IndraLab

Statements

ML277 inhibits KCNQ1. 3 / 3
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"It is believed that ML277 inhibits the voltage dependent inactivation kinetics of KCNQ1 to contribute to the augmentation of current amplitude while the hyperpolarizing shift of V (1/2) could significantly increase the maximal conductance [XREF_BIBR]."
25889101
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"It has been previously shown that ML277 prevents inactivation in KCNQ1 and that this is one of the mechanisms by which the drug increases current amplitude ."
35768468
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"While mutations of these residues did reduce the increase in KCNQ1 current amplitude by ML277 to variable degrees (albeit smaller than the mutants we identified), all but two still responded to ML277 (e.g., R243Q and F339A showed a greater than 50% increase in current amplitude) and showed the characteristic slower deactivation kinetics."
35957984