STAT6 phosphorylation inhibitors block eotaxin-3 secretion in bronchial epithelial cells.

Abstract

The STAT6 (signal transducer and activator of transcription 6) protein facilitates T-helper cell 2 (Th2) mediated responses that control IgE-mediated atopic diseases such as asthma. We have identified compounds that bind to STAT6 and inhibit STAT6 tyrosine phosphorylation induced by IL-4. In the bronchial epithelial cell line BEAS-2B, compound (R)-84 inhibits the secretion of eotaxin-3, a chemokine eliciting eosinophil infiltration. (R)-84 appears to prevent STAT6 from assuming the active dimer configuration by directly binding the protein and inhibiting tyrosine phosphorylation.

DOI: 10.1016/j.bmc.2011.12.006

Cite this paper

@article{Zhou2012STAT6PI, title={STAT6 phosphorylation inhibitors block eotaxin-3 secretion in bronchial epithelial cells.}, author={Li Zhou and Tomohiko Kawate and Xiaorong Liu and Young Bae Kim and Yajuan Zhao and Guohong Feng and Julian Banerji and Huw M. Nash and Charles E Whitehurst and Satish Jindal and Arshad Siddiqui and Brian Seed and Jia Liu Wolfe}, journal={Bioorganic & medicinal chemistry}, year={2012}, volume={20 2}, pages={750-8} }