Novel small molecule activators of β-catenin-mediated signaling pathway: structure–activity relationships of indirubins

doi:10.1016/j.bmcl.2009.02.083

Bioorganic & Medicinal Chemistry Letters

Volume 19, Issue 8, 15 April 2009, Pages 2282-2284

https://doi.org/10.1016/j.bmcl.2009.02.083 Get rights and content

Abstract

Based on the β-catenin-drived Wnt activator of bromoindirubin-3′-oxime (BIO), indirubin analogs were evaluated for β-catenin-mediated gene expression. A novel indirubin analog, indirubin-5-nitro-3′-oxime (INO), was considered a potential activator, and structure–activity studies were conducted with indirubins. These data suggest that INO might be a novel Wnt activator and has a potential of signaling regulator in β-catenin-mediated signaling pathways.

Graphical abstract

Based on the β-catenin-drived Wnt activator of 6-bromoindirubin-3′-oxime (BIO), indirubin analogs were evaluated for β-catenin-mediated gene expression. A novel indirubin analog, indirubin-5-nitro-3′-oxime (INO), was considered a potential activator, and structure–activity studies were conducted with indirubins.

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Acknowledgements

This work was supported by Grant No. R15-2006-020 from the National Core Research Center (NCRC) program of the Ministry of Education, Science and Technology (MEST) and the Korea Science and Engineering Foundation (KOSEF) through the Center for Cell Signalling & Drug Discovery Research at Ewha Womans University.

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Novel small molecule activators of β-catenin-mediated signaling pathway: structure–activity relationships of indirubins

Abstract

Graphical abstract

Section snippets

Acknowledgements

Science

Trends Cell Biol.

Nat. Cell Biol.

J. Cell Physiol.

J. Cell Biol.

Gene Dev.

Biochem. Biophys. Res. Commun.

Biochem. Biophys. Res. Commun.

Mech. Dev.

Endocrinology

J. Mammary Gland Biol. Neoplasia.

Brain Res. Rev.

Mol. Endocrinol.

J. Biol. Chem.

Chem. Biol.