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Beta adrenergic receptor kinase carboxyl-terminus
Beta adrenergic receptor kinase carboxyl-terminus (also βARKct) is a peptide composed of the last 194 amino acid residues of the carboxyl-terminus of beta adrenergic receptor kinase 1 (βARK1). It binds the βγ subunits of G proteins located in the plasma membrane of cells. It is currently an experimental gene therapy for the treatment of heart failure.
== Heart Failure ==
During heart failure, the heart is not able to pump enough blood to the rest of the body and will begin to undergo processes in order to compensate for its decreased function. These processes will attempt to increase the heart’s output; however, the heart may become overstressed and eventually dysfunctional as a result. The sympathetic nervous system increases norepinephrine release to stimulate β-adrenergic receptors (βARs) located on heart cell (cardiomyocyte) membranes to increase the heart’s rate and force of contraction. If the heart is already stressed or damaged, this will cause the heart to work above its capacity.〔 Continuous stimulation of the βARs leads to the activation of βARK1 which phosphorylates βARs to decrease their response to norepinephrine and other catecholamines. βARs are downregulated as a result, decreasing the control over the heart’s rate and force of contraction. A cycle begins as more norepinephrine is produced in an attempt to stimulate the heart to contract.
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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