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Exploring the utility of organo-polyoxometalate hybrids to inhibit SOX transcription factors

Cell Regeneration 2014年第1期3卷 69-75页

作者： Kamesh Narasimhan Kevin Micoine Emmanuel Lacôte serge thorimbert Edwin Cheung Bernold Hasenknopf Ralf Jauch Donnelly Centre for Cellular and Biomolecular Research University of TorontoToronto M5S 3E1Canada Genome Institute of Singapore 60 Biopolis StreetBuona Vista 138672Singapore Sorbonne Universités UPMC Univ Paris 06Institut Parisien de Chimie MoléculaireUMR 82324 Place Jussieu75005 ParisFrance CNRS Institut Parisien de Chimie MoléculaireUMR 82324 Place Jussieu75005 ParisFrance Faculty of Health Sciences University of MacaoAv.Padre Tomas PereiraTaipaMacaoChina Genome Regulation Laboratory Drug Development PipelineGuangzhou Institutes of Biomedicine190 Kai Yuan AvenueScience Park510530 GuangzhouChina

Background:SOX transcription factors constitute an attractive target class for intervention with small molecules as they play a prominent role in the field of regenerative biomedicine and cancer ***,rationally engineering specific inhibitors that interfere with transcription factor DNA interfaces continues to be a monumental challenge in the field of transcription factor chemical ***(POMs)are inorganic compounds that were previously shown to target the high-mobility group(HMG)of SOX proteins at nanomolar *** continuation of this work,we carried out an assessment of the selectivity of a panel of newly synthesized organo-polyoxometalate hybrids in targeting different transcription factor families to enable the usage of polyoxometalates as specific SOX transcription factor ***:The residual DNA-binding activities of 15 different transcription factors were measured after treatment with a panel of diverse *** belonging to the Dawson structural class were found to be more potent inhibitors than the Keggin ***,organically modified Dawson polyoxometalates were found to be the most potent in inhibiting transcription factor DNA binding *** size of the polyoxometalates and its derivitization were found to be the key determinants of their ***:Polyoxometalates are highly potent,nanomolar range inhibitors of the DNA binding activity of the Sox-HMG ***,binding assays involving a limited subset of structurally diverse polyoxometalates revealed a low selectivity profile against different transcription factor *** progress in achieving selectivity and deciphering structure-activity relationship of POMs require the identification of POM binding sites on transcription factors using elaborate approaches like X-ray crystallography and multidimensional *** summary,our report reaffirms that transcription factors are challenging molecular architec

关键词： architectures attractive rational

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