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(Received for publication, September 20, 1995) Here, we have studied the activity of a novel protein-tyrosine
kinase inhibitor that is selective for the Src family of tyrosine
kinases. We have focused our study on the effects of this compound on T
cell receptor-induced T cell activation, a process dependent on the
activity of the Src kinases Lck and FynT. This compound is a nanomolar
inhibitor of Lck and FynT, inhibits anti-CD3-induced protein-tyrosine
kinase activity in T cells, demonstrates selectivity for Lck and FynT
over ZAP-70, and preferentially inhibits T cell receptor-dependent
anti-CD3-induced T cell proliferation over non-T cell
receptor-dependent phorbol 12-myristate 13-acetate/interleukin-2
(IL-2)-induced T cell proliferation. Interestingly, this compound
selectively inhibits the induction of the IL-2 gene, but not the
granulocyte-macrophage colony-stimulating factor or IL-2 receptor
genes. This compound offers a useful new tool for examining the role of
the Lck and FynT tyrosine kinases versus ZAP-70 in T cell
activation as well as the role of other Src family kinases in receptor
function.
Volume 271,
Number 2,
Issue of January 12, 1996 pp. 695-701
©1996 by The American Society for Biochemistry and Molecular Biology, Inc.
STUDY OF Lck- AND FynT-DEPENDENT T CELL ACTIVATION
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