Investigation of 3-aryl-pyrimido[5,4-e][1,2,4]triazine-5,7-diones as small molecule antagonists of β-catenin/TCF transcription

Nearly all colorectal cancers (CRCs) and varied subsets of other cancers have somatic mutations leading to β-catenin stabilization and increased β-catenin/TCF transcriptional activity. Inhibition of stabilized β-catenin in CRC cell lines arrests their growth and highlights the potential of this mech...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-11, Vol.23 (21), p.5814-5820
Hauptverfasser:	Zeller, Jörg, Turbiak, Anjanette J., Powelson, Ian A., Lee, Surin, Sun, Duxin, Showalter, H.D. Hollis, Fearon, Eric R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals antagonists beta Catenin - antagonists & inhibitors beta Catenin - metabolism Cell Line Epithelial Cells - drug effects Epithelial Cells - metabolism genes intestinal mucosa mechanism of action molecular weight neoplasms Rats Small molecule antagonists Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology somatic mutation T-cell factor (TCF) TCF Transcription Factors - antagonists & inhibitors TCF Transcription Factors - metabolism therapeutics transcription (genetics) Transcriptional Activation - drug effects Triazines - chemistry Triazines - pharmacology Wnt signaling Wnt Signaling Pathway - drug effects β-Catenin
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