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雌激素作用的多样性及组织选择性的发现,促进了选择性雌激素受体调节剂(SERMs)的发展。SERMs是一类雌激素受体的配体,通过组织、信号转导通路或受体亚型特异性的方式产生激动剂或拮抗剂效应。作为雌激素受体的配体,SERMs具有调节心血管功能的作用:扩张冠状动脉、调节缺血损伤和心肌肥大及改善血脂、胆固醇谱等,而且其作用还受到共激活因子、共抑制因子以及雌激素结合蛋白的调控。因此,SERMs的作用表现有组织或通路的特异性。未来SERMs研制的策略是,保持其有益作用,去除不良副反应,使之可应用于冠心病等心血管疾病的防治。
The diversity of estrogen effects and the discovery of tissue selectivity have contributed to the development of selective estrogen receptor modulators (SERMs). SERMs are ligands for a class of estrogen receptors that produce agonist or antagonist effects through tissue, signal transduction pathways, or receptor subtype specificities. As a ligand of estrogen receptor, SERMs have the function of regulating cardiovascular function: dilating coronary artery, regulating ischemic injury and myocardial hypertrophy, improving blood lipid and cholesterol, and its function is also affected by co-activator, co-repressor and Regulation of estrogen binding proteins. Therefore, the role of SERMs is characterized by tissue or pathways. The strategy developed by SERMs in the future is to maintain its beneficial effect and eliminate adverse side effects so that it can be applied to the prevention and treatment of cardiovascular diseases such as coronary heart disease.