Liu Gang, Li Si Qi, Hu Ping Ping, Tong Xiao Yong
Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, Chongqing, China.
Diab Vasc Dis Res. 2018 Jul;15(4):322-335. doi: 10.1177/1479164118774313. Epub 2018 May 15.
Sarco(endo)plasmic reticulum calcium adenosine triphosphatase is responsible for transporting cytosolic calcium into the sarcoplasmic reticulum and endoplasmic reticulum to maintain calcium homeostasis. Sarco(endo)plasmic reticulum calcium adenosine triphosphatase is the dominant isoform expressed in cardiac tissue, which is regulated by endogenous protein inhibitors, post-translational modifications, hormones as well as microRNAs. Dysfunction of sarco(endo)plasmic reticulum calcium adenosine triphosphatase is associated with heart failure, which makes sarco(endo)plasmic reticulum calcium adenosine triphosphatase a promising target for heart failure therapy. This review summarizes current approaches to ameliorate sarco(endo)plasmic reticulum calcium adenosine triphosphatase function and focuses on phospholamban, an endogenous inhibitor of sarco(endo)plasmic reticulum calcium adenosine triphosphatase, pharmacological tools and gene therapies.
肌浆(内质)网钙腺苷三磷酸酶负责将胞质钙转运至肌浆网和内质网,以维持钙稳态。肌浆(内质)网钙腺苷三磷酸酶是心脏组织中表达的主要亚型,受内源性蛋白质抑制剂、翻译后修饰、激素以及微小RNA的调控。肌浆(内质)网钙腺苷三磷酸酶功能障碍与心力衰竭相关,这使得肌浆(内质)网钙腺苷三磷酸酶成为心力衰竭治疗的一个有前景的靶点。本综述总结了改善肌浆(内质)网钙腺苷三磷酸酶功能的当前方法,并重点关注受磷蛋白,即肌浆(内质)网钙腺苷三磷酸酶的一种内源性抑制剂、药理学工具和基因疗法。