Search Results - "KAWAI, Stephen"

Distinct Effects of Two HIV-1 Capsid Assembly Inhibitor Families That Bind the Same Site within the N-Terminal Domain of the Viral CA Protein by LEMKE, Christopher T, TITOLO, Steve, GAGNON, Alexandre, KAWAI, Stephen H, RANCOURT, Jean, TREMBLAY, Martin, YOAKIM, Christiane, SIMONEAU, Bruno, ARCHAMBAULT, Jacques, SUNDQUIST, Wesley I, MASON, Stephen W, VON SCHWEDLER, Uta, GOUDREAU, Nathalie, MERCIER, Jean-François, WARDROP, Elizabeth, FAUCHER, Anne-Marie, COULOMBE, Rene, BANIK, Soma S. R, FADER, Lee

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Ligand Bioactive Conformation Plays a Critical Role in the Design of Drugs That Target the Hepatitis C Virus NS3 Protease by LaPlante, Steven R., Nar, Herbert, Lemke, Christopher T., Jakalian, Araz, Aubry, Norman, Kawai, Stephen H.

“…A ligand-focused strategy employed NMR, X-ray, modeling, and medicinal chemistry to expose the critical role that bioactive conformation played in the design…”
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Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV‑1 by Fader, Lee D, Malenfant, Eric, Parisien, Mathieu, Carson, Rebekah, Bilodeau, François, Landry, Serge, Pesant, Marc, Brochu, Christian, Morin, Sébastien, Chabot, Catherine, Halmos, Ted, Bousquet, Yves, Bailey, Murray D, Kawai, Stephen H, Coulombe, René, LaPlante, Steven, Jakalian, Araz, Bhardwaj, Punit K, Wernic, Dominik, Schroeder, Patricia, Amad, Ma’an, Edwards, Paul, Garneau, Michel, Duan, Jianmin, Cordingley, Michael, Bethell, Richard, Mason, Stephen W, Bös, Michael, Bonneau, Pierre, Poupart, Marc-André, Faucher, Anne-Marie, Simoneau, Bruno, Fenwick, Craig, Yoakim, Christiane, Tsantrizos, Youla

“…An assay recapitulating the 3′ processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection. Hit-to-lead and…”
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Preclinical Profile of BI 224436, a Novel HIV-1 Non-Catalytic-Site Integrase Inhibitor by FENWICK, Craig, AMAD, Ma'an, FADER, Lee D, FAUCHER, Anne-Marie, GARNEAU, Michel, JAKALIAN, Araz, KAWAI, Stephen, LAMORTE, Louie, LAPLANTE, Steven, LAIBIN LUO, MASON, Steve, POUPART, Marc-André, BAILEY, Murray D, RIOUX, Nathalie, SCHROEDER, Patricia, SIMONEAU, Bruno, TREMBLAY, Sonia, TSANTRIZOS, Youla, WITVROUW, Myriam, YOAKIM, Christiane, BETHELL, Richard, BÖS, Michael, BONNEAU, Pierre, CORDINGLEY, Michael, COULOMBE, René, DUAN, Jianmin, EDWARDS, Paul

“…BI 224436 is an HIV-1 integrase inhibitor with effective antiviral activity that acts through a mechanism that is distinct from that of integrase strand…”
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Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly by Fader, Lee D., Bethell, Richard, Bonneau, Pierre, Bös, Michael, Bousquet, Yves, Cordingley, Michael G., Coulombe, René, Deroy, Patrick, Faucher, Anne-Marie, Gagnon, Alexandre, Goudreau, Nathalie, Grand-Maître, Chantal, Guse, Ingrid, Hucke, Oliver, Kawai, Stephen H., Lacoste, Jean-Eric, Landry, Serge, Lemke, Christopher T., Malenfant, Eric, Mason, Stephen, Morin, Sébastien, O’Meara, Jeff, Simoneau, Bruno, Titolo, Steve, Yoakim, Christiane

“…The discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly is described. Synthesis of analogs of the…”
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An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus by Lamarre, Daniel, Anderson, Paul C, Bailey, Murray, Beaulieu, Pierre, Bolger, Gordon, Bonneau, Pierre, Bös, Michael, Cameron, Dale R, Cartier, Mireille, Cordingley, Michael G, Faucher, Anne-Marie, Goudreau, Nathalie, Kawai, Stephen H, Kukolj, George, Lagacé, Lisette, LaPlante, Steven R, Narjes, Hans, Poupart, Marc-André, Rancourt, Jean, Sentjens, Roel E, St George, Roger, Simoneau, Bruno, Steinmann, Gerhard, Thibeault, Diane, Tsantrizos, Youla S, Weldon, Steven M, Yong, Chan-Loi, Llinàs-Brunet, Montse

