Výsledky vyhledávání - "Robert J. Mourey"

Inhibition of Hepatobiliary Transporters by A Novel Kinase Inhibitor Contributes to Hepatotoxicity in Beagle Dogs

Autor: Yurong Lai, Daniel Walker, John Scott Daniels, Rouchelle Mireles, Robert J. Mourey, Jeffrey Stevens, Sarah A. South, John W. Davis, Laurence O. Whiteley, David R. Anderson, Jeremy W. Mckenzie, Bo Feng, Po-Chang Chiang

Publikováno v: Scopus-Elsevier

PF-022 (1) is a novel polycyclic benzothiophene kinase inhibitor selective for mitogen-activated protein kinase-activated protein kinase 2 (MK2). Compound 1 emerged as an inhibitor bearing submicromolar potency against MK2 (IC 50 5 nM) and demonstrat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b56779e7e3046894e2e88dcb550435fa
https://doi.org/10.2174/18723128112066660018

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A Benzothiophene Inhibitor of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 Inhibits Tumor Necrosis Factor α Production and Has Oral Anti-Inflammatory Efficacy in Acute and Chronic Models of Inflammation

Autor: Robert J. Mourey, Matthew J. Saabye, Marvin J. Meyers, J. Scott Daniels, William F. Hood, Stephen J. Mnich, Jian Zhang, Jeffrey L. Hirsch, Sarah J. Brustkern, Betsy Pierce, Barry L. Burnette, David R. Anderson, John F. Schindler, Elizabeth G. Webb, Sarah A. South

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 333:797-807

Activation of the p38 kinase pathway in immune cells leads to the transcriptional and translational regulation of proinflammatory cytokines. Mitogen-activated protein kinase-activated protein kinase 2 (MK2), a direct downstream substrate of p38 kinas

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a1b053fe059b5214cc7c10c699da95f
https://doi.org/10.1124/jpet.110.166173

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Benzothiophene inhibitors of MK2. Part 1: Structure–activity relationships, assessments of selectivity and cellular potency

Autor: Ravi G. Kurumbail, Marvin J. Meyers, Matthew W. Mahoney, Robert J. Mourey, David R. Anderson, Gennadiy Poda, Nicole Caspers, Betsy Pierce, Scott A. Long

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:4878-4881

Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure-activity relationship (SAR) studies, selectivity assessments against CDK2, cellular potency and mechanism of action are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e06e93b2318a4cbb4137761ef77f8efc
https://doi.org/10.1016/j.bmcl.2009.02.015

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Aqueous versus non-aqueous salt delivery strategies to enhance oral bioavailability of a mitogen-activated protein kinase-activated protein kinase (MK-2) inhibitor in rats

Autor: Steve P. Wene, Jon G. Selbo, Robert J. Mourey, Lesley A. Albin, Po-Chang Chiang, J. Scott Daniels, Sarah A. South, David R. Anderson

Publikováno v: Journal of Pharmaceutical Sciences. 98:248-256

A potent pyridine-containing MK2 inhibitor has recently been internally discovered. In pre-clinical dosing, the low solubility of the neutral form limited oral bioavailability and dose escalation in toxicity studies. A mesylate salt was developed as

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cbd0cfaa94b6d9838c3229faef62b376
https://doi.org/10.1002/jps.21425

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Benzothiophene inhibitors of MK2. Part 2: Improvements in kinase selectivity and cell potency

Autor: Ravi G. Kurumbail, Betsy Pierce, Gennadiy Poda, Marvin J. Meyers, Mihir D. Parikh, Robert J. Mourey, Nicole Caspers, Matthew W. Mahoney, Scott A. Long, David R. Anderson

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:4882-4884

Optimization of kinase selectivity for a set of benzothiophene MK2 inhibitors provided analogs with potencies of less than 500 nM in a cell based assay. The selectivity of the inhibitors can be rationalized by examination of X-ray crystal structures

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77c556984b177bb872a50ccc0db6b977
https://doi.org/10.1016/j.bmcl.2009.02.017

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Identification of a hormonally regulated protein tyrosine phosphatase associated with bone and testicular differentiation

Autor: Beverley M. Skrobacz, Jack E. Dixon, Laura J. Mauro, Alan R. Davis, Robert J. Mourey, Elizabeth A. Olmsted

Publikováno v: Journal of Biological Chemistry. 269:30659-30667

Absence of the tyrosine kinase activity of c-src and c-fms results in impairment of bone remodeling. Such dysfunction underscores the importance of tyrosine phosphorylation, yet the role of protein tyrosine phosphatases in bone metabolism remains une

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::915bfaa6ead14e688ca70790dfd4da8d
https://doi.org/10.1016/s0021-9258(18)43864-1

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Protein tyrosine phosphatases: characterization of extracellular and intracellular domains

Autor: Robert J. Mourey, Jack E. Dixon

Publikováno v: Current Opinion in Genetics & Development. 4:31-39

Protein tyrosine phosphatases (PTPs) play an important role in the regulation of cell growth and differentiation. With over 30 PTPs identified, the specific functions of these enzymes are now being addressed. The identification of extracellular domai

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::934b759a237560d1c13e9ad07a1b5d10
https://doi.org/10.1016/0959-437x(94)90088-4

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Inhibition of the protein kinase MK-2 protects podocytes from nephrotic syndrome-related injury

Autor: Richard F. Ransom, Robert J. Mourey, Adam J. Guess, Rainer Benndorf, Joshua Manley, Ruma Pengal, Shipra Agrawal, William E. Smoyer

While mitogen-activated protein kinase (MAPK) activation has been implicated in the pathogenesis of various glomerular diseases, including nephrotic syndrome (NS), its specific role in podocyte injury is not known. We hypothesized that MK-2, a downst

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5af405dc040d71eaf1483501381088a
https://europepmc.org/articles/PMC3174552/

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Inositol 1,4,5-trisphosphate receptors: Labeling the inositol 1,4,5-trisphosphate binding site with photoaffinity ligands

Autor: Robert J. Mourey, Glenn D. Prestwich, Solomon H. Snyder, Virginia A. Estevez, James F. Marecek, Roxanne K. Barrow

Publikováno v: Biochemistry. 32:1719-1726

We have photolabeled the inositol 1,4,5-trisphosphate (IP3) receptor and probed the IP3 ligand binding site using two novel photoaffinity ligands, [125I] (azidosalicyl)aminopropyl-IP3 ([125I]ASA-IP3) and [3H] (benzoyldihydrocinnamyl)aminopropyl-IP3 (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22da31440d4006c68bfef5e5ee625214
https://doi.org/10.1021/bi00058a004

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