IndraLab

Statements

SSD609 inhibits KCNQ1. 3 / 3
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"As shown in XREF_FIG, SSD609 reversibly inhibited the channel conductance of I ks (KCNQ1 and KCNE1), specifically affecting the KCNE1 auxiliary subunit, because no inhibition of the KCNQ1 channel expressed in CHO cells was observed."
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"A significantly bigger clinical problem is loss-of-function mutations in KCNE1 and KCNQ1 leading to Long QT Syndrome [64], and hence it will be interesting in future research to examine whether SSD609 can be engineered to agonize rather than inhibit KCNQ1, although in this case, on-target toxicity might be difficult to avoid.3.2."
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"Although SSD609 inhibited KCNQ1 and KCNE3, the distribution of the KCNQ1 and KCNE3 complex in the colon and other non cardiac cells XREF_BIBR precluded any inhibitory effect of SSD609 on KCNQ1 and KCNE3 in the cardiovascular system."
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