“…Hepatitis C virus (HCV) infection is a serious cause of chronic liver disease worldwide with more than 170 million infected individuals at risk of developing…”
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Discovery of a Potent and Selective Noncovalent Linear Inhibitor of the Hepatitis C Virus NS3 Protease (BI 201335) by Llinàs-Brunet, Montse, Bailey, Murray D, Goudreau, Nathalie, Bhardwaj, Punit K, Bordeleau, Josée, Bös, Michael, Bousquet, Yves, Cordingley, Michael G, Duan, Jiamin, Forgione, Pat, Garneau, Michel, Ghiro, Elise, Gorys, Vida, Goulet, Sylvie, Halmos, Ted, Kawai, Stephen H, Naud, Julie, Poupart, Marc-André, White, Peter W

“…C-Terminal carboxylic acid containing inhibitors of the NS3 protease are reported. A novel series of linear tripeptide inhibitors that are very potent and…”
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Inhibition of HIV-1 capsid assembly: Optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold by Tremblay, Martin, Bonneau, Pierre, Bousquet, Yves, DeRoy, Patrick, Duan, Jianmin, Duplessis, Martin, Gagnon, Alexandre, Garneau, Michel, Goudreau, Nathalie, Guse, Ingrid, Hucke, Oliver, Kawai, Stephen H., Lemke, Christopher T., Mason, Stephen W., Simoneau, Bruno, Surprenant, Simon, Titolo, Steve, Yoakim, Christiane

“…A uHTS campaign led to the discovery of a 5-(5-furan-2-ylpyrazol-1-yl)-1H-benzimidazole series that inhibits assembly of HIV-1 capsid. Synthetic manipulations…”
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Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 1: Addressing configurational instability through scaffold modification by Fader, Lee D., Landry, Serge, Morin, Sébastien, Kawai, Stephen H., Bousquet, Yves, Hucke, Oliver, Goudreau, Nathalie, Lemke, Christopher T., Bonneau, Pierre, Titolo, Steve, Mason, Stephen, Simoneau, Bruno

“…The optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly that possess a labile stereocenter at C3 is…”
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Mobiles, Molecules and the Coalescence of Processes by Kawai, Stephen H.

“…The author provides an account of his development and experiences as both a visual (mobile) artist and a chemist. He describes the surprising similarities…”
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Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 2: Structure–activity relationships (SAR) of the C3-phenyl moiety by Fader, Lee D., Landry, Serge, Goulet, Sylvie, Morin, Sébastien, Kawai, Stephen H., Bousquet, Yves, Dion, Isabelle, Hucke, Oliver, Goudreau, Nathalie, Lemke, Christopher T., Rancourt, Jean, Bonneau, Pierre, Titolo, Steve, Amad, Ma’an, Garneau, Michel, Duan, Jianmin, Mason, Stephen, Simoneau, Bruno

“…Detailed structure–activity relationships of the C3-phenyl moiety that allow for the optimization of antiviral potency of a series of…”
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Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs by Fader, Lee D, Bailey, Murray, Beaulieu, Eric, Bilodeau, François, Bonneau, Pierre, Bousquet, Yves, Carson, Rebekah J, Chabot, Catherine, Coulombe, René, Duan, Jianmin, Fenwick, Craig, Garneau, Michel, Halmos, Ted, Jakalian, Araz, James, Clint, Kawai, Stephen H, Landry, Serge, LaPlante, Steven R, Mason, Stephen W, Morin, Sebastien, Rioux, Nathalie, Simoneau, Bruno, Surprenant, Simon, Thavonekham, Bounkham, Thibeault, Carl, Trinh, Thao, Tsantrizos, Youla, Tsoung, Jennifer, Yoakim, Christiane, Wernic, Dominik

