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Cambridge, MA, United States

Zhou L.,Massachusetts General Hospital | Kawate T.,Massachusetts General Hospital | Liu X.,Massachusetts General Hospital | Kim Y.B.,Massachusetts General Hospital | And 9 more authors.
Bioorganic and Medicinal Chemistry | Year: 2012

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. © 2011 Elsevier Ltd. All rights reserved.

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