Key result
In HEK-293 cells, hSKCa1 channels are inhibited by genistein, T25, and AG556 via EGFR tyrosine kinase inhibition, which is related to the phosphorylation of Tyr(109) in the N-terminus.
EGFR tyrosine kinase regulates hSKCa1 channels via phosphorylation of Tyr(109), which may affect electrical activity in myocardium and other tissues.
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May affect myocardial electrical activity; hypothesis-generating for EGFR inhibitor effects on cardiac electrophysiology.
Wu et al. (2013) studied this question. PTK inhibitors (genistein, T25, AG556) was evaluated on hSKCa1 current and tyrosine phosphorylation level. In HEK-293 cells, hSKCa1 channels are inhibited by genistein, T25, and AG556 via EGFR tyrosine kinase inhibition, which is related to the phosphorylation of Tyr(109) in the N-terminus.
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