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Lin, R., Connolly, P.J., Huang, S., et al. (2005) 1-Acyl- 1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: Synthesis and evaluation of biological activities. Journal of Medicinal Chemistry, 48, 4208-4211. doi:10.1021/jm050267e

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• TITLE: Inhibitors of protein kinases affecting cAMP-dependent proteolysis of GATA-6

  AUTHORS: Hironori Ushijima, Masatomo Maeda

  KEYWORDS: cAMP; GATA-6; Kinase Inhibitor; Proteolysis; Transcription Factor

  JOURNAL NAME: Advances in Biological Chemistry, Vol.2 No.4, November 28, 2012

  ABSTRACT: We screened 95 kinase inhibitors whether they affect cAMP-dependent proteolysis of GATA-6 or not. Among them 7 inhibitors inhibited the proteolysis at the concentration range of μM around their IC50. They are inhibitors for protein kinase A (H-89 and 4- cyano-3-methylisoquinoline), c-Jun N-terminal kinase (SP600125), phosphatidylinositol 3-kinase (Wort- mannin and LY-294002), casein kinase II (TBB) and cyclin dependent kinase (Cdk1/2 inhibitor III). It is of interest how these kinases play roles in the degradation process of GATA-6 since this transcription factor is essential for development and tissue-specific gene expression of mammals. Inhibitors identified in this study would be helpful to study molecular mechanisms of phenomena in which GATA-6 participates.