Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α

A Xenopus laevis two-reporter screen identifies the antihelminthic drug pyrvinium as an inhibitor of the Wnt/β-catenin signaling pathway that works by activating CK1α, which is likely working at the level of Pygopus, a core transcriptional component of the Wnt pathway. Wnt/β-catenin signaling is cri...

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Veröffentlicht in:	Nature chemical biology 2010-11, Vol.6 (11), p.829-836
Hauptverfasser:	Thorne, Curtis A, Hanson, Alison J, Schneider, Judsen, Tahinci, Emilios, Orton, Darren, Cselenyi, Christopher S, Jernigan, Kristin K, Meyers, Kelly C, Hang, Brian I, Waterson, Alex G, Kim, Kwangho, Melancon, Bruce, Ghidu, Victor P, Sulikowski, Gary A, LaFleur, Bonnie, Salic, Adrian, Lee, Laura A, Miller, David M, Lee, Ethan
Format:	Artikel
Sprache:	eng
Schlagworte:	631/80/86 631/92/607/275 631/92/609 631/92/613 Adaptor Proteins, Signal Transducing Adenomatous Polyposis Coli - genetics Adenomatous Polyposis Coli - metabolism Animals Axin Protein beta Catenin - genetics beta Catenin - metabolism Biochemical Engineering Biochemistry Bioorganic Chemistry Casein Kinase I - genetics Casein Kinase I - metabolism Casein Kinase Ialpha - metabolism Cell Biology Cell Extracts Cell Line, Tumor Cell Proliferation - drug effects Chemistry Chemistry and Materials Science Chemistry/Food Science Colonic Neoplasms - metabolism Colonic Neoplasms - pathology Dose-Response Relationship, Drug Enzyme Activation - drug effects Enzyme Inhibitors - pharmacology Humans Intracellular Signaling Peptides and Proteins - genetics Intracellular Signaling Peptides and Proteins - metabolism Oocytes - cytology Oocytes - metabolism Pyrvinium Compounds - pharmacology Repressor Proteins - genetics Repressor Proteins - metabolism Signal Transduction - drug effects Wnt Proteins - antagonists & inhibitors Wnt Proteins - chemistry Wnt Proteins - genetics Wnt Proteins - metabolism Xenopus laevis Xenopus Proteins
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