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

被引：16
|
作者：
Yao, Ke [1 ]
Cho, Yong-Yeon [1 ]
Bode, Ann M. [1 ]
Vummenthala, Anuradha [2 ]
Park, Jewn Giew [2 ]
Liu, Kangdong [1 ]
Pang, Yuan-Ping [2 ]
Dong, Zigang [1 ]
机构：
[1] Univ Minnesota, Hormel Inst, Austin, MN 55912 USA
[2] Mayo Clin, Comp Aided Mol Design Lab, Rochester, MN USA
来源：
FEBS LETTERS | 2009年 / 583卷 / 13期
关键词：
AV-7; Small-molecule inhibitor; c-Jun N-terminal kinase inhibitor; c-Jun phosphorylation; Sub-G1; accumulation; SIGNAL-TRANSDUCTION PATHWAY; LUNG-CARCINOMA CELLS; INSULIN-RESISTANCE; JNK; TRANSFORMATION; ACTIVATION; GROWTH; SUPPRESSION; APOPTOSIS; OBESITY;
D O I：
10.1016/j.febslet.2009.06.017
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 summary: MINT-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) (C) 2009 Federation of European Biochemical Societies. Published by Elsevier B. V. All rights reserved.
引用
收藏
页码：2208 / 2212
页数：5
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