A selective small-molecule inhibitor of c-Jun N-terminal kinase 1.
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.
Mesh Terms:
Aniline Compounds, Animals, Cells, Cultured, Embryo, Mammalian, Humans, Mice, Mice, Knockout, Mitogen-Activated Protein Kinase 10, Mitogen-Activated Protein Kinase 8, Mitogen-Activated Protein Kinase 9, Phosphorylation, Protein Kinase Inhibitors, Pyrazoles, Ultraviolet Rays
Aniline Compounds, Animals, Cells, Cultured, Embryo, Mammalian, Humans, Mice, Mice, Knockout, Mitogen-Activated Protein Kinase 10, Mitogen-Activated Protein Kinase 8, Mitogen-Activated Protein Kinase 9, Phosphorylation, Protein Kinase Inhibitors, Pyrazoles, Ultraviolet Rays
FEBS Lett.
Date: Jul. 07, 2009
PubMed ID: 19527717
View in: Pubmed Google Scholar
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