

de Béthune MP, Hertogs K.

Curr Med Res Opin. 2006 Dec;22(12):2603-12. Review.

PMID:
17166342
23.

A dual chamber model of female cervical mucosa for the study of HIV transmission and for the evaluation of candidate HIV microbicides.

Van Herrewege Y, Michiels J, Waeytens A, De Boeck G, Salden E, Heyndrickx L, van den Mooter G, de Béthune MP, Andries K, Lewi P, Praet M, Vanham G.

Antiviral Res. 2007 May;74(2):111-24. Epub 2006 Nov 7.

PMID:
17097156
24.

Potent nonnucleoside reverse transcriptase inhibitors target HIV-1 Gag-Pol.

Figueiredo A, Moore KL, Mak J, Sluis-Cremer N, de Bethune MP, Tachedjian G.

PLoS Pathog. 2006 Nov;2(11):e119.

25.

Short-term antiviral activity of TMC278--a novel NNRTI--in treatment-naive HIV-1-infected subjects.

Goebel F, Yakovlev A, Pozniak AL, Vinogradova E, Boogaerts G, Hoetelmans R, de Béthune MP, Peeters M, Woodfall B.

AIDS. 2006 Aug 22;20(13):1721-6.

PMID:
16931936
26.

Modulation of human immunodeficiency virus type 1 synergistic inhibition by reverse transcriptase mutations.

Basavapathruni A, Vingerhoets J, de Béthune MP, Chung R, Bailey CM, Kim J, Anderson KS.

Biochemistry. 2006 Jun 13;45(23):7334-40.

PMID:
16752922
27.

TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments.

Vingerhoets J, Azijn H, Fransen E, De Baere I, Smeulders L, Jochmans D, Andries K, Pauwels R, de Béthune MP.

J Virol. 2005 Oct;79(20):12773-82.

28.

TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates.

De Meyer S, Azijn H, Surleraux D, Jochmans D, Tahri A, Pauwels R, Wigerinck P, de Béthune MP.

Antimicrob Agents Chemother. 2005 Jun;49(6):2314-21.

29.

Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.

Guillemont J, Pasquier E, Palandjian P, Vernier D, Gaurrand S, Lewi PJ, Heeres J, de Jonge MR, Koymans LM, Daeyaert FF, Vinkers MH, Arnold E, Das K, Pauwels R, Andries K, de Béthune MP, Bettens E, Hertogs K, Wigerinck P, Timmerman P, Janssen PA.

J Med Chem. 2005 Mar 24;48(6):2072-9.

PMID:
15771449
30.

Design of HIV-1 protease inhibitors active on multidrug-resistant virus.

Surleraux DL, de Kock HA, Verschueren WG, Pille GM, Maes LJ, Peeters A, Vendeville S, De Meyer S, Azijn H, Pauwels R, de Bethune MP, King NM, Prabu-Jeyabalan M, Schiffer CA, Wigerinck PB.

J Med Chem. 2005 Mar 24;48(6):1965-73.

PMID:
15771440
31.

4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.

Benjahad A, Croisy M, Monneret C, Bisagni E, Mabire D, Coupa S, Poncelet A, Csoka I, Guillemont J, Meyer C, Andries K, Pauwels R, de Béthune MP, Himmel DM, Das K, Arnold E, Nguyen CH, Grierson DS.

J Med Chem. 2005 Mar 24;48(6):1948-64.

PMID:
15771439
32.

Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.

Heeres J, de Jonge MR, Koymans LM, Daeyaert FF, Vinkers M, Van Aken KJ, Arnold E, Das K, Kilonda A, Hoornaert GJ, Compernolle F, Cegla M, Azzam RA, Andries K, de Béthune MP, Azijn H, Pauwels R, Lewi PJ, Janssen PA.

J Med Chem. 2005 Mar 24;48(6):1910-8.

PMID:
15771435
33.

In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).

