前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型 (PCSK9) 诱导低密度脂蛋白受体 (LDLR) 降解，导致 LDL 胆固醇血浆浓度升高。因此，抑制 PCSK9 和 LDLR 之间的相互作用是治疗高胆固醇血症的理想治疗目标。适体是 RNA 或单链 DNA 序列，可以根据其二级结构识别其目标。适体对结合靶分子表现出高选择性和亲和力。通过指数富集进行配体系统进化 (SELEX) 是一种生物学方法的组合，用于体外筛选大多数适体。由于其独特的优势，适配体自被发现以来就引起了人们的极大兴趣，并在各个领域得到了广泛的应用。适体已越来越多地用于生物传感器的开发，用于敏感检测病原体、分析物、毒素、药物残留和恶性细胞。此外，与单克隆抗体类似，适体可以作为治疗工具。与某些蛋白质疗法不同，适体不会引发抗体反应，并且它们在 2' 位的修饰糖通常会阻止 Toll 样受体介导的先天免疫反应。本综述的重点是基于适体的 PCSK9 靶向以及适体作为生物传感器和治疗剂的应用。© 2024。作者。

The degradation of low-density lipoprotein receptor (LDLR) is induced by proprotein convertase subtilisin/kexin type 9 (PCSK9), resulting in elevated plasma concentrations of LDL cholesterol. Therefore, inhibiting the interactions between PCSK9 and LDLR is a desirable therapeutic goal for managing hypercholesterolemia. Aptamers, which are RNA or single-stranded DNA sequences, can recognize their targets based on their secondary structure. Aptamers exhibit high selectivity and affinity for binding to target molecules. The systematic evolution of ligands by exponential enrichment (SELEX), a combination of biological approaches, is used to screen most aptamers in vitro. Due to their unique advantages, aptamers have garnered significant interest since their discovery and have found extensive applications in various fields. Aptamers have been increasingly utilized in the development of biosensors for sensitive detection of pathogens, analytes, toxins, drug residues, and malignant cells. Furthermore, similar to monoclonal antibodies, aptamers can serve as therapeutic tools. Unlike certain protein therapeutics, aptamers do not elicit antibody responses, and their modified sugars at the 2'-positions generally prevent toll-like receptor-mediated innate immune responses. The focus of this review is on aptamer-based targeting of PCSK9 and the application of aptamers both as biosensors and therapeutic agents.© 2024. The Author(s).