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HERG
hERG (the human '' Ether-à-go-go''-Related Gene) is a gene () that codes for a protein known as Kv11.1, the alpha subunit of a potassium ion channel. This ion channel (sometimes simply denoted as 'hERG') is best known for its contribution to the electrical activity of the heart that coordinates the heart's beating (i.e., the hERG channel mediates the repolarizing ''I''Kr current in the cardiac action potential). When this channel's ability to conduct electrical current across the cell membrane is inhibited or compromised, either by application of drugs or by rare mutations in some families, it can result in a potentially fatal disorder called long QT syndrome; a number of clinically successful drugs in the market have had the tendency to inhibit hERG, and create a concomitant risk of sudden death, as a side-effect, which has made hERG inhibition an important antitarget that must be avoided during drug development. hERG has also been associated with modulating the functions of some cells of the nervous system〔
〕 and with establishing and maintaining cancer-like features in leukemic cells.
== Function ==
hERG forms the major portion of one of the ion channel proteins (the 'rapid' delayed rectifier current (''I''Kr)) that conducts potassium (K+) ions out of the muscle cells of the heart (cardiac myocytes), and this current is critical in correctly timing the return to the resting state (repolarization) of the cell membrane during the cardiac action potential.〔 Sometimes, when referring to the pharmacological effects of drugs, the terms "hERG channels" and ''I''Kr are used interchangeably, but, in the technical sense, "hERG channels" can be made only by scientists in the laboratory; in formal terms, the naturally occurring channels in the body that include hERG are referred to by the name of the electrical current that has been measured in that cell type, so, for example, in the heart, the correct name is ''I''Kr. This difference in nomenclature becomes clearer in the controversy as to whether the channels conducting ''I''Kr include other subunits (e.g., beta subunits〔 〕) or whether the channels include a mixture of different types (isoforms) of hERG, but, when the originally-discovered form of hERG is experimentally transferred into cells that previously lacked hERG (i.e., heterologous expression), a potassium ion channel is formed, and this channel has many signature features of the cardiac 'rapid' delayed rectifier current (''I''Kr), including ''I''Kr's inward rectification that results in the channel producing a 'paradoxical resurgent current' in response to repolarization of the membrane.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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