Search Results - "COULOMBE, René"

Oxygen Access to the Active Site of Cholesterol Oxidase through a Narrow Channel Is Gated by an Arg-Glu Pair by Coulombe, R, Yue, K Q, Ghisla, S, Vrielink, A

“…Cholesterol oxidase is a monomeric flavoenzyme that catalyzes the oxidation and isomerization of cholesterol to cholest-4-en-3-one. Two forms of the enzyme are…”
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Compound Aggregation in Drug Discovery: Implementing a Practical NMR Assay for Medicinal Chemists by LaPlante, Steven R, Carson, Rebekah, Gillard, James, Aubry, Norman, Coulombe, René, Bordeleau, Sylvain, Bonneau, Pierre, Little, Michael, O’Meara, Jeff, Beaulieu, Pierre L

“…The pharmaceutical industry has recognized that many drug-like molecules can self-aggregate in aqueous media and have physicochemical properties that skew…”
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Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X‑Ray Cocrystallography by Smith, Christopher R., Chen, Dan, Christensen, James G., Coulombe, René, Féthière, James, Gunn, Robin J., Hollander, Johan, Jones, Benjamin, Ketcham, John M., Khare, Shilpi, Kuehler, Jon, Lawson, J. David, Marx, Matthew A., Olson, Peter, Pearson, Kelly E., Ren, Cynthia, Tsagris, Denise, Ulaganathan, Thirumalaiselvi, Van’t Veer, Inge, Wang, Xiaolun, Ivetac, Anthony

“…SOS1 and SOS2 are guanine nucleotide exchange factors that mediate RTK-stimulated RAS activation. Selective SOS1:KRAS PPI inhibitors are currently under…”
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Monitoring Drug Self-Aggregation and Potential for Promiscuity in Off-Target In Vitro Pharmacology Screens by a Practical NMR Strategy by LaPlante, Steven R, Aubry, Norman, Bolger, Gordon, Bonneau, Pierre, Carson, Rebekah, Coulombe, René, Sturino, Claudio, Beaulieu, Pierre L

“…A simple NMR assay was applied to monitor the tendency of compounds to self-aggregate in aqueous media. The observation of unusual spectral trends as a…”
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Enantiomeric Atropisomers Inhibit HCV Polymerase and/or HIV Matrix: Characterizing Hindered Bond Rotations and Target Selectivity by LaPlante, Steven R., Forgione, Pat, Boucher, Colette, Coulombe, René, Gillard, James, Hucke, Oliver, Jakalian, Araz, Joly, Marc-André, Kukolj, George, Lemke, Christopher, McCollum, Robert, Titolo, Steve, Beaulieu, Pierre L., Stammers, Timothy

“…An anthranilic acid series of allosteric thumb pocket 2 HCV NS5B polymerase inhibitors exhibited hindered rotation along a covalent bond axis, and the…”
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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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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

“…Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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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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Conformation-Based Restrictions and Scaffold Replacements in the Design of Hepatitis C Virus Polymerase Inhibitors: Discovery of Deleobuvir (BI 207127) by LaPlante, Steven R., Bös, Michael, Brochu, Christian, Chabot, Catherine, Coulombe, René, Gillard, James R., Jakalian, Araz, Poirier, Martin, Rancourt, Jean, Stammers, Timothy, Thavonekham, Bounkham, Beaulieu, Pierre L., Kukolj, George, Tsantrizos, Youla S.

