Oral, anti-inflammatory activity of a potent, selective, protein kinase C inhibitor
| Autor: | D. Bradshaw, Elliott Lh, Davis Peter David, T. A. Griffiths, John S. Nixon, Hill Christopher Huw, S. E. Wilkinson, Lawton Geoffrey, J. Wadsworth, D. Westmacott, A. D. Sedgwick, M. J. Mulqueen, H. Kumar |
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| Rok vydání: | 1992 |
| Předmět: |
Blood Platelets
Male Indoles CD3 Complex Phosphorylase Kinase medicine.drug_class T-Lymphocytes Immunology Administration Oral Down-Regulation In Vitro Techniques Biology Mitogen-activated protein kinase kinase Toxicology MAP2K7 Maleimides Mice medicine Animals Edema Humans Pharmacology (medical) ASK1 c-Raf Protein kinase A Protein Kinase C Pharmacology MAP kinase kinase kinase Anti-Inflammatory Agents Non-Steroidal Cyclin-dependent kinase 2 Protein kinase inhibitor Rats Biochemistry biology.protein Cattle Female Rabbits |
| Zdroj: | Agents and Actions. 37:85-89 |
| ISSN: | 1420-908X 0065-4299 |
| Popis: | The protein kinase C family of enzymes is thought to be important in mediating signal transduction. Ro 31-8830 is a novel, potent inhibitor of protein kinase C, derived from the non-selective protein kinase inhibitor staurosporine. In this paper we demonstrate the selectivity of Ro 31-8830 for protein kinase C over other protein kinases and its ability to inhibit protein kinase-C-mediated events in platelets and lymphocytes. In addition, we describe a novel system for the in vivo evaluation of inhibitors of protein kinase C, and we demonstrate the oral anti-inflammatory activity of Ro 31-8830. This finding has implications for the treatment of inflammatory disorders in the clinic. |
| Databáze: | OpenAIRE |
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