“…Optimization of pyridine-based noncatalytic site integrase inhibitors (NCINIs) based on compound 2 has led to the discovery of molecules capable of inhibiting…”
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Synthesis of BILN 2061, an HCV NS3 Protease Inhibitor with Proven Antiviral Effect in Humans by Faucher, Anne-Marie, Bailey, Murray D, Beaulieu, Pierre L, Brochu, Christian, Duceppe, Jean-Simon, Ferland, Jean-Marie, Ghiro, Elise, Gorys, Vida, Halmos, Ted, Kawai, Stephen H, Poirier, Martin, Simoneau, Bruno, Tsantrizos, Youla S, Llinàs-Brunet, Montse

“…The synthesis of BILN 2061, an NS3 protease inhibitor with proven antiviral effect in humans, was accomplished in a convergent manner from four building…”
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Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV by Fader, Lee D, Carson, Rebekah, Morin, Sébastien, Bilodeau, François, Chabot, Catherine, Halmos, Ted, Bailey, Murray D, Kawai, Stephen H, Coulombe, René, Laplante, Steven, Mekhssian, Kevork, Jakalian, Araz, Garneau, Michel, Duan, Jianmin, Mason, Stephen W, Simoneau, Bruno, Fenwick, Craig, Tsantrizos, Youla, Yoakim, Christiane

“…A scaffold replacement approach was used to identifying the pyridine series of noncatalytic site integrase inhibitors. These molecules bind with higher…”
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The Use of Chemical Double-Mutant Cycles in Biomolecular Recognition Studies: Application to HCV NS3 Protease Inhibitors by Kawai, Stephen H., Bailey, Murray D., Halmos, Ted, Forgione, Pat, LaPlante, Steven R., Llinàs-Brunet, Montse, Naud, Julie, Goudreau, Natalie

“…Things don′t always add up: Our understanding of biomolecular recognition processes is often complicated by the fact that the binding contributions of…”
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The effect of the P1 side chain on the binding of optimized carboxylate and activated carbonyl inhibitors of the hepatitis C virus NS3 protease by Kawai, Stephen H, LaPlante, Steven R, Llinàs-Brunet, Montse, Hucke, Oliver

“…Peptidyl inhibitors of the hepatitis C virus NS3 protease hold much promise as direct-acting antiviral agents against hepatitis C infection. The optimization…”
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Dimethylthiazolidine Carboxylic Acid as a Rigid P3 Unit in Inhibitors of Serine Proteases: Application to Two Targets by Kawai, Stephen H., Aubry, Norman, Duceppe, Jean-Simon, Llinàs-Brunet, Montse, LaPlante, Steven R.

“…Serine proteases are a very large class of enzymes, many of which represent important targets for therapeutic agents against a wide variety of disease states…”
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Characterization of the Human Cytomegalovirus Protease As an Induced-Fit Serine Protease and the Implications to the Design of Mechanism-Based Inhibitors by LaPlante, Steven R, Bonneau, Pierre R, Aubry, Norman, Cameron, Dale R, Déziel, Robert, Grand-Maître, Chantal, Plouffe, Céline, Tong, Liang, Kawai, Stephen H

“…The conformational properties of the N-tert-butylacetyl-l-tert-butylglycyl-l-N δ,N δ-dimethylasparagyl-l-alanyl methyl ketone (MK) 1 and its terminal…”
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Evidence of a Conformational Change in the Human Cytomegalovirus Protease upon Binding of Peptidyl-Activated Carbonyl Inhibitors by Bonneau, Pierre R, Grand-Maître, Chantal, Greenwood, Daniel J, Lagacé, Lisette, LaPlante, Steven R, Massariol, Marie-Josée, Ogilvie, William W, O'Meara, Jeff A, Kawai, Stephen H

“…A series of N-tert-butylacetyl-l-tert-butylglycyl-l-N γ,N γ-dimethylasparagyl-l-alanyl-derived inhibitors (trifluoromethyl ketone 1, pentafluoroethyl ketone,…”
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Human Cytomegalovirus Protease Complexes Its Substrate Recognition Sequences in an Extended Peptide Conformation by LaPlante, Steven R, Aubry, Norman, Bonneau, Pierre R, Cameron, Dale R, Lagacé, Lisette, Massariol, Marie-Josée, Montpetit, Hélène, Plouffe, Céline, Kawai, Stephen H, Fulton, Bruce D, Chen, Zhigang, Ni, Feng

“…Substrate hydrolysis by human cytomegalovirus (HCMV) protease is essential to viral capsid assembly. The interaction of HCMV protease and the N-terminal…”
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