title: Activation of human ether-a-go-go related gene (hERG) potassium channels by small molecules.
abstract: Human ether-a-go-go related gene (hERG) potassium (K(+)) channels play a critical role in cardiac action potential repolarization. Mutations that reduce hERG conductance or surface expression may cause congenital long QT syndrome (LQTS). However, the channels can be inhibited by structurally diverse small molecules, resulting in an acquired form of LQTS. Consequently, small molecules that increase the hERG current may be of value for treatment for LQTS. So far, nine hERG activators have been reported. The aim of this review is to discuss recent advances concerning the identification and action mechanism of hERG activators.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Ping-zheng
authors.initials: PZ
authors.lastname: Zhou
authors.forename: Joseph
authors.initials: J
authors.lastname: Babcock
authors.forename: Lian-qing
authors.initials: LQ
authors.lastname: Liu
authors.forename: Min
authors.initials: M
authors.lastname: Li
authors.forename: Zhao-bing
authors.initials: ZB
authors.lastname: Gao
mesh_terms: D000818:Animals; D001665:Binding Sites; D051638:Ether-A-Go-Go Potassium Channels / Q000235:genetics / Q000378:metabolism* / Q000502:physiology; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects; D008133:Long QT Syndrome / Q000151:congenital / Q000188:drug therapy / Q000378:metabolism*; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D051638:Ether-A-Go-Go Potassium Channels; D054852:Small Molecule Libraries