Search Results - "LAPLANTE, Steven"

Challenge of Atropisomerism in Drug Discovery by Clayden, Jonathan, Moran, Wesley J, Edwards, Paul J, LaPlante, Steven R

“…A twist in the tale: Recent reports have highlighted solutions to the problems encountered when drug candidates exist as slowly interconverting conformers or…”
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Drug Self-Aggregation into Nano-Entities Has the Potential to Induce Immune Responses by Shahout, Fatma, Vanharen, Marion, Saafane, Abdelaziz, Gillard, James, Girard, Denis, LaPlante, Steven R.

“…The free-state solution behaviors of small molecules profoundly affect their respective properties. It is becoming more obvious that compounds can adopt a…”
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Assessing Atropisomer Axial Chirality in Drug Discovery and Development by LaPlante, Steven R, D. Fader, Lee, Fandrick, Keith R, Fandrick, Daniel R, Hucke, Oliver, Kemper, Ray, Miller, Stephen P. F, Edwards, Paul J

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Revealing Atropisomer Axial Chirality in Drug Discovery by LaPlante, Steven R., Edwards, Paul J., Fader, Lee D., Jakalian, Araz, Hucke, Oliver

“…An often overlooked source of chirality is atropisomerism, which results from slow rotation along a bond axis due to steric hindrance and/or electronic…”
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Dynamic microfluidic single-cell screening identifies pheno-tuning compounds to potentiate tuberculosis therapy by Mistretta, Maxime, Cimino, Mena, Campagne, Pascal, Volant, Stevenn, Kornobis, Etienne, Hebert, Olivier, Rochais, Christophe, Dallemagne, Patrick, Lecoutey, Cédric, Tisnerat, Camille, Lepailleur, Alban, Ayotte, Yann, LaPlante, Steven R., Gangneux, Nicolas, Záhorszká, Monika, Korduláková, Jana, Vichier-Guerre, Sophie, Bonhomme, Frédéric, Pokorny, Laura, Albert, Marvin, Tinevez, Jean-Yves, Manina, Giulia

“…Drug-recalcitrant infections are a leading global-health concern. Bacterial cells benefit from phenotypic variation, which can suggest effective antimicrobial…”
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NMR strategies to support medicinal chemistry workflows for primary structure determination by Oguadinma, Paul, Bilodeau, Francois, LaPlante, Steven R.

“…[Display omitted] Central to drug discovery is the correct characterization of the primary structures of compounds. In general, medicinal chemists make great…”
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Exposing Small-Molecule Nanoentities by a Nuclear Magnetic Resonance Relaxation Assay by Ayotte, Yann, Marando, Victoria M, Vaillancourt, Louis, Bouchard, Patricia, Heffron, Gregory, Coote, Paul W, Larda, Sacha T, LaPlante, Steven R

“…Small molecules can self-assemble in aqueous solution into a wide range of nanoentity types and sizes (dimers, n-mers, micelles, colloids, etc.), each having…”
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Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings by Fnaiche, Ahmed, Mélin, Léa, Suárez, Narjara González, Paquin, Alexis, Vu, Victoria, Li, Fengling, Allali-Hassani, Abdellah, Bolotokova, Albina, Allemand, Frédéric, Gelin, Muriel, Cotelle, Philippe, Woo, Simon, LaPlante, Steven R., Barsyte-Lovejoy, Dalia, Santhakumar, Vijayaratnam, Vedadi, Masoud, Guichou, Jean-François, Annabi, Borhane, Gagnon, Alexandre

“…[Display omitted] The Hippo pathway regulates organ size and tissue homeostasis by controlling cell proliferation and apoptosis. The YAP–TEAD transcription…”
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Fragment‐Based Phenotypic Lead Discovery: Cell‐Based Assay to Target Leishmaniasis by Ayotte, Yann, Bilodeau, François, Descoteaux, Albert, LaPlante, Steven R.

“…A rapid and practical approach for the discovery of new chemical matter for targeting pathogens and diseases is described. Fragment‐based phenotypic lead…”
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NMR spectroscopy can help accelerate antiviral drug discovery programs by LaPlante, Steven R., Coric, Pascale, Bouaziz, Serge, França, Tanos C.C.

