Research Topics
| Jeffrey A SmithSummaryAffiliation: University of Virginia Country: USA Publications
| Collaborators
|
Detail Information
Publications
Influence of rhamnose substituents on the potency of SL0101, an inhibitor of the Ser/Thr kinase, RSKJeffrey A Smith
Center for Cell Signaling, University of Virginia, Charlottesville, VA 22908, USA
Bioorg Med Chem 14:6034-42. 2006..Thus the discovery of 3Ac-SL0101 as a more potent RSK-specific inhibitor than SL0101 should facilitate the development of RSK inhibitors as anti-cancer chemotherapeutic agents...
Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferationJeffrey A Smith
Center for Cell Signaling, Department of Pathology, University of Virginia Health Science Center, 7041 Multistory Building, Charlottesville, VA 22908 0577, USA
Cancer Res 65:1027-34. 2005..SL0101 will provide a powerful new tool to dissect the molecular functions of RSK in cancer cells...
Creation of a stress-activated p90 ribosomal S6 kinase. The carboxyl-terminal tail of the MAPK-activated protein kinases dictates the signal transduction pathway in which they functionJ A Smith
Howard Hughes Medical Institute and the Markey Center for Cell Signaling, Departments of Medicine and Pharmacology, University of Virginia, Charlottesville, Virginia 22908, USA
J Biol Chem 275:31588-93. 2000..It is apparent that mechanisms controlling events downstream of the proline-directed MAPKs involve specific MAPK docking sites within the carboxyl termini of the MAPKAPKs that determine the cascade in which the MAPKAPK functions...
Structural basis for the activity of the RSK-specific inhibitor, SL0101Jeffrey A Smith
Center for Cell Signaling, Department of Pathology, University of Virginia, Charlottesville, VA 22908, USA
Bioorg Med Chem 15:5018-34. 2007..These studies should facilitate the development of a RSK inhibitor, based on the SL0101 pharmacophore, as an anti-cancer chemotherapeutic agent...
Extracellular signal-regulated kinase 7, a regulator of hormone-dependent estrogen receptor destructionLorin M Henrich
Department of Microbiology and Center for Cell Signaling, University of Virginia, Charlottesville, Virginia 22908, USA
Mol Cell Biol 23:5979-88. 2003..ERK7 targets the ER alpha ligand-binding domain for destruction by enhancing its ubiquitination. Thus, ERK7 is a novel regulator of estrogen responsiveness through its control of ER alpha turnover...
Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSKYa-ming Xu
Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA
Bioorg Med Chem 14:3974-7. 2006..Of these, compound 2 was found to be the best inhibitor with an IC(50) value of 89 nM...
Codependent functions of RSK2 and the apoptosis-promoting factor TIA-1 in stress granule assembly and cell survivalT S Karin Eisinger-Mathason
Department of Microbiology, University of Virginia, Charlottesville, VA 22908, USA
Mol Cell 31:722-36. 2008..Hence, RSK2 is a pivotal factor linking the stress response to survival and proliferation...
Comparison of three techniques to measure unsaturated-zone air permeability at Picatinny Arsenal, NJM S Olson
Department of Civil Engineering, University of Virginia, Charlottesville 22904 4742, USA
J Contam Hydrol 53:1-19. 2001....
Enteroaggregative Escherichia coli expresses a novel flagellin that causes IL-8 release from intestinal epithelial cellsT S Steiner
Division of Geographic and International Medicine, University of Virginia Health Sciences Center, Charlottesville, Virginia, USA
J Clin Invest 105:1769-77. 2000..Furthermore, they open new approaches for diagnosis and vaccine development. This novel pathogenic mechanism of EAEC extends an emerging paradigm of bacterial flagella as inflammatory stimuli...
Identification of an extracellular signal-regulated kinase (ERK) docking site in ribosomal S6 kinase, a sequence critical for activation by ERK in vivoJ A Smith
Howard Hughes Medical Institute and the Markey Center for Cell Signaling, Department of Medicine and Pharmacology, University of Virginia, Charlottesville, Virginia 22908, USA
J Biol Chem 274:2893-8. 1999..The number and placement of lysine and arginine residues within the conserved region correlate with specificity for activation by ERK and p38 MAPKs in vivo...
Rsk2 allosterically activates estrogen receptor alpha by docking to the hormone-binding domainD E Clark
Center for Cell Signaling and PharmaBiologicals, University of Virginia, Charlottesville, VA 22908 0577, USA
EMBO J 20:3484-94. 2001..The allosteric regulation of a target protein, independent of phosphorylation, may be paradigmatic of a general function for protein kinase docking sites...
Distributed-rate model configured in series to simulate sorption of organic pollutants to natural soilJ A Smith
Department of Civil Engineering, University of Virginia, Charlottesville 22904, USA
Bull Environ Contam Toxicol 72:94-100. 2004
The serine/threonine protein kinase, p90 ribosomal S6 kinase, is an important regulator of prostate cancer cell proliferationD E Clark
Department of Microbiology, University of Virginia, Charlottesville, VA 22908, USA
Cancer Res 65:3108-16. 2005..These results suggest that proliferation of some prostate cancer cells is dependent on RSK activity and support the hypothesis that RSK may be an important chemotherapeutic target for prostate cancer...
Homology model of RSK2 N-terminal kinase domain, structure-based identification of novel RSK2 inhibitors, and preliminary common pharmacophoreTam Luong Nguyen
Target Structure Based Drug Discovery Group, SAIC Frederick, Inc, NCI Frederick, Frederick, MD 21702, USA
Bioorg Med Chem 14:6097-105. 2006..The RSK2 NTD model was used to identify two novel RSK2 inhibitors from the National Cancer Institute open chemical repository and to develop a preliminary structure-based pharmacophore model...
