Author: Zheng, Yueming; Zhu, Xuejing; Zhou, Pingzheng; Lan, Xi; Xu, Haiyan; Li, Min; Gao, Zhaobing
Title: Hexachlorophene Is a Potent KCNQ1/KCNE1 Potassium Channel Activator Which Rescues LQTs Mutants Document date: 2012_12_12
ID: 1manzf3l_3
Snippet: Recently, a number of activators of KCNQ channels have been reported [8] [9] [10] [11] [12] . However, activators for KCNQ1 are still rare and few are effective on the physiologically relevant KCNQ1/ KCNE1 complex [13] . Two known examples include R-L3 and zinc pyrithione (ZnPy) [13, 14] . Both potentiate homomeric KCNQ1 channel but lack sensitivity to the KCNQ1/KCNE1 complex. To date, only three small molecule activators for the KCNQ1/KCNE1 comp.....
Document: Recently, a number of activators of KCNQ channels have been reported [8] [9] [10] [11] [12] . However, activators for KCNQ1 are still rare and few are effective on the physiologically relevant KCNQ1/ KCNE1 complex [13] . Two known examples include R-L3 and zinc pyrithione (ZnPy) [13, 14] . Both potentiate homomeric KCNQ1 channel but lack sensitivity to the KCNQ1/KCNE1 complex. To date, only three small molecule activators for the KCNQ1/KCNE1 complex have been identified. They are mefenamic acid (MFA), DIDS and phenylboronic acid (PBA). Initially, MFA and DIDS were identified as chloride channel blockers [15] . These compounds strongly potentiate the KCNQ1/ KCNE1 but exhibit little effect on homomeric KCNQ1. In contrast, PBA, an aromatic derivative of boronic acids, potentiates both the homomeric KCNQ1 and the KCNQ1/KCNE1 complex with millimolar effective concentration [16] .
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