NDLI: SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase

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SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase

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SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Anderson, D. W. Bennett, B. L. Pierce, S. Satoh, Y. Bhagwat, S. S. Sakata, S. T. Xu, W. Motiwala, A. O'leary, E. C. Murray, B. W. Sasaki, D. T. Leisten, J. C. Manning, A. M.
Description	Author Affiliation: Bennett BL ( Signal Research Division, Celgene Corporation, 5555 Oberlin Drive, San Diego, CA 92121 USA. bbennett@signalpharm.com);
Abstract	Jun N-terminal kinase (JNK) is a stress-activated protein kinase that can be induced by inflammatory cytokines, bacterial endotoxin, osmotic shock, UV radiation, and hypoxia. We report the identification of an anthrapyrazolone series with significant inhibition of JNK1, -2, and -3 (K(i) = 0.19 microM). SP600125 is a reversible ATP-competitive inhibitor with >20-fold selectivity vs. a range of kinases and enzymes tested. In cells, SP600125 dose dependently inhibited the phosphorylation of c-Jun, the expression of inflammatory genes COX-2, IL-2, IFN-gamma, TNF-alpha, and prevented the activation and differentiation of primary human CD4 cell cultures. In animal studies, SP600125 blocked (bacterial) lipopolysaccharide-induced expression of tumor necrosis factor-alpha and inhibited anti-CD3-induced apoptosis of CD4(+) CD8(+) thymocytes. Our study supports targeting JNK as an important strategy in inflammatory disease, apoptotic cell death, and cancer.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	24
Volume Number	98
Language	English
Publisher	National Academy of Sciences
Publisher Date	2001-11-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Anthracenes Pharmacology Enzyme Inhibitors Mitogen-Activated Protein Kinases Antagonists & Inhibitors Pyrazolones Adenosine Triphosphate Metabolism Animals Chemistry Anthraquinones Binding, Competitive CD4-Positive T-Lymphocytes Cytology Drug Effects Immunology Cell Differentiation Cells, Cultured Cytokines Gene Expression JNK Mitogen-Activated Protein Kinases Jurkat Cells Lymphocyte Activation Mice Mice, Inbred C57BL Molecular Structure Monocytes Protein Kinase Inhibitors Pyrazoles Structure-Activity Relationship Tumor Necrosis Factor-alpha Biosynthesis Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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