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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
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
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, 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
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
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
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. 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
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
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 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
Characterization of HIV-1 strains isolated from patients treated with TIBO R82913. Pauwels R 1994 AIDS research and human retroviruses
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
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
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
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
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
Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. Pauwels R 1989 Biochemical and biophysical research communications
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
Selective activity of several cholic acid derivatives against human immunodeficiency virus replication in vitro. Pauwels R 1989 Journal of acquired immune deficiency syndromes
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
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
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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