| Autor: |
Faltynek, Connie, Wang, Su, Miller, Deborah, Mauvais, Patricia, Gauvin, Bruce, Reid, John, Xie, Wen, Hoekstra, Susan, Juniewicz, Paul, Sarup, Jay, Lehr, Ruth, Sawutz, David, Murphy, Dennis |
| Zdroj: |
Journal of Enzyme Inhibition; 1995, Vol. 9 Issue: 2 p111-122, 12p |
| Abstrakt: |
A new p56idk tyrosine kinase inhibitor WIN 61651 [1,4-dihydro-7-(4-methyl-1-piperizinyl)-1-(4-(4-methyl-1-piperizinyl))phenyl-4-oxo-3-quinolinecarboxamide) is described. WIN 61651, which is competitive with AP, demonstrates selectivity for the lymphoid restricted tyrosine kinase p56lck over serine/threonine kinases, such as protein kinase C and protein kinase A, and over some other tyrosine kinases, including erbB2, epidermal growth factor receptor, and insulin receptor; however, it is equipotent for inhibition of p56lck and the platelet derived growth factor receptor tyrosine kinases. WIN 61651 inhibits p56lck activity in cell-free assays, tyrosine kinase activity in a T lymphocytic cell line, and T cell activation, as measured by IL-2 production by purified CD4 positive peripheral blood T lymphocytes and the mixed lymphocyte reaction. WIN 61651 constitutes a new tool for studies on the role for tyrosine kinases in lymphocyte function. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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