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dc.contributor.authorYeo, Alan T.en_US
dc.contributor.authorChennamadhavuni, Spandanen_US
dc.contributor.authorWhitty, Adrianen_US
dc.contributor.authorPorco, John A.en_US
dc.contributor.authorGilmore, Thomas D.en_US
dc.coverage.spatialSwitzerlanden_US
dc.date2015-04-20
dc.date.accessioned2018-01-25T20:17:37Z
dc.date.available2018-01-25T20:17:37Z
dc.date.issued2015-04-23
dc.identifierhttps://www.ncbi.nlm.nih.gov/pubmed/25915462
dc.identifier.citationAlan T Yeo, Spandan Chennamadhavuni, Adrian Whitty, John A Porco, Thomas D Gilmore. 2015. "Inhibition of Oncogenic Transcription Factor REL by the Natural Product Derivative Calafianin Monomer 101 Induces Proliferation Arrest and Apoptosis in Human B-Lymphoma Cell Lines.." Molecules, Volume 20, Issue 5, pp. 7474 - 7494.
dc.identifier.issn1420-3049
dc.identifier.urihttps://hdl.handle.net/2144/26429
dc.description.abstractIncreased activity of transcription factor NF-κB has been implicated in many B-cell lymphomas. We investigated effects of synthetic compound calafianin monomer (CM101) on biochemical and biological properties of NF-κB. In human 293 cells, CM101 selectively inhibited DNA binding by overexpressed NF-κB subunits REL (human c-Rel) and p65 as compared to NF-κB p50, and inhibition of REL and p65 DNA binding by CM101 required a conserved cysteine residue. CM101 also inhibited DNA binding by REL in human B-lymphoma cell lines, and the sensitivity of several B-lymphoma cell lines to CM101-induced proliferation arrest and apoptosis correlated with levels of cellular and nuclear REL. CM101 treatment induced both phosphorylation and decreased expression of anti-apoptotic protein Bcl-XL, a REL target gene product, in sensitive B-lymphoma cell lines. Ectopic expression of Bcl-XL protected SUDHL-2 B-lymphoma cells against CM101-induced apoptosis, and overexpression of a transforming mutant of REL decreased the sensitivity of BJAB B-lymphoma cells to CM101-induced apoptosis. Lipopolysaccharide-induced activation of NF-κB signaling upstream components occurred in RAW264.7 macrophages at CM101 concentrations that blocked NF-κB DNA binding. Direct inhibitors of REL may be useful for treating B-cell lymphomas in which REL is active, and may inhibit B-lymphoma cell growth at doses that do not affect some immune-related responses in normal cells.en_US
dc.description.sponsorshipR01 GM094551 - NIGMS NIH HHS; P50 GM067041 - NIGMS NIH HHS; GM094551 - NIGMS NIH HHS; R24 GM111625 - NIGMS NIH HHS; GM067041 - NIGMS NIH HHSen_US
dc.format.extentp. 7474 - 7494en_US
dc.languageeng
dc.relation.ispartofMolecules
dc.rights© 2015 by the authors. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).en_US
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subjectLife sciences & biomedicineen_US
dc.subjectBiochemistry & molecular biologyen_US
dc.subjectChemistryen_US
dc.subjectc-Relen_US
dc.subjectNF-kappaBen_US
dc.subjectChemical inhibitoren_US
dc.subjectB-cell lymphomaen_US
dc.subjectCalafianinen_US
dc.subjectNatural producten_US
dc.subjectEpoxyquinone A monomeren_US
dc.subjectC-RELen_US
dc.subjectSesquiterpene lactonesen_US
dc.subjectPhosphorylationen_US
dc.subjectCysteine residiesen_US
dc.subjectCanceren_US
dc.subject3T3 cellsen_US
dc.subjectAnimalsen_US
dc.subjectApoptosisen_US
dc.subjectCell line, tumoren_US
dc.subjectCell proliferationen_US
dc.subjectDNA-binding proteinsen_US
dc.subjectEnzyme activationen_US
dc.subjectHEK293 cellsen_US
dc.subjectHumansen_US
dc.subjectL cells (cell line)en_US
dc.subjectLipopolysaccharidesen_US
dc.subjectLymphoma, B-cellen_US
dc.subjectMacrophagesen_US
dc.subjectMiceen_US
dc.subjectNF-kappa B p50 subuniten_US
dc.subjectPhosphorylationen_US
dc.subjectProto-oncogene proteins c-Relen_US
dc.subjectTranscription factor RelAen_US
dc.subjectTyrosineen_US
dc.subjectBcl-X proteinen_US
dc.subjectOrganic chemistryen_US
dc.titleInhibition of oncogenic transcription factor REL by the natural product derivative calafianin monomer 101 induces proliferation arrest and apoptosis in human B-lymphoma cell linesen_US
dc.typeArticleen_US
dc.identifier.doi10.3390/molecules20057474
pubs.elements-sourcepubmeden_US
pubs.notesEmbargo: Not knownen_US
pubs.organisational-groupBoston Universityen_US
pubs.organisational-groupBoston University, Administrationen_US
pubs.organisational-groupBoston University, College of Arts & Sciencesen_US
pubs.organisational-groupBoston University, College of Arts & Sciences, Department of Biologyen_US
pubs.organisational-groupBoston University, College of Arts & Sciences, Department of Chemistryen_US
pubs.publication-statusPublished onlineen_US


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©  2015  by  the  authors. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license
(http://creativecommons.org/licenses/by/4.0/).
Except where otherwise noted, this item's license is described as © 2015 by the authors. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).