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

J Zeller, AJ Turbiak, IA Powelson, S Lee, D Sun…

文献索引：Zeller, Joerg; Turbiak, Anjanette J.; Powelson, Ian A.; Lee, Surin; Sun, Duxin; Showalter, H.D. Hollis; Fearon, Eric R. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 21 p. 5814 - 5820

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被引用次数: 8

摘要

Abstract 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 mechanism for novel cancer therapeutics. We have pursued efforts to develop small molecules that inhibit β-catenin/TCF transcriptional ...