Abstract：
:A series of compounds based on a 4-phenyl-2-phenylaminopyridine scaffold that are potent and selective inhibitors of Traf2- and Nck-interacting kinase (TNIK) activity are described. These compounds were used as tools to test the importance of TNIK kinase activity in signaling and proliferation in Wnt-activated colorectal cancer cells. The results indicate that pharmacological inhibition of TNIK kinase activity has minimal effects on either Wnt/TCF4/β-catenin-driven transcription or viability. The findings suggest that the kinase activity of TNIK may be less important to Wnt signaling than other aspects of TNIK function, such as its putative role in stabilizing the TCF4/β-catenin transcriptional complex.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Ho KK,Parnell KM,Yuan Y,Xu Y,Kultgen SG,Hamblin S,Hendrickson TF,Luo B,Foulks JM,McCullar MV,Kanner SBdoi
10.1016/j.bmcl.2012.11.013subject
Has Abstractpub_date
2013-01-15 00:00:00pages
569-73issue
2eissn
0960-894Xissn
1464-3405pii
S0960-894X(12)01456-4journal_volume
23pub_type
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