Search Results - "AUBRY, Norman"

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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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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Solution Structure of Substrate-based Ligands When Bound to Hepatitis C Virus NS3 Protease Domain by LaPlante, S R, Cameron, D R, Aubry, N, Lefebvre, S, Kukolj, G, Maurice, R, Thibeault, D, Lamarre, D, Llinàs-Brunet, M

“…The interactions of the NS3 protease domain with inhibitors that are based on N-terminal cleavage products of peptide substrates were studied by NMR methods…”
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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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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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Determining the Predominant Conformations of Mortiamides A–D in Solution Using NMR Data and Molecular Modeling Tools by Franca, Tanos C. C., Goncalves, Arlan da Silva, Bérubé, Christopher, Voyer, Normand, Aubry, Norman, LaPlante, Steven R.

“…Macrocyclic peptidomimetics have been seriously contributing to our arsenal of drugs to combat diseases. The search for nature’s discoveries led us to…”
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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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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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RCM of Tripeptide Dienes Containing a Chiral Vinylcyclopropane Moiety:  Impact of Different Ru-Based Catalysts on the Stereochemical Integrity of the Macrocyclic Products by Poirier, Martin, Aubry, Norman, Boucher, Colette, Ferland, Jean-Marie, LaPlante, Steve, Tsantrizos, Youla S

“…Tripeptide dienes containing an (1R,2S)-vinyl aminocyclopropylcarboxylate residue were cyclized to β-strand scaffolds under ring-closing metathesis (RCM)…”
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Binding Mode Determination of Benzimidazole Inhibitors of the Hepatitis C Virus RNA Polymerase by a Structure and Dynamics Strategy by LaPlante, Steven R., Jakalian, Araz, Aubry, Norman, Bousquet, Yves, Ferland, Jean-Marie, Gillard, James, Lefebvre, Sylvain, Poirier, Martin, Tsantrizos, Youla S., Kukolj, George, Beaulieu, Pierre L.

“…A novel strategy involving NMR, medicinal chemistry, and molecular modeling is described for determining the binding mode of ligands and the binding roles of…”
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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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Quantifying trifluoroacetic acid as a counterion in drug discovery by 19F NMR and capillary electrophoresis by Little, Michael J., Aubry, Norman, Beaudoin, Marie-Eve, Goudreau, Nathalie, LaPlante, Steven R.

“…Drug discovery compounds are often isolated as salts of trifluoroacetate from preparative high performance liquid chromatography, which are then used for…”
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RCM of tripeptide dienes containing a chiral vinylcyclopropane moiety : Impact of different ru-based catalysts on the stereochemical integrity of themacrocyclic products by POIRIER, Martin, AUBRY, Norman, BOUCHER, Colette, FERLAND, Jean-Marie, LAPLANTE, Steve, TSANTRIZOS, Youla S

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NMR line-broadening and transferred NOESY as a medicinal chemistry tool for studying inhibitors of the hepatitis C virus NS3 protease domain by LaPlante, Steven R, Aubry, Norman, Bonneau, Pierre R, Kukolj, George, Lamarre, Daniel, Lefebvre, Sylvain, Li, Hong, Llinàs-Brunet, Montse, Plouffe, Céline, Cameron, Dale R

“…This work describes the use of NMR as a medicinal chemistry tool for better understanding the binding characteristics of inhibitors of the HCV NS3 protease…”
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Transferred 13C T1 Relaxation at Natural Isotopic Abundance:  A Practical Method for Determining Site-Specific Changes in Ligand Flexibility upon Binding to a Macromolecule by LAPLANTE, Steven R., AUBRY, Norman, DéZIEL, Robert, NI, Feng, XU, Ping

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Transferred 13 C T 1 Relaxation at Natural Isotopic Abundance:  A Practical Method for Determining Site-Specific Changes in Ligand Flexibility upon Binding to a Macromolecule by LaPlante, Steven R., Aubry, Norman, Déziel, Robert, Ni, Feng, Xu, Ping

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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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The Conformation of a Peptidyl Methyl Ketone Inhibitor Bound to the Human Cytomegalovirus Protease by LaPlante, Steven R., Cameron, Dale R., Aubry, Norman, Bonneau, Pierre R., Déziel, Robert, Grand-Maître, Chantal, Ogilvie, William W., Kawai, Stephen H.

“…A weak inhibitor means faster exchange! Since the methyl ketone MK2 is a weak noncovalent peptidyl inhibitor of the human cytomegalovirus protease, exchange…”
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Binding Mode Determination of Benzimidazole Inhibitors of the Hepatitis C Virus RNA Polymerase by a Structure and Dynamics Strategy by LaPlante, Steven R., Jakalian, Araz, Aubry, Norman, Bousquet, Yves, Ferland, Jean-Marie, Gillard, James, Lefebvre, Sylvain, Poirier, Martin, Tsantrizos, Youla S., Kukolj, George, Beaulieu, Pierre L.

“…Eine neuartige Strategie, die NMR‐Spektroskopie, medizinische Chemie und Molecular Modeling umfasst, diente zur Bestimmung der Bindungsweise von Liganden und…”
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Transferred 13C T 1 Relaxation at Natural Isotopic Abundance:  A Practical Method for Determining Site-Specific Changes in Ligand Flexibility upon Binding to a Macromolecule by LaPlante, Steven R, Aubry, Norman, Déziel, Robert, Ni, Feng, Xu, Ping

“…An NMR strategy is described for measuring changes in 13C spin−lattice relaxation times (T 1) of ligand molecules, at natural isotopic abundance, upon binding…”
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