The voltage-dependent @entity972 channel, @entity12309 , is modulated by the @entity470 ( @entity470 ) and the @entity2690 receptor @entity669 kinases. When the @entity470 and @entity12309 are coexpressed in HEK 293 cells, acute treatment of the cells with EGF during a patch recording can suppress the @entity12309 current within tens of minutes. This effect appears to be due to @entity669 phosphorylation of the channel, as it is blocked by treatment with the @entity669 kinase inhibitor @entity10912 , or by mutation of the @entity669 at channel @entity535 position 479 to @entity815 . Previous work has shown that there is a large increase in the @entity669 phosphorylation of @entity12309 when it is coexpressed with the @entity470 . Pretreatment of @entity470 and @entity12309 cotransfected cells with EGF before patch recording also results in a decrease in peak @entity12309 current. Furthermore, pretreatment of cotransfected cells with an antibody to the @entity470 ligand binding domain (alpha- @entity470 ), which blocks receptor dimerization and @entity669 kinase activation, blocks the @entity470 -mediated suppression of @entity12309 current. @entity2690 treatment during patch recording also causes an inhibition of @entity12309 current after tens of minutes, while pretreatment for 18 h produces almost total suppression of current. In addition to depressing peak @entity12309 current, EGF treatment produces a speeding of C-type inactivation, while pretreatment with the alpha- @entity470 slows C-type inactivation. In contrast, @entity2690 does not influence C-type inactivation kinetics. Mutational analysis indicates that the EGF-induced modulation of the inactivation rate occurs by a mechanism different from that of the EGF-induced decrease in peak current. Thus, receptor @entity669 kinases differentially modulate the current magnitude and kinetics of a voltage-dependent @entity972 channel.

Modulation of the @entity12309 @entity972 channel by receptor XXXX kinases.

@entity10912 :: ('MESH:C048212', 'Chemical') :: ['erbstatin'] @entity470 :: ('1956', 'Gene') :: ['epidermal growth factor receptor', 'EGFr'] @entity535 :: ('CHEBI:33704', 'Chemical') :: ['amino acid'] @entity2690 :: ('3630', 'Gene') :: ['Insulin', 'insulin'] @entity815 :: ('CHEBI:28044', 'Chemical') :: ['phenylalanine'] @entity972 :: ('MESH:D011188', 'Chemical') :: ['potassium'] @entity12309 :: ('3738', 'Gene') :: ['Kv1.3'] @entity669 :: ('CHEBI:18186', 'Chemical') :: ['tyrosine']
@entity669 :: (CHEBI:18186,Chemical) :: ['tyrosine']
