Research Topics
| Peter W WhiteSummaryAffiliation: Boehringer Ingelheim Publications
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Detail Information
Publications
Small molecule inhibitors of the human papillomavirus E1-E2 interactionPeter W White
Boehringer Ingelheim Ltd, Canada
Curr Top Microbiol Immunol 348:61-88. 2011..Binding modes for the two series are compared, and some general conclusions about the discovery of protein-protein interaction inhibitors are drawn from the work described...- Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A proteasePeter W White
Boehringer Ingelheim Canada Ltd, 2100 Cunard St, Laval, QC, Canada
Antimicrob Agents Chemother 54:4611-8. 2010..BI 201335 is a highly potent and selective NS3-NS4A protease inhibitor with good in vitro and animal ADME properties, consistent with its good human PK profile, and shows great promise as a treatment for HCV infection... - Protease and helicase activities of hepatitis C virus genotype 4, 5, and 6 NS3-NS4A proteinsMarie Josée Massariol
Boehringer Ingelheim Canada Ltd, Department of Biological Sciences, 2100 Cunard St, Laval, QC, Canada
Biochem Biophys Res Commun 391:692-7. 2010..With the availability of these proteins, inhibitors developed based on their activity against genotype 1 can be tested against all the other major genotypes, providing a path to improved treatment for all HCV patients... - Use of the fused NS4A peptide-NS3 protease domain to study the importance of the helicase domain for protease inhibitor binding to hepatitis C virus NS3-NS4ADiane Thibeault
Boehringer Ingelheim Canada Ltd, 2100 Cunard Street, Laval, QC, Canada H7S 2G5
Biochemistry 48:744-53. 2009..Thus, the protease domain with the NS4A peptide, in a covalent or noncovalent complex, is a good model for the protease activity of native NS3-NS4A... - Combined X-ray, NMR, and kinetic analyses reveal uncommon binding characteristics of the hepatitis C virus NS3-NS4A protease inhibitor BI 201335Christopher T Lemke
Boehringer Ingelheim Canada Ltd, Research and Development, Laval, Quebec, Canada
J Biol Chem 286:11434-43. 2011.... - Biphenylsulfonacetic acid inhibitors of the human papillomavirus type 6 E1 helicase inhibit ATP hydrolysis by an allosteric mechanism involving tyrosine 486Peter W White
Department of Biological Sciences, Boehringer Ingelheim Canada Ltd, 2100 Cunard St, Laval, Quebec, Canada H7S 2G5
Antimicrob Agents Chemother 49:4834-42. 2005..These studies implicate Tyr-486 as a key residue for inhibitor binding and define an allosteric pocket on HPV E1 that can be exploited for future drug discovery efforts... - Optimization and determination of the absolute configuration of a series of potent inhibitors of human papillomavirus type-11 E1-E2 protein-protein interaction: a combined medicinal chemistry, NMR and computational chemistry approachNathalie Goudreau
Department of Chemistry, Boehringer Ingelheim Canada Ltd, Research and Development, 2100 Cunard Street, Laval, Que, Canada H7S 2G5
Bioorg Med Chem 15:2690-700. 2007..In addition, we report a combined NMR and computational chemistry approach which allowed the successful determination of the absolute stereochemistry of the active species originating from the initial racemic lead... - Inhibition of human papillomavirus DNA replication by small molecule antagonists of the E1-E2 protein interactionPeter W White
Department of Biological Sciences and the Department of Chemistry, Boehringer Ingelheim Ltd, Laval H7S 2G5, Canada
J Biol Chem 278:26765-72. 2003..These results highlight the potential of the E1-E2 interaction as a small molecule antiviral target... - Sensitivity of NS3 serine proteases from hepatitis C virus genotypes 2 and 3 to the inhibitor BILN 2061Diane Thibeault
Department of Biological Sciences, Boehringer Ingelheim Canada Ltd, Research and Development, Laval, Quebec H7S 2G5, Canada
J Virol 78:7352-9. 2004..This in vitro potency, in conjunction with the good pharmacokinetic data reported for humans, suggests that there is potential for BILN 2061 as an antiviral agent for individuals infected with non-genotype-1 HCV... - Discovery of the first series of inhibitors of human papillomavirus type 11: inhibition of the assembly of the E1-E2-Origin DNA complexChristiane Yoakim
Department of Chemistry, Boehringer Ingelheim Canada Ltd, 2100 Cunard Street, Laval, Quebec, Canada H7S 2G5
Bioorg Med Chem Lett 13:2539-41. 2003..We have discovered a series of inhibitors of the assembly of the HPV11 E1-E2-origin DNA complex, which incorporate an indandione fused to a substituted tetrahydrofuran... - Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335)Montse Llinas-Brunet
Department of Medicinal Chemistry, Boehringer Ingelheim Canada Ltd, 2100 Cunard Street, Laval, Quebec H7S 2G5, Canada
J Med Chem 53:6466-76. 2010..Structure-activity studies on the C8-bromo derivatives ultimately led to the discovery of clinical candidate 29 (BI 201335), a very potent and selective inhibitor of genotype1 NS3 protease with a promising PK profile in rats... - In vitro resistance profile of the hepatitis C virus NS3 protease inhibitor BI 201335Lisette Lagacé
Boehringer Ingelheim Canada Ltd, Laval, Quebec, Canada H7S2G5
Antimicrob Agents Chemother 56:569-72. 2012..In contrast to macrocyclic and covalent protease inhibitors, changes at V36, T54, F43, and Q80 did not confer resistance to BI 201335... - Blunting the Swiss army knife of hepatitis C virus: inhibitors of NS3/4A proteasePeter W White
Boehringer Ingelheim (Canada) Ltd, Laval, Canada
Prog Med Chem 44:65-107. 2006 - Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicaseAnne Marie Faucher
Boehringer Ingelheim Canada Ltd, Research and Development, 2100 Cunard Street, Laval Quebec, Canada, H7S 2G5
J Med Chem 47:18-21. 2004..A hit-to-lead exercise rapidly converted 1 into a low nanomolar lead series... - Cross-species absorption, metabolism, distribution and pharmacokinetics of BI 201335, a potent HCV genotype 1 NS3/4A protease inhibitorJianmin Duan
Department of Biological Sciences, Research and Development, Boehringer Ingelheim Canada Ltd, Laval, Quebec, Canada
Xenobiotica 42:164-72. 2012..The averaged Vss/F from all tested preclinical animals provided the best prediction of human Vss and the resulting "effective" t(1/2)... - Development and validation of a high-throughput screening assay for the hepatitis C virus p7 viroporinChristian Gervais
Department of Biological Sciences, Research and Development, Boehringer Ingelheim Canada Ltd, Laval, QC, Canada
J Biomol Screen 16:363-9. 2011..The p7 liposome-based assay displayed robust statistics (Z' > 0.75), and sensitivity to inhibition was confirmed using known inhibitors... - An ATPase assay using scintillation proximity beads for high-throughput screening or kinetic analysisJamie A Jeffery
Department of Biological Sciences, Boehringer Ingelheim (Canada) Ltd, 2100 Cunard St, Laval, Quebec, H7S 2G5, Canada
Anal Biochem 304:55-62. 2002....