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dc.contributor.authorWalker, Sarah R.en_US
dc.contributor.authorFrank, David A.en_US
dc.date.accessioned2014-03-10T16:17:24Z
dc.date.issued2012en_US
dc.identifier.citationWalker, Sarah R., and David A. Frank. 2012. “Screening approaches to generating STAT inhibitors: Allowing the hits to identify the targets.” JAK-STAT 1 (4): 292-299. doi:10.4161/jkst.22662. http://dx.doi.org/10.4161/jkst.22662.en
dc.identifier.issn2162-3988en
dc.identifier.urihttp://nrs.harvard.edu/urn-3:HUL.InstRepos:11877091
dc.description.abstractSTAT transcription factors are regulators of critical cellular processes such as proliferation, survival, and self-renewal. While the activity of these proteins is tightly regulated under physiological conditions, they can become constitutively activated in a broad range of human cancers. This inappropriate STAT activation leads to enhanced transcription of genes that can directly lead to the malignant phenotype. Since STATs are largely dispensable for normal cell function, this has raised the possibility that STATs might be key targets for cancer therapy. Although a number of structure-based strategies have been used to develop STAT inhibitors, an alternate approach is to use cell-based assays that make use of the transcriptional function of STATs. Employing these systems, one can screen large chemical libraries to identify compounds that specifically block the function of a given STAT. This approach can lead to the identification of compounds that inhibit STATs by a variety of mechanisms, and can suggest novel targets for therapy. This type of functional screening strategy has already identified a drug that potently inhibits STAT3, and which is now being evaluated in a clinical trial for patients with chronic lymphocytic leukemia.en
dc.language.isoen_USen
dc.publisherLandes Bioscienceen
dc.relation.isversionofdoi:10.4161/jkst.22662en
dc.relation.hasversionhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC3670287/pdf/en
dash.licenseLAAen_US
dc.subjecttranscription factorsen
dc.subjectphosphorylationen
dc.subjectdrug discoveryen
dc.subjectcancer therapyen
dc.subjectapoptosisen
dc.titleScreening approaches to generating STAT inhibitors: Allowing the hits to identify the targetsen
dc.typeJournal Articleen_US
dc.description.versionVersion of Recorden
dc.relation.journalJAK-STATen
dash.depositing.authorWalker, Sarah R.en_US
dc.date.available2014-03-10T16:17:24Z
dc.identifier.doi10.4161/jkst.22662*
dash.contributor.affiliatedFrank, David
dash.contributor.affiliatedWalker, Sarah


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