PCSK9
前蛋白转化酶
可欣
低密度脂蛋白受体
前蛋白转化酶类
枯草杆菌素
临床试验
药理学
化学
胆固醇
医学
脂蛋白
生物化学
内科学
酶
作者
Enrico Mario Alessandro Fassi,Andrea Citarella,Marco Albani,Eva Milano,Laura Legnani,Carmen Lammi,Alessandra Silvani,Giovanni Grazioso
标识
DOI:10.1080/13543776.2024.2340569
摘要
Proprotein convertase subtilisin/kexin 9 (PCSK9) plays a crucial role in breaking down the hepatic low-density lipoprotein receptor (LDLR), thereby influencing the levels of circulating low-density lipoprotein cholesterol (LDL-C). Consequently, inhibiting PCSK9 through suitable ligands has been established as a validated therapeutic strategy for combating hypercholesterolemia and cardiovascular diseases.Patent literature claiming novel compounds inhibiting PCSK9 disclosed from 2018 to June 2023 available in the espacenet database, which contains more than 150 million patent documents from over 100 patent-granting authorities worldwide.The undisputable beneficial influence of PCSK9 as a pharmacological target has prompted numerous private and public institutions to patent chemical frameworks as inhibitors of PCSK9. While several compounds have advanced to clinical trials for treating hypercholesterolemia, they have not completed these trials yet. These compounds must contend in a complex market where new, costly, and advanced drugs, such as monoclonal antibodies and siRNA, are prescribed instead of inexpensive and less potent statins.
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