Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 6 (STAT6) with Cell-Permeable, Phosphatase-Stable Phosphopeptide Mimics Potently Inhibits Tyr641 Phosphorylation and Transcriptional Activity.

@article{Mandal2015TargetingTS,
  title={Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 6 (STAT6) with Cell-Permeable, Phosphatase-Stable Phosphopeptide Mimics Potently Inhibits Tyr641 Phosphorylation and Transcriptional Activity.},
  author={P. Mandal and Pietro Morlacchi and J. Knight and T. Link and Gilbert R. Lee and R. Nurieva and Divyendu Singh and A. Dhanik and L. Kavraki and D. Corry and J. Ladbury and J. McMurray},
  journal={Journal of medicinal chemistry},
  year={2015},
  volume={58 22},
  pages={
          8970-84
        }
}
Signal transducer and activator of transcription 6 (STAT6) transmits signals from cytokines IL-4 and IL-13 and is activated in allergic airway disease. We are developing phosphopeptide mimetics targeting the SH2 domain of STAT6 to block recruitment to phosphotyrosine residues on IL-4 or IL-13 receptors and subsequent Tyr641 phosphorylation to inhibit the expression of genes contributing to asthma. Structure-affinity relationship studies showed that phosphopeptides based on Tyr631 from IL-4R… Expand
Small molecule targeting of the STAT5/6 Src homology 2 (SH2) domains to inhibit allergic airway disease
Cytosolic delivery of peptidic STAT3 SH2 domain inhibitors.
Structural basis for DNA recognition by STAT6
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