PMID: 8583249Jan 1, 1995Paper

Inhibition of T lymphocyte activation by a novel p56lck tyrosine kinase inhibitor

Journal of Enzyme Inhibition
C R FaltynekJ Sarup

Abstract

A new p56lck tyrosine kinase inhibitor WIN 61651 [1,4-dihydro-7-(4-methyl-1-piperizinyl)-1-(4-(4-methyl-1-piperi zinyl))phenyl- 4-oxo-3-quinolinecarboxamide) is described. WIN 61651, which is competitive with ATP, 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.

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Citations

Dec 1, 1996·Tissue Antigens·J GuardiolaS Sartoris
Nov 20, 2002·The Journal of Pharmacology and Experimental Therapeutics·Stephen Rapecki, Rodger Allen
Jan 31, 2014·Molecular Biology of the Cell·Kazumasa OhashiKensaku Mizuno

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