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  1. Book ; Online: NMR Spectroscopy Can Help Accelerate Antiviral Drug Discovery Programs

    Laplante, Steven R. / Coric, Pascale / Bouaziz, Serge / França, Tanos Celmar Costa

    2023  

    Abstract: Small molecule drugs have an important role to play in combating viral infections, and biophysics support has been central for contributing to the discovery and design of direct acting antivirals. Perhaps one of the most successful biophysical tools for ... ...

    Abstract Small molecule drugs have an important role to play in combating viral infections, and biophysics support has been central for contributing to the discovery and design of direct acting antivirals. Perhaps one of the most successful biophysical tools for this purpose is NMR spectroscopy when utilized strategically and pragmatically within team workflows and timelines. This report describes some clear examples of how NMR applications contributed to the design of antivirals when combined with medicinal chemistry, biochemistry, X-ray crystallography and computational chemistry. Overall, these multidisciplinary approaches allowed teams to reveal and expose compound physical properties from which design ideas were spawned and tested to achieve the desired successes. Examples are discussed for the discovery of antivirals that target HCV, HIV and SARS-CoV-2.
    Keywords Quantitative Biology - Biomolecules
    Publishing date 2023-11-29
    Publishing country us
    Document type Book ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Fatty acid mimetic PBI-4547 restores metabolic homeostasis via GPR84 in mice with non-alcoholic fatty liver disease.

    Simard, Jean-Christophe / Thibodeau, Jean-François / Leduc, Martin / Tremblay, Mikael / Laverdure, Alexandre / Sarra-Bournet, François / Gagnon, William / Ouboudinar, Jugurtha / Gervais, Liette / Felton, Alexandra / Letourneau, Sylvie / Geerts, Lilianne / Cloutier, Marie-Pier / Hince, Kathy / Corpuz, Ramon / Blais, Alexandra / Quintela, Vanessa Marques / Duceppe, Jean-Simon / Abbott, Shaun D /
    Blais, Amélie / Zacharie, Boulos / Laurin, Pierre / Laplante, Steven R / Kennedy, Christopher R J / Hébert, Richard L / Leblond, François A / Grouix, Brigitte / Gagnon, Lyne

    Scientific reports

    2020  Volume 10, Issue 1, Page(s) 12778

    Abstract: Non-alcoholic Fatty Liver Disease (NAFLD) is the most common form of liver disease and is associated with metabolic dysregulation. Although G protein-coupled receptor 84 (GPR84) has been associated with inflammation, its role in metabolic regulation ... ...

    Abstract Non-alcoholic Fatty Liver Disease (NAFLD) is the most common form of liver disease and is associated with metabolic dysregulation. Although G protein-coupled receptor 84 (GPR84) has been associated with inflammation, its role in metabolic regulation remains elusive. The aim of our study was to evaluate the potential of PBI-4547 for the treatment of NAFLD and to validate the role of its main target receptor, GPR84. We report that PBI-4547 is a fatty acid mimetic, acting concomitantly as a GPR84 antagonist and GPR40/GPR120 agonist. In a mouse model of diet-induced obesity, PBI-4547 treatment improved metabolic dysregulation, reduced hepatic steatosis, ballooning and NAFLD score. PBI-4547 stimulated fatty acid oxidation and induced gene expression of mitochondrial uncoupling proteins in the liver. Liver metabolomics revealed that PBI-4547 improved metabolic dysregulation induced by a high-fat diet regimen. In Gpr84
    MeSH term(s) Acetates/pharmacology ; Animals ; Binding, Competitive ; Biosensing Techniques ; Cholesterol/metabolism ; Disease Models, Animal ; Disease Progression ; Drug Discovery ; Fatty Acids/pharmacology ; Female ; Glucose/metabolism ; Glucose Tolerance Test ; HEK293 Cells ; Homeostasis ; Humans ; Ligands ; Magnetic Resonance Spectroscopy ; Male ; Metabolomics ; Mice ; Mitochondria/metabolism ; Non-alcoholic Fatty Liver Disease/drug therapy ; Non-alcoholic Fatty Liver Disease/metabolism ; Obesity/metabolism ; Oxygen/metabolism ; Plasmids/metabolism ; Protein Binding ; Receptors, G-Protein-Coupled/metabolism
    Chemical Substances Acetates ; Fatty Acids ; Gpr84 protein, mouse ; Ligands ; PBI-4547 ; Receptors, G-Protein-Coupled ; Cholesterol (97C5T2UQ7J) ; Glucose (IY9XDZ35W2) ; Oxygen (S88TT14065)
    Language English
    Publishing date 2020-07-29
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-020-69675-8
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Assessing atropisomer axial chirality in drug discovery and development.

    Laplante, Steven R / D Fader, Lee / Fandrick, Keith R / Fandrick, Daniel R / Hucke, Oliver / Kemper, Ray / Miller, Stephen P F / Edwards, Paul J

    Journal of medicinal chemistry

    2011  Volume 54, Issue 20, Page(s) 7005–7022

    MeSH term(s) Amides/chemistry ; Drug Discovery ; Heterocyclic Compounds, 4 or More Rings/chemistry ; Legislation, Drug ; Macrocyclic Compounds/chemistry ; Models, Molecular ; Pharmaceutical Preparations/chemistry ; Pharmacokinetics ; Stereoisomerism ; Structure-Activity Relationship ; Thermodynamics ; United States ; United States Food and Drug Administration
    Chemical Substances Amides ; Heterocyclic Compounds, 4 or More Rings ; Macrocyclic Compounds ; Pharmaceutical Preparations
    Language English
    Publishing date 2011-10-27
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm200584g
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
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  4. Article ; Online: The use of chemical double-mutant cycles in biomolecular recognition studies: application to HCV NS3 protease inhibitors.

    Kawai, Stephen H / Bailey, Murray D / Halmos, Ted / Forgione, Pat / Laplante, Steven R / Llinàs-Brunet, Montse / Naud, Julie / Goudreau, Natalie

    ChemMedChem

    2008  Volume 3, Issue 11, Page(s) 1654–1657

    MeSH term(s) Antiviral Agents/pharmacology ; Catalytic Domain ; Chemistry, Pharmaceutical/methods ; Drug Design ; Gene Deletion ; Glycine/chemistry ; Hepacivirus/metabolism ; Inhibitory Concentration 50 ; Molecular Conformation ; Mutation ; Peptides/chemistry ; Protein Structure, Tertiary ; Structure-Activity Relationship ; Thermodynamics ; Viral Nonstructural Proteins/genetics ; Viral Nonstructural Proteins/metabolism
    Chemical Substances Antiviral Agents ; NS3 protein, hepatitis C virus ; Peptides ; Viral Nonstructural Proteins ; Glycine (TE7660XO1C)
    Language English
    Publishing date 2008-11
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2218496-X
    ISSN 1860-7187 ; 1860-7179
    ISSN (online) 1860-7187
    ISSN 1860-7179
    DOI 10.1002/cmdc.200800214
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6280: Show issues Location:
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