Zobrazeno 1 - 8 of 8 pro vyhledávání: '"Heidi R. Hope"'
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Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the MK2 Inhibitor ATI-450 in Healthy Subjects: A Placebo-Controlled, Randomized Phase 1 Study
Autor: David Burt, Edward T Hellriegel, Heidi R. Hope, David Gordon, Joseph B. Monahan
Publikováno v: Clinical Pharmacology : Advances and Applications
David Gordon,1 Edward T Hellriegel,1 Heidi Rath Hope,2 David Burt,1 Joseph B Monahan2 1Research and Development, Aclaris Therapeutics, Inc., Wayne, PA, USA; 2Research and Development, Aclaris Therapeutics, Inc., and Confluence Discovery Technologies,
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63f99e69e6e52c1669292ef34fd7d167
http://europepmc.org/articles/PMC8203602
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3
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design
Autor: Lori Krim Gavrin, David Hepworth, Jennifer R. Thomason, Iain Kilty, Joel Adam Goldberg, Christoph W. Zapf, Vikram R. Rao, Brian P. Boscoe, Akshay Patny, Peter T. Symanowicz, Marina W.H. Shen, Kevin J. Curran, Elizabeth Murphy, Martin Hegen, Fabien Vincent, Richard Vargas, Satwik Kamtekar, Heidi M. Morgan, Heidi R. Hope, Richard K. Frisbie, Jeanne S. Chang, Ken Dower, Susan E. Drozda, Strohbach Joseph Walter, Mathias John Paul, David R. Anderson, Jacqueline E. Day, Stephen W. Wright, Ivan J. Samardjiev, Seungil Han, Julia H Shin, Frank Lovering, Andrea G Bree, Arthur Lee, Holly H. Soutter, Joanne Brodfuehrer, John David Trzupek, Brian Samas, Christoph Martin Dehnhardt, Michael Dennis Lowe, Catherine M. Ambler, Seung Won Chung, Eddine Saiah, Nikolaos Papaioannou, Pierce Betsy S, Jiangli Yan, Katherine L. Lee, Lih-Ling Lin, Chulho Choi
Publikováno v: Journal of Medicinal Chemistry. 60:5521-5542
Through fragment-based drug design focused on engaging the active site of IRAK4 and leveraging three-dimensional topology in a ligand-efficient manner, a micromolar hit identified from a screen of a Pfizer fragment library was optimized to afford IRA
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54d71e108dde9e50f577dacbc8e3364e
https://doi.org/10.1021/acs.jmedchem.7b00231
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4
Selective inhibition of the p38α MAPK-MK2 axis inhibits inflammatory cues including inflammasome priming signals
Autor: E. Jon Jacobsen, Matthew J. Saabye, Chun Wang, Jeffrey L. Hirsch, Sheri L. Bonar, Gabriel Mbalaviele, Shaun R. Selness, Hal M. Hoffman, Susan L. Hockerman, Yael Alippe, Joseph B. Monahan, William F. Hood, Stephen J. Mnich, Yousef Abu-Amer, Ariela Haimovich, Heidi R. Hope
Publikováno v: The Journal of Experimental Medicine
A unique p38α MAPK–MK2 pathway inhibitor, CDD-450, is used to uncover the function of this protein complex in inflammasome priming signals. Importantly, CDD-450 is as efficacious as global p38α MAPK inhibitors in decreasing inflammation in diseas
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::531a33bf2ac0ef32007b6033ed6f2f52
https://pubmed.ncbi.nlm.nih.gov/29686326
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5
Interleukin-1β-induced interleukin-6 production in A549 cells is mediated by both phosphatidylinositol 3-kinase and interleukin-1 receptor-associated kinase-4
Autor: Joseph B. Monahan, Heidi R. Hope, Barry L. Burnette, Hiroyuki Eda, Hideaki Shimada
Publikováno v: Cell Biology International. 35:355-358
The aim of this study is to investigate whether PI3K (phosphatidylinositol-3-kinase) is involved in IL-1β (interleukin-1β)-induced IL-6 production in A549 (human lung adenocarcinoma epithelial cell) and human RASF (rheumatoid arthritis synovial fib
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9d7889f3561a62f90f962dd4e80265f
https://doi.org/10.1042/cbi20100247
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6
SD0006: A Potent, Selective and Orally Available Inhibitor of p38 Kinase
Autor: Jeffrey L. Hirsch, Robert H. Keith, Loreen Stillwell, Pamela De Ciechi, Jian Zhang, Ravi G. Kurumbail, Richard M. Leimgruber, Shaun R. Selness, Huey S. Shieh, Stephen J. Mnich, Yan Zhang, Barry L. Burnette, Michael Hepperle, Robert P. Compton, Raj Devraj, Gail Jungbluth, Win Naing, Joseph B. Monahan, Joseph Portanova, Gary D. Anderson, Heidi R. Hope
Publikováno v: Pharmacology. 84:42-60
SD0006 is a diarylpyrazole that was prepared as an inhibitor of p38 kinase-alpha (p38alpha). In vitro, SD0006 was selective for p38alpha kinase over 50 other kinases screened (including p38gamma and p38delta with modest selectivity over p38beta). Cry
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::417af8711e84292fd44a13daf8ddc013
https://doi.org/10.1159/000227286
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7
Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation
Autor: Gabriel Mbalaviele, Rajesh V. Devraj, Elizabeth G. Webb, Jeffrey L. Hirsch, Heidi R. Hope, Matthew J. Saabye, Dean Messing, Jian Zhang, Joseph B. Monahan, Shaun R. Selness, John F. Schindler, Loreen Stillwell, Barry L. Burnette, Gary D. Anderson, Robert P. Compton, Xiong Li, Robert H. Keith
Publikováno v: The Journal of pharmacology and experimental therapeutics. 331(3)
Signal transduction through the p38 mitogen-activated protein (MAP) kinase pathway is central to the transcriptional and translational control of cytokine and inflammatory mediator production. p38 MAP kinase inhibition hence constitutes a promising t
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43bf14977f74059927334568730cf7b0
https://pubmed.ncbi.nlm.nih.gov/19720877
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8
Structural bioinformatics-based prediction of exceptional selectivity of p38 MAP kinase inhibitor PH-797804
Autor: Jennifer M. Williams, Li Xing, Ravi G. Kurumbail, Devadas Balekudru, Jeffrey L. Hirsch, Alan G. Benson, Heidi R. Hope, Roderick A. Stegeman, Zara Walden, Joseph B. Monahan, Shaun R. Selness, Rajesh V. Devraj, Richard M. Broadus, Huey S. Shieh, John K. Walker, Robert P. Compton, John F. Schindler
Publikováno v: Biochemistry. 48(27)
PH-797804 is a diarylpyridinone inhibitor of p38alpha mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer (aS), first proposed by molecular modeling and subsequently confirmed by experiments. On the ba
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2167645ed381b042a0fce22befe0bfe1
https://pubmed.ncbi.nlm.nih.gov/19496616
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