Proprotein convertase subtilisin kexin like type 9 (PCSK9) has since its discovery been a key protein target for the modulation of LDL cholesterol. The interest in PCSK9 has grown even more with the positive clinical trial outcomes in cardiovascular disease recently reported for two PCSK9 antibodies. Currently, there are no PCSK9 small molecule programs active in clinical development. However, there has been a steady increase in publications and patent applications within the PCSK9 small molecule field. This digest will provide a summary of small molecule and peptide PCSK9 modulators reported both in scientific journals and in patent applications, most of them originating from the last 3–4 years. As such, this digest will serve as an introduction to the field and assist further identification and discovery of small molecule PCSK9 modulators.

自从发现像9型前蛋白转化酶枯草杆菌蛋白酶kexin（PCSK9）以来，它一直是调节LDL胆固醇的关键蛋白靶标。随着最近报道的两种PCSK9抗体在心血管疾病方面的积极临床试验结果，人们对PCSK9的兴趣日益增长。当前，没有在临床开发中活跃的PCSK9小分子程序。但是，PCSK9小分子领域内的出版物和专利申请一直在稳定增长。该摘要将总结科学期刊和专利申请中报道的小分子和肽PCSK9调节剂，其中大多数来自最近3-4年。这样，该文摘将作为该领域的简介，并有助于进一步鉴定和发现小分子PCSK9调节剂。