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Publication : A selective small-molecule inhibitor of c-Jun N-terminal kinase 1.

First Author  Yao K Year  2009
Journal  FEBS Lett Volume  583
Issue  13 Pages  2208-12
PubMed ID  19527717 Mgi Jnum  J:150843
Mgi Id  MGI:3851887 Doi  10.1016/j.febslet.2009.06.017
Citation  Yao K, et al. (2009) A selective small-molecule inhibitor of c-Jun N-terminal kinase 1. FEBS Lett 583(13):2208-12
abstractText  Indiscriminately suppressing total c-Jun N-terminal kinase (JNK) activity is not an appropriate strategy because each JNK appears to have a distinct function in cancer, asthma, diabetes, or Parkinson's disease. Herein, we report that 7-(6-N-phenylaminohexyl)amino-2H-anthra[1,9-cd]pyrazol-6-one (AV-7) inhibited JNK1 activity, but not JNK2 or JNK3. We found that ultraviolet B (UVB) induced c-Jun phosphorylation and sub-G1 accumulation in JNK2(-/-) murine embryonic fibroblasts, which contain an abundance of JNK1, but not JNK2. These results demonstrate that AV-7 is an isoform selective small-molecule inhibitor of JNK1 activity, which might be developed as a therapeutic against diabetes.
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