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  • Title: A selective small-molecule inhibitor of c-Jun N-terminal kinase 1.
    Author: Yao K, Cho YY, Bode AM, Vummenthala A, Park JG, Liu K, Pang YP, Dong Z.
    Journal: FEBS Lett; 2009 Jul 07; 583(13):2208-12. PubMed ID: 19527717.
    Abstract:
    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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