Laboratoire Inserm UMR 1188 DéTROI, Université de La Réunion, Sainte-Clotilde, France.
Laboratoire Inserm UMR 1188 DéTROI, Université de La Réunion, Sainte-Clotilde, France; CHU de La Réunion, Service de Chirurgie Vasculaire, Saint-Denis, France.
Pathology. 2019 Feb;51(2):177-183. doi: 10.1016/j.pathol.2018.10.012. Epub 2018 Dec 4.
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a crucial protein governing the circulating levels of low density lipoprotein-cholesterol (LDL-C), by virtue of its pivotal role in the degradation of the LDL receptor (LDLR). In the last 15 years, in vitro and in vivo studies have allowed our understanding of the physiological role of PCSK9. In the current report, we review the key studies that have established the mode of action of PCSK9, leading to the development of PCSK9 inhibitors for clinical use. Data from clinical trials investigating these therapies clearly and unambiguously demonstrate the safety and efficacy of these new drugs that have the power to dramatically reduce LDL-C and associated cardiovascular diseases.
前蛋白转化酶枯草溶菌素 9（PCSK9）是一种重要的蛋白，通过其在 LDL 受体（LDLR）降解中的关键作用，调节着循环中 LDL-胆固醇（LDL-C）的水平。在过去的 15 年中，体外和体内研究使我们能够了解 PCSK9 的生理作用。在本报告中，我们回顾了确定 PCSK9 作用模式的关键研究，这些研究导致了 PCSK9 抑制剂的开发并应用于临床。临床试验的数据清楚而明确地证明了这些新药的安全性和有效性，它们具有显著降低 LDL-C 和相关心血管疾病的能力。
