PCSK9:心血管疾病相关治疗靶点研究进展

Q2 Pharmacology, Toxicology and Pharmaceutics Current Bioactive Compounds Pub Date : 2023-09-30 DOI:10.2174/0115734072270060230921093431
Sonia Singh, Manas Kumar Jha
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引用次数: 0

摘要

蛋白转化酶枯草菌素/酶蛋白9型被认为是一种酶原,广泛存在于肝脏中。PCSK9在血浆循环中被发现,它附着在细胞表面的低密度脂蛋白(LDL)受体上,被内化,随后指导受体被溶酶体降解。自然或有机的调查发现PCSK9基因变异,产生高水平的血浆LDL胆固醇偏差和不同的动脉粥样硬化比例因子,释放了大量的药物以及生物和生命科学研究。我们对PCSK9生理控制的理解取得了重大进展,导致了PCSK9生物抑制剂的发展,现在可以购买。这些抑制剂降低了LDL胆固醇水平,并改善了其他心血管结果。目前的手稿将展示PCSK9的快速发展,从它作为一种新基因的发现,到它作为治疗靶点的使用,接着是它在动物和人类身上的测试,最后,它在结果试验和临床应用中的使用。
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Review on PCSK9: A Pertinent Therapeutic Target in Cardiovascular Disease
A Proprotein convertase subtilisin/kexin type-9 is considered a zymogen, extensively found in the liver. PCSK9 is found in circulation in the plasma, where it attaches to low-density lipoprotein (LDL) receptors on the cell surface, is internalized, and subsequently directs the receptors to be degraded by lysosomes. Investigations of naturally or organically found PCSK9 gene variations, which generated high levels of plasma LDL cholesterol deviations and varied atherosclerosis proportion factors, released floods of pharmaceutical along with biological and live sciences research into the world. Significant advances in our understanding of the physiological control of PCSK9 led quickly to the development of biological inhibitors of PCSK9 that are now available for purchase. These inhibitors decreased LDL cholesterol levels with other improved cardiovascular outcomes. The current manuscript will show the rapid development of PCSK9, beginning with its discovery as a novel gene and progressing through its use as a therapeutic target, followed by its testing on animals and humans and, eventually, its use in outcome trials and clinical applications.
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来源期刊
Current Bioactive Compounds
Current Bioactive Compounds Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.90
自引率
0.00%
发文量
112
期刊介绍: The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.
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