[HERG K+ channel, the target of anti-arrhythmias drugs].
Rapidly activating component of delayed rectifier potassium current (I(Kr)) plays a key role in the repolarization phase of cardiac action potential. Human ether-a-go-go-related gene (HERG) encodes the alpha subunit of this potassium channel. Mutations of HERG gene induce genetic long QT syndrome (LQTS). Furthermore, I(Kr)/HERG is the target of some drugs which may cause cardiac QT interval prolongation. Some other drugs with different chemical structures also may block the channel and prolong QT interval, which even developed into acquired arrhythmias. This review summarized the recent progress of structure, gating mechanisms and functions of I(Kr)/HERG channel, I(Kr)/HERG related arrhythmias, interaction between K+ channel and drugs, and strategies of grading-up the I(Kr)/HERG target.
Guan
Feng-ying
FY
Department of Pharmacology, School of Basic Medical Sciences, Jilin University, Changchun 130021, China.
Yang
Shi-jie
SJ
D000889:Anti-Arrhythmia Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D001145:Arrhythmias, Cardiac / Q000188:drug therapy* / Q000378:metabolism; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics* / Q000378:metabolism; D006801:Humans; D015640:Ion Channel Gating; D008133:Long QT Syndrome / Q000188:drug therapy / Q000209:etiology* / Q000235:genetics / Q000378:metabolism; D009154:Mutation; D026902:Potassium Channel Blockers / Q000494:pharmacology
D000889:Anti-Arrhythmia Agents; D051638:Ether-A-Go-Go Potassium Channels; D026902:Potassium Channel Blockers