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Pauwels R

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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. Pauwels R Journal of computer-aided molecular design
Discovery, development and characterization of agents active against the AIDS virus. Pauwels R Journal of receptor and signal transduction research
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). Pauwels R 2005 J Med Chem
TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. Pauwels R 2005 Journal of virology
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. Pauwels R 2005 Journal of medicinal chemistry
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. Pauwels R 2005 Journal of medicinal chemistry
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. Pauwels R 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. Pauwels R 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. Pauwels R 2004 Antimicrob Agents Chemother
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. Pauwels R 2001 Bioorganic & medicinal chemistry letters
Evolution of anti-HIV drug candidates. Part 2: Diaryltriazine (DATA) analogues. Pauwels R 2001 Bioorganic & medicinal chemistry letters
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). Pauwels R 2001 Bioorganic & medicinal chemistry letters
A family of insertion mutations between codons 67 and 70 of human immunodeficiency virus type 1 reverse transcriptase confer multinucleoside analog resistance. Pauwels R 1999 Antimicrob Agents Chemother
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. Pauwels R 1996 Journal of molecular biology
Development of vaginal microbicides for the prevention of heterosexual transmission of HIV. Pauwels R 1996 Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association
Betulinic acid derivatives: a new class of specific inhibitors of human immunodeficiency virus type 1 entry. Pauwels R 1996 Journal of medicinal chemistry
New arylpyrido-diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase. Pauwels R 1996 Antiviral research
Betulinic acid derivatives: a new class of human immunodeficiency virus type 1 specific inhibitors with a new mode of action. Pauwels R 1996 Journal of medicinal chemistry
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. Pauwels R 1994 Journal of molecular biology
Characterization of HIV-1 strains isolated from patients treated with TIBO R82913. Pauwels R 1994 AIDS research and human retroviruses
New tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione derivatives are potent inhibitors of human immunodeficiency virus type 1 replication and are synergistic with 2',3'-dideoxynucleoside analogs. Pauwels R 1994 Antimicrobial agents and chemotherapy
Kinetics of different human immunodeficiency virus type 1 reverse transcriptases resistant to human immunodeficiency virus type 1-specific reverse transcriptase inhibitors. Pauwels R 1993 Molecular pharmacology
Common features in the interaction of tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives with the human immunodeficiency virus type 1 reverse transcriptase. Pauwels R 1992 Molecular pharmacology
Specific HIV-1 reverse transcriptase inhibitors. Pauwels R 1992 Journal of enzyme inhibition
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. Pauwels R 1992 Molecular pharmacology
Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents. Pauwels R 1992 Molecular pharmacology
Kinetics of inhibition of endogenous human immunodeficiency virus type 1 reverse transcription by 2',3'-dideoxynucleoside 5'-triphosphate, tetrahydroimidazo-[4,5,1-jk][1,4]-benzodiazepin-2(1H)-thion e, and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives. Pauwels R 1992 The Journal of biological chemistry
Resistance of human immunodeficiency virus type 1 reverse transcriptase to TIBO derivatives induced by site-directed mutagenesis. Pauwels R 1992 Virology
Differential inhibitory effects of TIBO derivatives on different strains of simian immunodeficiency virus. Pauwels R 1992 The Journal of general virology
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. Pauwels R 1991 Proceedings of the National Academy of Sciences of the United States of America
Flow cytometric method to demonstrate whether anti-HIV-1 agents inhibit virion binding to T4+ cells. Pauwels R 1989 Journal of acquired immune deficiency syndromes
Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. Pauwels R 1989 Biochemical and biophysical research communications
Selective activity of several cholic acid derivatives against human immunodeficiency virus replication in vitro. Pauwels R 1989 Journal of acquired immune deficiency syndromes
Fuchsin acid selectively inhibits human immunodeficiency virus (HIV) replication in vitro. Pauwels R 1988 Biochemical and biophysical research communications
Alpha, beta- and beta, gamma-methylene 5'-phosphonate derivatives of 3'-azido-2',3'-dideoxythymidine-5'-triphosphate. Correlation between affinity for reverse transcriptase, susceptibility to hydrolysis by phosphodiesterases and anti-retrovirus activity. Pauwels R 1988 Biochemical pharmacology
Mechanism of inhibitory effect of dextran sulfate and heparin on replication of human immunodeficiency virus in vitro. Pauwels R 1988 Proceedings of the National Academy of Sciences of the United States of America
Inhibitory effect of glycyrrhizin on the in vitro infectivity and cytopathic activity of the human immunodeficiency virus [HIV (HTLV-III/LAV)]. Pauwels R 1987 Antiviral research
Glycosylation inhibitors block the expression of LAV/HTLV-III (HIV) glycoproteins. Pauwels R 1986 Biochemical and biophysical research communications
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