“…Conformational restrictions of flexible torsion angles were used to guide the identification of new chemotypes of HCV NS5B inhibitors. Sites for rigidification…”
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Structure of rat procathepsin B: model for inhibition of cysteine protease activity by the proregion by Cygler, Miroslaw, Sivaraman, J, Grochulski, Pawel, Coulombe, René, Storer, Andrew C, Mort, John S

“…Background: Cysteine proteases of the papain superfamily are synthesized as inactive precursors with a 60–110 residue N-terminal prosegment. The propeptides…”
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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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Importance of Ligand Bioactive Conformation in the Discovery of Potent Indole-Diamide Inhibitors of the Hepatitis C Virus NS5B by LaPlante, Steven R, Gillard, James R, Jakalian, Araz, Aubry, Norman, Coulombe, René, Brochu, Christian, Tsantrizos, Youla S, Poirier, Martin, Kukolj, George, Beaulieu, Pierre L

“…Significant advances have led to receptor induced-fit and conformational selection models for describing bimolecular recognition, but a more comprehensive view…”
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Molecular Dynamics Simulations and Structure-Based Rational Design Lead to Allosteric HCV NS5B Polymerase Thumb Pocket 2 Inhibitor with Picomolar Cellular Replicon Potency by Hucke, Oliver, Coulombe, René, Bonneau, Pierre, Bertrand-Laperle, Mégan, Brochu, Christian, Gillard, James, Joly, Marc-André, Landry, Serge, Lepage, Olivier, Llinàs-Brunet, Montse, Pesant, Marc, Poirier, Martin, Poirier, Maude, McKercher, Ginette, Marquis, Martin, Kukolj, George, Beaulieu, Pierre L., Stammers, Timothy A.

“…The design and preliminary SAR of a new series of 1H-quinazolin-4-one (QAZ) allosteric HCV NS5B thumb pocket 2 (TP-2) inhibitors was recently reported. To…”
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Integrated Strategies for Identifying Leads That Target the NS3 Helicase of the Hepatitis C Virus by LaPlante, Steven R., Padyana, Anil K., Abeywardane, Asitha, Bonneau, Pierre, Cartier, Mireille, Coulombe, René, Jakalian, Araz, Wildeson-Jones, Jessi, Li, Xiang, Liang, Shuang, McKercher, Ginette, White, Peter, Zhang, Qiang, Taylor, Steven J.

“…Future treatments for individuals infected by the hepatitis C virus (HCV) will likely involve combinations of compounds that inhibit multiple viral targets…”
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Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases by Gagnon, Alexandre, Landry, Serge, Coulombe, René, Jakalian, Araz, Guse, Ingrid, Thavonekham, Bounkham, Bonneau, Pierre R., Yoakim, Christiane, Simoneau, Bruno

“…Different acyclic, cyclic and heterocyclic tetrazole replacements were investigated in order to evaluate the conformational and electronic contribution of the…”
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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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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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N- versus O-alkylation: Utilizing NMR methods to establish reliable primary structure determinations for drug discovery by LaPlante, Steven R., Bilodeau, François, Aubry, Norman, Gillard, James R., O’Meara, Jeff, Coulombe, René

“…A classic synthetic issue that remains unresolved is the reaction that involves the control of N- versus O-alkylation of ambident anions. This common chemical…”
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Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay by Stammers, Timothy A., Coulombe, René, Duplessis, Martin, Fazal, Gulrez, Gagnon, Alexandre, Garneau, Michel, Goulet, Sylvie, Jakalian, Araz, LaPlante, Steven, Rancourt, Jean, Thavonekham, Bounkham, Wernic, Dominik, Kukolj, George, Beaulieu, Pierre L.

“…Optimization efforts on the anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors 1 and 2 resulted in the identification of multiple structural…”
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Structure-based design of novel HCV NS5B thumb pocket 2 allosteric inhibitors with submicromolar gt1 replicon potency: Discovery of a quinazolinone chemotype by Beaulieu, Pierre L., Coulombe, René, Duan, Jianmin, Fazal, Gulrez, Godbout, Cédrickx, Hucke, Oliver, Jakalian, Araz, Joly, Marc-André, Lepage, Olivier, Llinàs-Brunet, Montse, Naud, Julie, Poirier, Martin, Rioux, Nathalie, Thavonekham, Bounkham, Kukolj, George, Stammers, Timothy A.

“…We describe the structure-based design of a novel lead chemotype that binds to thumb pocket 2 of HCV NS5B polymerase and inhibits cell-based gt1 subgenomic…”
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