Search Results - "Breinlinger, Eric"

Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists by Amaudrut, Jérôme, Argiriadi, Maria A., Barth, Martine, Breinlinger, Eric C., Bressac, Didier, Broqua, Pierre, Calderwood, David J., Chatar, Mohamed, Cusack, Kevin P., Gauld, Stephen B., Jacquet, Sébastien, Kamath, Rajesh V., Kort, Michael E., Lepais, Valérie, Luccarini, Jean-Michel, Masson, Philippe, Montalbetti, Christian, Mounier, Laurent, Potin, Dominique, Poupardin, Olivia, Rouaud, Sylvie, Spitzer, Luc, Wallace, Craig D.

“…[Display omitted] A high-throughput screen against Inventiva’s compound library using a Gal4/RORγ-LBD luciferase reporter gene assay led to the discovery of a…”
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Discovery of Selective and Orally Bioavailable Protein Kinase Cθ (PKCθ) Inhibitors from a Fragment Hit by George, Dawn M., Breinlinger, Eric C., Friedman, Michael, Zhang, Yang, Wang, Jianfei, Argiriadi, Maria, Bansal-Pakala, Pratima, Barth, Martine, Duignan, David B., Honore, Prisca, Lang, QingYu, Mittelstadt, Scott, Potin, Dominique, Rundell, Lian, Edmunds, Jeremy J.

“…Protein kinase Cθ (PKCθ) regulates a key step in the activation of T cells. On the basis of its mechanism of action, inhibition of this kinase is hypothesized…”
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Optimized Protein Kinase Cθ (PKCθ) Inhibitors Reveal Only Modest Anti-inflammatory Efficacy in a Rodent Model of Arthritis by George, Dawn M., Breinlinger, Eric C., Argiriadi, Maria A., Zhang, Yang, Wang, Jianfei, Bansal-Pakala, Pratima, Duignan, David B., Honore, Prisca, Lang, QingYu, Mittelstadt, Scott, Rundell, Lian, Schwartz, Annette, Sun, Jiakang, Edmunds, Jeremy J.

“…We previously demonstrated that selective inhibition of protein kinase Cθ (PKCθ) with triazinone 1 resulted in dose-dependent reduction of paw swelling in a…”
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Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3 by Hayes, Martin E., Breinlinger, Eric C., Wallace, Grier A., Grongsaard, Pintipa, Miao, Wenyan, McPherson, Michael J., Stoffel, Robert H., Green, David W., Roth, Gregory P.

“…Modification of a 2-iminobenzimidazole series derived from an HTS hit resulted in compounds with improved in-vitro species selectivity. Incorporation of an…”
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Model Systems for Flavoenzyme Activity. Modulation of Flavin Redox Potentials through π-Stacking Interactions by Breinlinger, Eric C, Rotello, Vincent M

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Modulation of Flavin Recognition and Redox Properties through Donor Atom−π Interactions by Breinlinger, Eric C, Keenan, Christopher J, Rotello, Vincent M

“…Computational and experimental model studies establish the importance of donor atom−π bonding on the recognition and function of flavins. This noncovalent…”
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Electrochemical Control of Recognition Processes. A Three-Component Molecular Switch by Deans, Robert, Niemz, Angelika, Breinlinger, Eric C, Rotello, Vincent M

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Controlled Multi-Stage Recognition of Guests Using Orthogonal Electro- and Photochemical Inputs by Goodman, Allan, Breinlinger, Eric, Ober, Matthias, Rotello, Vincent M

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Model Systems for Flavoenzyme Activity. Control of Flavin Recognition via Specific Electrostatic Interactions by Goodman, Allan J, Breinlinger, Eric C, McIntosh, Catherine M, Grimaldi, Lisa N, Rotello, Vincent M

“…A model system has been used to study the interactions of dipole-containing aromatic systems with oxidized and reduced flavin. Ab initio computational and…”
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Targeting the Tyrosine Kinase 2 (TYK2) Pseudokinase Domain: Discovery of the Selective TYK2 Inhibitor ABBV-712 by Breinlinger, Eric, Van Epps, Stacy, Friedman, Michael, Argiriadi, Maria, Chien, Ellen, Chhor, Gekleng, Cowart, Marlon, Dunstan, Theresa, Graff, Candace, Hardee, David, Herold, J. Martin, Little, Andrew, McCarthy, Richard, Parmentier, Julie, Perham, Matthew, Qiu, Wei, Schrimpf, Michael, Vargo, Thomas, Webster, Matthew P., Wu, Fei, Bennett, Dawn, Edmunds, Jeremy

“…Tyrosine kinase 2 (TYK2) is a nonreceptor tyrosine kinase that belongs to the JAK family also comprising JAK1, JAK2, and JAK3. TYK2 is an attractive target for…”
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DNA-Compatible Copper-Catalyzed Oxidative Amidation of Aldehydes with Non-Nucleophilic Arylamines by Li, Ke, Qu, Yi, An, Yulong, Breinlinger, Eric, Webster, Matthew P, Wen, Huanan, Ding, Duanchen, Zhao, Meng, Shi, Xiaodong, Wang, Jiangong, Su, Wenji, Cui, Weiren, Satz, Alexander L, Yang, Hongfang, Kuai, Letian, Little, Andrew, Peng, Xuanjia

“…We report a DNA-compatible protocol for synthesizing amides from DNA-bound aldehydes and non-nucleophilic arylamines including aza-substituted anilines,…”
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Inhibition of Interleukin-23-Mediated Inflammation with a Novel Small Molecule Inverse Agonist of ROR γ t by Gauld, Stephen B, Jacquet, Sebastien, Gauvin, Donna, Wallace, Craig, Wang, Yibing, McCarthy, Richard, Goess, Christian, Leys, Laura, Huang, Susan, Su, Zhi, Edelmayer, Rebecca, Wetter, Joseph, Salte, Katherine, McGaraughty, Steven P, Argiriadi, Maria A, Honore, Prisca, Luccarini, Jean-Michel, Bressac, Didier, Desino, Kelly, Breinlinger, Eric, Cusack, Kevin, Potin, Dominique, Kort, Michael E, Masson, Philippe J

“…Blockade of interleukin (IL)-23 or IL-17 with biologics is clinically validated as a treatment of psoriasis. However, the clinical impact of targeting other…”
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Selective transport of riboflavin through a liquid organic membrane by Lambert, Edward, Breinlinger, Eric C., Rotello, Vincent M.

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Model Systems for Flavoenzyme Activity. Stabilization of the Flavin Radical Anion through Specific Hydrogen Bond Interactions by Breinlinger, Eric, Niemz, Angelika, Rotello, Vincent M

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Model systems for flavoenzyme activity molecular recognition in multiple oxidation states by Breinlinger, Eric C

“…Flavoenzymes mediate a large number of oxidation and reduction reactions throughout nature. This wide variety of catalytic transformations is accomplished by…”
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