These authors contributed equally to this paper.
A Small-Molecule Agonist of the Wnt Signaling Pathway†
Article first published online: 21 FEB 2005
Copyright © 2005 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 44, Issue 13, pages 1987–1990, March 18, 2005
How to Cite
Liu, J., Wu, X., Mitchell, B., Kintner, C., Ding, S. and Schultz, P. G. (2005), A Small-Molecule Agonist of the Wnt Signaling Pathway. Angew. Chem. Int. Ed., 44: 1987–1990. doi: 10.1002/anie.200462552
This work was supported by the Novartis Research Foundation and the Skaggs Institute for Chemical Biology (P.G.S.). We thank Dr. Xiang-ju Gu and Dr. Carsten Andersen for various reagents and technical assistance in GSK-3β kinase assays. This is manuscript 16945-CH of the Scripps Research Institute.
- Issue published online: 16 MAR 2005
- Article first published online: 21 FEB 2005
- Manuscript Received: 9 NOV 2004
- cellular adhesion;
- gene expression;
- high-throughput screening;
- signal transduction
A new tool for developmental biology: A screen of combinatorial chemical libraries identified the 2-amino-4,6-disubstituted pyrimidine 1 as a dose-dependent agonist of Wnt signaling. Tadpoles that developed from embryos treated with 1 had substantial head defects (see right-hand image; left=control). Compound 1 appears to mimic the effects of a Wnt ligand in a Xenopus model and may be a useful tool in the study of physiological processes that involve the Wnt pathway.