Janssen PA, Lewi PJ, Arnold E, Daeyaert F, de Jonge M, Heeres J, Koymans L, Vinkers M, Guillemont J, Pasquier E, Kukla M, Ludovici D, Andries K, de Béthune MP, Pauwels R, Das K, Clark AD Jr, Frenkel YV, Hughes SH, Medaer B, De Knaep F, Bohets H, De Clerck F, Lampo A, Williams P, Stoffels P.

J Med Chem. 2005 Mar 24;48(6):1901-9. Review.

PMID:
15771434
34.

Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor.

Surleraux DL, Tahri A, Verschueren WG, Pille GM, de Kock HA, Jonckers TH, Peeters A, De Meyer S, Azijn H, Pauwels R, de Bethune MP, King NM, Prabu-Jeyabalan M, Schiffer CA, Wigerinck PB.

J Med Chem. 2005 Mar 24;48(6):1813-22.

PMID:
15771427
35.

TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1.

Andries K, Azijn H, Thielemans T, Ludovici D, Kukla M, Heeres J, Janssen P, De Corte B, Vingerhoets J, Pauwels R, de Béthune MP.

Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6.

36.

4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.

Benjahad A, Courté K, Guillemont J, Mabire D, Coupa S, Poncelet A, Csoka I, Andries K, Pauwels R, de Béthune MP, Monneret C, Bisagni E, Nguyen CH, Grierson DS.

J Med Chem. 2004 Oct 21;47(22):5501-14.

PMID:
15481987
37.

Structural and thermodynamic basis for the binding of TMC114, a next-generation human immunodeficiency virus type 1 protease inhibitor.

King NM, Prabu-Jeyabalan M, Nalivaika EA, Wigerinck P, de Béthune MP, Schiffer CA.

J Virol. 2004 Nov;78(21):12012-21.

38.

Correlations between factors determining the pharmacokinetics and antiviral activity of HIV-1 non-nucleoside reverse transcriptase inhibitors of the diaryltriazine and diarylpyrimidine classes of compounds.

Lewi P, Arnold E, Andries K, Bohets H, Borghys H, Clark A, Daeyaert F, Das K, de Béthune MP, de Jonge M, Heeres J, Koymans L, Leempoels J, Peeters J, Timmerman P, Van den Broeck W, Vanhoutte F, Van't Klooster G, Vinkers M, Volovik Y, Janssen PA.

Drugs R D. 2004;5(5):245-57.

PMID:
15357624
39.

Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants.

Das K, Clark AD Jr, Lewi PJ, Heeres J, De Jonge MR, Koymans LM, Vinkers HM, Daeyaert F, Ludovici DW, Kukla MJ, De Corte B, Kavash RW, Ho CY, Ye H, Lichtenstein MA, Andries K, Pauwels R, De Béthune MP, Boyer PL, Clark P, Hughes SH, Janssen PA, Arnold E.

J Med Chem. 2004 May 6;47(10):2550-60.

PMID:
15115397
40.

On the detection of multiple-binding modes of ligands to proteins, from biological, structural, and modeling data.

Lewi PJ, de Jonge M, Daeyaert F, Koymans L, Vinkers M, Heeres J, Janssen PA, Arnold E, Das K, Clark AD Jr, Hughes SH, Boyer PL, de Béthune MP, Pauwels R, Andries K, Kukla M, Ludovici D, De Corte B, Kavash R, Ho C.

J Comput Aided Mol Des. 2003 Feb-Apr;17(2-4):129-34. Erratum in: J Comput Aided Mol Des. 2003 May-Jun;17(5-6):398. Lewis PJ [corrected to Lewi PJ].

PMID:
13677481
41.

Replication-deficient human adenovirus type 35 vectors for gene transfer and vaccination: efficient human cell infection and bypass of preexisting adenovirus immunity.

