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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
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
Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability. 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
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
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
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
The Lys103Asn mutation of HIV-1 RT: a novel mechanism of drug resistance. Janssen PA 2001 Journal of molecular biology
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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