Chemogenomic identification of Ref-1/AP-1 as a therapeutic target for asthma

  title={Chemogenomic identification of Ref-1/AP-1 as a therapeutic target for asthma},
  author={C{\`u} L{\^e} Nguy{\^e}n and Jia-Ling Teo and Akihisa Matsuda and Masakatsu Eguchi and Emil Y. Chi and William R Henderson and Michael Kahn},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  pages={1169 - 1173}
  • C. Nguyên, J. Teo, M. Kahn
  • Published 24 January 2003
  • Biology, Chemistry
  • Proceedings of the National Academy of Sciences of the United States of America
Asthma is characterized by an oxidant/antioxidant imbalance in the lungs leading to activation of redox-sensitive transcription factors, nuclear factor κB (NF-κB), and activator protein-1 (AP-1). To develop therapeutic strategies for asthma, we used a chemogenomics approach to screen for small molecule inhibitor(s) of AP-1 transcription. We developed a β-strand mimetic template that acts as a reversible inhibitor (pseudosubstrate) of redox proteins. This template incorporates an enedione moiety… 

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