摘要
背景:低密度脂蛋白(LDL)受体(LDL- r)是一种跨膜蛋白,在有效的脂质稳态中起着至关重要的作用。各种治疗药物已被用于治疗血脂异常,但治疗靶点的结果仍有争议。 目的:综述和全面了解当前有关LDL-R的概念及其分子特性、代谢途径、影响LDL-R活性的因素和现有的药理学干预手段。此外,还介绍了LDL-R的非脂质相关特性。 方法:从PubMed数据库中提取文献,以识别1984年至2017年间关于LDL-R和治疗药物对血脂异常管理的论文。 结果:我们分析了与LDL-R相关的试剂的基本数据(甾醇调节元件结合蛋白- SREBPs、ARH蛋白、IDOL、甲状腺激素、血液病、kexin9 - PCSK-9、- iii蛋白转化酶subtilisin)以及LDL-R的非脂质相关特性,同时,所有相关的(常见的和新的)药理学干预(他汀类、纤维酸、胆固醇吸收抑制剂、胆汁酸螯合剂和PCSK- 9)也被提及。 结论: LDL-R及其分子特性与脂质内稳态有关,可能为心血管患者设定治疗目标,但这一问题一直存在争议。为了充分了解其特性,并找到可能对胆固醇稳态和各种疾病有益的潜在药物干预,以达到最适当的治疗目标,还需要进一步的研究。
关键词: 低密度脂蛋白受体,脂质代谢平衡,家族性高胆固醇血症,动脉粥样硬化,蛋白转化酶枯草素kexin9 (PCSK-9),甾醇调节元件结合蛋白(SREBPs)。
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