“…Small molecule drugs have an important role to play in combating viral infections, and biophysics support has been central for contributing to the discovery…”
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A Multi-epitope Vaccine Candidate Against Bolivian Hemorrhagic fever Caused by Machupo Virus by Ali, Zeeshan, Cardoza, Jyothsna Volisha, Basak, Srijita, Narsaria, Utkarsh, Bhattacharjee, Surjit, G., Unnati Meher, Isaac, Samuel Paul, Franca, Tanos C. C., LaPlante, Steven R., George, Sudhan S.

“…Bolivian hemorrhagic fever (BHF) caused by Machupo virus (MACV) is a New World arenavirus having a reported mortality rate of 25–35%. The BHF starts with…”
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Practical Considerations and Guidelines for Spectral Referencing for Fluorine NMR Ligand Screening by Ayotte, Yann, Woo, Simon, LaPlante, Steven R

“…Fluorine (19F) NMR strategies are increasingly being employed for evaluating ligand binding to macromolecules, among many other uses. 19F NMR offers many…”
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Structure-thermodynamics-relationships of hepatitis C viral NS3 protease inhibitors by Wypych, Rachel M., LaPlante, Steven R., White, Peter W., Martin, Stephen F.

“…Thermodynamic parameters were determined for structurally-related inhibitors of HCV NS3 protease to assess how binding entropies and enthalpies vary with…”
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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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Fragment-Based Phenotypic Lead Discovery To Identify New Drug Seeds That Target Infectious Diseases by Ayotte, Yann, Bernet, Eve, Bilodeau, François, Cimino, Mena, Gagnon, Dominic, Lebughe, Marthe, Mistretta, Maxime, Ogadinma, Paul, Ouali, Sarah-Lisa, Sow, Aïssatou Aïcha, Chatel-Chaix, Laurent, Descoteaux, Albert, Manina, Giulia, Richard, Dave, Veyrier, Frédéric, LaPlante, Steven R

“…Fragment-based lead discovery has emerged over the last decades as one of the most powerful techniques for identifying starting chemical matter to target…”
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Probing the free-state solution behavior of drugs and their tendencies to self-aggregate into nano-entities by LaPlante, Steven R., Roux, Valérie, Shahout, Fatma, LaPlante, Gabriela, Woo, Simon, Denk, Maria M., Larda, Sacha T., Ayotte, Yann

“…The free-state solution behaviors of drugs profoundly affect their properties. Therefore, it is critical to properly evaluate a drug’s unique multiphase…”
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Robust Strategy for Hit-to-Lead Discovery: NMR for SAR by Larda, Sacha T., Ayotte, Yann, Denk, Maria M., Coote, Paul, Heffron, Gregory, Bendahan, David, Shahout, Fatma, Girard, Nicolas, Iddir, Mustapha, Bouchard, Patricia, Bilodeau, Francois, Woo, Simon, Farmer, Luc J., LaPlante, Steven R.

“…Establishing robust structure–activity relationships (SARs) is key to successful drug discovery campaigns, yet it often remains elusive due to screening and…”
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N-Phenylpyridine-3-Carboxamide and 6-Acetyl-1H-Indazole Inhibit the RNA Replication Step of the Dengue Virus Life Cycle by Sow, Aïssatou Aïcha, Pahmeier, Felix, Ayotte, Yann, Anton, Anaïs, Mazeaud, Clément, Charpentier, Tania, Angelo, Léna, Woo, Simon, Cerikan, Berati, Falzarano, Darryl, Abrahamyan, Levon, Lamarre, Alain, Labonté, Patrick, Cortese, Mirko, Bartenschlager, Ralf, LaPlante, Steven R, Chatel-Chaix, Laurent

“…Dengue virus (DENV) is a that causes the most prevalent arthropod-borne viral disease. Clinical manifestation of DENV infection ranges from asymptomatic to…”
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Molecular modeling of Mannich phenols as reactivators of human acetylcholinesterase inhibited by A-series nerve agents by Vieira, Leandro A., Almeida, Joyce S.F.D., De Koning, Martijn C., LaPlante, Steven R., Borges Jr, Itamar, França, Tanos C.C.

“…The A-series is the most recent generation of chemical warfare nerve agents (CWA) which act directly on the inhibition of the human acetylcholinesterase…”
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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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