Zobrazeno 1 - 10 of 56 pro vyhledávání: '"Robert W, Marquis"'
1
Akademický článek
MLKL Compromises Plasma Membrane Integrity by Binding to Phosphatidylinositol Phosphates
Autor: Yves Dondelinger, Wim Declercq, Sylvie Montessuit, Ria Roelandt, Amanda Goncalves, Inge Bruggeman, Paco Hulpiau, Kathrin Weber, Clark A. Sehon, Robert W. Marquis, John Bertin, Peter J. Gough, Savvas Savvides, Jean-Claude Martinou, Mathieu J.M. Bertrand, Peter Vandenabeele
Publikováno v: Cell Reports, Vol 7, Iss 4, Pp 971-981 (2014)
Although mixed lineage kinase domain-like (MLKL) protein has emerged as a specific and crucial protein for necroptosis induction, how MLKL transduces the death signal remains poorly understood. Here, we demonstrate that the full four-helical bundle d
Externí odkaz: https://doaj.org/article/861d16d1f33d45d7a36b240ef8000808
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3
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase
Autor: Stéphane Sautet, Emilie Jigorel, Nicolas Faucher, Jamel Meslamani, Lara Kathryn Leister, Pascal Grondin, Julie A. Cox, Bryan W. King, Pamela Nassau, Gemma Victoria White, Brad J. Geddes, Alain Claude-Marie Daugan, Helen H. Sun, Michael T. Ouellette, Pauline Lamoureux, Elizabeth J. Rivera, Scott B. Berger, James H. Thorpe, Philip A. Harris, J. Mosley, Susan E. Hutchinson, Frédéric Donche, John Bertin, Sandra J. Hoffman, Natalie Wellaway, Patrick M. Eidam, Paris Ward, Florent Potvain, Clark A. Sehon, Sebastien Andre Campos, Robert W. Marquis, Peter J. Gough, Mukesh K. Mahajan, Veronique Beneton, Jae U. Jeong, Michelle C. Schaeffer, John D. Lich, Allison M. Beal, Rakesh Nagilla, James Michael Woolven, Bonnie L. Hoffman, Anderson Niall Andrew, Marie-Hélène Fouchet, Deepak Bandyopadhyay, Carol A. Capriotti, Rachel D. Totoritis, Joshua N. Finger, Kishore K. Pasikanti, David D. Wisnoski, Sze-Ling Ng, Nino Campobasso, Nicolas George, Michael Reilly
Publikováno v: Journal of Medicinal Chemistry. 62:5096-5110
RIP1 kinase regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including inflammatory and neurological diseases. Currently, RIP1 kinase inhibitors have advanced into early clinical
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49ff65b82b2e1feff6acc28b9dcac4dc
https://doi.org/10.1021/acs.jmedchem.9b00318
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4
Akademický článek
Identification of selective small molecule inhibitors of the nucleotide-binding oligomerization domain 1 (NOD1) signaling pathway.
Autor: David J Rickard, Clark A Sehon, Viera Kasparcova, Lorena A Kallal, Pamela A Haile, Xin Zeng, Monica N Montoute, Derek D Poore, Hu Li, Zining Wu, Patrick M Eidam, John G Emery, Robert W Marquis, Peter J Gough, John Bertin
Publikováno v: PLoS ONE, Vol 9, Iss 5, p e96737 (2014)
NOD1 is an intracellular pattern recognition receptor that recognizes diaminopimelic acid (DAP), a peptidoglycan component in gram negative bacteria. Upon ligand binding, NOD1 assembles with receptor-interacting protein (RIP)-2 kinase and initiates a
Externí odkaz: https://doaj.org/article/d8966b29a270430a972aa590bfa33f4f
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5
Overcoming the Pregnane X Receptor Liability: Rational Design to Eliminate PXR-Mediated CYP Induction
Autor: Ami S. Lakdawala, Shawn P. Williams, Demartino Michael P, Ramanjulu Joshi M, Yunfeng Lan, Robert W. Marquis
Publikováno v: ACS Med Chem Lett
[Image: see text] The pregnane X receptor (PXR) regulates expression of proteins responsible for all three phases required for the detoxification mechanism, which include CYP450 enzymes, phase II enzymes, and multidrug efflux pumps. Therefore, PXR is
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84549be94c9b79941145ba5ddc1e2096
https://pubmed.ncbi.nlm.nih.gov/34531948
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6
Akademický článek
Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway.
Autor: David J Rickard, Clark A Sehon, Viera Kasparcova, Lorena A Kallal, Xin Zeng, Monica N Montoute, Tushar Chordia, Derek D Poore, Hu Li, Zining Wu, Patrick M Eidam, Pamela A Haile, Jong Yu, John G Emery, Robert W Marquis, Peter J Gough, John Bertin
Publikováno v: PLoS ONE, Vol 8, Iss 8, p e69619 (2013)
NOD2 is an intracellular pattern recognition receptor that assembles with receptor-interacting protein (RIP)-2 kinase in response to the presence of bacterial muramyl dipeptide (MDP) in the host cell cytoplasm, thereby inducing signals leading to the
Externí odkaz: https://doaj.org/article/5e593a2a329d48da9774642aa0357266
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9
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer
Autor: Joshua N. Finger, Michael T. Ouellette, Helen H. Sun, Robert W. Marquis, Viera Kasparcova, James H. Thorpe, Scott B. Berger, Philip A. Harris, Rakesh Nagilla, George Miller, Anirudh Chirala, James Kang, Elizabeth J. Rivera, John Bertin, Peter J. Gough, Mukesh K. Mahajan, Daohua Zhang, John D. Lich, Julie A. Cox, Wei Wang, Lara Kathryn Leister, Jill M. Marinis, Rachel D. Totoritis, Patrick M. Eidam, Michael Reilly, Jae U. Jeong, Dongling Wu, Alan R. Rendina
Publikováno v: ACS Medicinal Chemistry Letters
'ACS Medicinal Chemistry Letters ', vol: 10, pages: 857-862 (2019)
RIP1 regulates cell death and inflammation and is believed to play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases and cancer. While small-molecule inhibitors of RIP1 kinase have be
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc54611512d75002b3dd48f05749d17f
https://pubmed.ncbi.nlm.nih.gov/31223438
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10
Synthesis of ( S )-3-amino-benzo[ b ][1,4]oxazepin-4-one via Mitsunobu and S N Ar reaction for a first-in-class RIP1 kinase inhibitor GSK2982772 in clinical trials
Autor: Jae Uk Jeong, James Kang, Joseph J. Romano, Philip A. Harris, Xiaoyang Dong, Lara Kathryn Leister, Yunfeng Lan, Robert W. Marquis
Publikováno v: Tetrahedron Letters. 58:2306-2308
Two new synthetic routes were developed to prepare the RIP1 kinase inhibitor clinical candidate GSK2982772 involving a key (S)-3-amino-benzo[b][1,4]oxazepin-4-one intermediate prepared via Mitsunobu and SNAr cyclization reactions. Both routes are pra
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::637de1387e4bf16986aa1ccee7c48b88
https://doi.org/10.1016/j.tetlet.2017.05.001
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