A selective small-molecule inhibitor of c-Jun N-terminal kinase 1 |
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| Authors: | Ke Yao Yong-Yeon Cho Ann M. Bode Jewn Giew Park Yuan-Ping Pang |
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| Affiliation: | a The Hormel Institute, University of Minnesota, 801 16th Ave NE, Austin, MN 55912, United States
b Computer-Aided Molecular Design Laboratory, Mayo Clinic, Rochester, MN, United States |
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| 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.Structured summaryMINT-7148332: JNK3 (uniprotkb:P53779) phosphorylates (MI:0217) c-JUN (uniprotkb:P05412) by protein kinase assay (MI:0424)MINT-7148323: JNK2 (uniprotkb:P45984) phosphorylates (MI:0217) c-JUN (uniprotkb:P05412) by protein kinase assay (MI:0424)MINT-7148314: JNK1 (uniprotkb:P45983) phosphorylates (MI:0217) c-JUN (uniprotkb:P05412) by protein kinase assay (MI:0424) |
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| Keywords: | JNK, c-Jun N-terminal kinase MEF, mouse embryonic fibroblast UVB, ultraviolet B |
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