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Janssen PA

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Publications:

Title Authors Year Journal
On the detection of multiple-binding modes of ligands to proteins, from biological, structural, and modeling data. Janssen PA Journal of computer-aided molecular design
Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability. Janssen PA 2005 J Med Chem
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. Janssen PA 2005 Journal of medicinal chemistry
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 2005 J Med Chem
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. Janssen PA 2005 Journal of medicinal chemistry
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. Janssen PA 2004 J Med Chem
TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Janssen PA 2004 Antimicrob Agents Chemother
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. Janssen PA 2004 Drugs in R&D
The Lys103Asn mutation of HIV-1 RT: a novel mechanism of drug resistance. Janssen PA 2001 Journal of molecular biology
Evolution of anti-HIV drug candidates. Part 2: Diaryltriazine (DATA) analogues. Janssen PA 2001 Bioorganic & medicinal chemistry letters
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). Janssen PA 2001 Bioorganic & medicinal chemistry letters
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. Janssen PA 2001 Bioorganic & medicinal chemistry letters
Molecular modeling of HIV-1 reverse transcriptase drug-resistant mutant strains: implications for the mechanism of polymerase action. Janssen PA 1997 Protein engineering
Evaluation of the efficacy and tolerance of R 018893, R 089439 (loviride) and placebo in asymptomatic HIV-1-infected patients. Loviride Collaborative Study Group. Janssen PA 1996 Antiviral therapy
Crystal structures of 8-Cl and 9-Cl TIBO complexed with wild-type HIV-1 RT and 8-Cl TIBO complexed with the Tyr181Cys HIV-1 RT drug-resistant mutant. Janssen PA 1996 Journal of molecular biology
Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors. Janssen PA 1995 Nat Struct Biol
Molecular modeling studies of HIV-1 reverse transcriptase nonnucleoside inhibitors: total energy of complexation as a predictor of drug placement and activity. Janssen PA 1995 Protein science : a publication of the Protein Society
Locations of anti-AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase. Implications for mechanisms of drug inhibition and resistance. Janssen PA 1994 Journal of molecular biology
Allosteric inhibition of human immunodeficiency virus type 1 reverse transcriptase by tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione compounds. Janssen PA 1992 Molecular pharmacology
An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives. Janssen PA 1991 Proceedings of the National Academy of Sciences of the United States of America

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