Vogels R, Zuijdgeest D, van Rijnsoever R, Hartkoorn E, Damen I, de Béthune MP, Kostense S, Penders G, Helmus N, Koudstaal W, Cecchini M, Wetterwald A, Sprangers M, Lemckert A, Ophorst O, Koel B, van Meerendonk M, Quax P, Panitti L, Grimbergen J, Bout A, Goudsmit J, Havenga M.

J Virol. 2003 Aug;77(15):8263-71.

42.

Inhibition of vaginal transmission of HIV-1 in hu-SCID mice by the non-nucleoside reverse transcriptase inhibitor TMC120 in a gel formulation.

Di Fabio S, Van Roey J, Giannini G, van den Mooter G, Spada M, Binelli A, Pirillo MF, Germinario E, Belardelli F, de Bethune MP, Vella S.

AIDS. 2003 Jul 25;17(11):1597-604.

PMID:
12853741
43.

Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.

Ludovici DW, De Corte BL, Kukla MJ, Ye H, Ho CY, Lichtenstein MA, Kavash RW, Andries K, de Béthune MP, Azijn H, Pauwels R, Lewi PJ, Heeres J, Koymans LM, de Jonge MR, Van Aken KJ, Daeyaert FF, Das K, Arnold E, Janssen PA.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2235-9.

PMID:
11527705
44.

Evolution of anti-HIV drug candidates. Part 2: Diaryltriazine (DATA) analogues.

Ludovici DW, Kavash RW, Kukla MJ, Ho CY, Ye H, De Corte BL, Andries K, de Béthune MP, Azijn H, Pauwels R, Moereels HE, Heeres J, Koymans LM, de Jonge MR, Van Aken KJ, Daeyaert FF, Lewi PJ, Das K, Arnold E, Janssen PA.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2229-34.

PMID:
11527704
45.

Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).

Ludovici DW, Kukla MJ, Grous PG, Krishnan S, Andries K, de Béthune MP, Azijn H, Pauwels R, De Clercq E, Arnold E, Janssen PA.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2225-8.

PMID:
11527703
46.

Charge modification of plasma and milk proteins results in antiviral active compounds.

Swart PJ, Harmsen MC, Kuipers ME, Van Dijk AA, Van Der Strate BW, Van Berkel PH, Nuijens JH, Smit C, Witvrouw M, De Clercq E, de Béthune MP, Pauwels R, Meijer DK.

J Pept Sci. 1999 Dec;5(12):563-76.

PMID:
10628656
47.

RT-PCR for Amplification of Specific Fragments of HIV-1 Genome.

de Béthune MP, Hertogs K.

Methods Mol Med. 2000;24:269-82. doi: 10.1385/1-59259-245-7:269.

PMID:
21331915
48.

Patterns of resistance and cross-resistance to human immunodeficiency virus type 1 reverse transcriptase inhibitors in patients treated with the nonnucleoside reverse transcriptase inhibitor loviride.

Miller V, de Béthune MP, Kober A, Stürmer M, Hertogs K, Pauwels R, Stoffels P, Staszewski S.

Antimicrob Agents Chemother. 1998 Dec;42(12):3123-9.

49.

The M184V mutation in HIV-1 reverse transcriptase (RT) conferring lamivudine resistance does not result in broad cross-resistance to nucleoside analogue RT inhibitors.

Miller V, Stürmer M, Staszewski S, Gröschel B, Hertogs K, de Béthune MP, Pauwels R, Harrigan PR, Bloor S, Kemp SD, Larder BA.

AIDS. 1998 May 7;12(7):705-12.

PMID:
9619801
50.

Dual resistance to zidovudine and lamivudine in patients treated with zidovudine-lamivudine combination therapy: association with therapy failure.

Miller V, Phillips A, Rottmann C, Staszewski S, Pauwels R, Hertogs K, de Béthune MP, Kemp SD, Bloor S, Harrigan PR, Larder BA.

J Infect Dis. 1998 Jun;177(6):1521-32.

PMID:
9607829

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