Tyrphostin-induced inhibition of p210bcr-abl tyrosine kinase activity induces K562 to differentiate

M Anafi, A Gazit, A Zehavi, Y Ben-Neriah, A Levitzki - 1993 - ashpublications.org
M Anafi, A Gazit, A Zehavi, Y Ben-Neriah, A Levitzki
1993ashpublications.org
We report on the potency of two Tyrphostin tyrosine kinase blockers, AG 1112 and AG 568,
to inhibit p210bcr-abl tyrosine kinase activity in K562 cells, concomitant with the induction of
erythroid differentiation. AG 568 and especially AG 1112 represent a specific group of
nontoxic protein tyrosine kinase blockers among more than 1,400 tested. These compounds
possess therapeutic potential for purging Philadelphia chromosome-positive cells in
preparation for autologous bone marrow transplantation in chronic myelogenous leukemia.
Abstract
We report on the potency of two Tyrphostin tyrosine kinase blockers, AG 1112 and AG 568, to inhibit p210bcr-abl tyrosine kinase activity in K562 cells, concomitant with the induction of erythroid differentiation. AG 568 and especially AG 1112 represent a specific group of nontoxic protein tyrosine kinase blockers among more than 1,400 tested. These compounds possess therapeutic potential for purging Philadelphia chromosome-positive cells in preparation for autologous bone marrow transplantation in chronic myelogenous leukemia.
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