ArticleJournal of enzyme inhibition and medicinal chemistry2022
Discovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors.
Article in Journal of enzyme inhibition and medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed, 9 citations in OpenAlex.
- Discovery of Novel PCSK9-LDLR PPI Inhibitors by a Structural Modification Approach.Drug development research · 2026Article
- A novel small-molecule PCSK9 inhibitor E28362 ameliorates hyperlipidemia and atherosclerosis.Acta pharmacologica Sinica · 2024Article
- Research on Hepatocyte Regulation of PCSK9-LDLR and Its Related Drug Targets.Chinese journal of integrative medicine · 2024Review
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Authors and funding
4 authors at 1 institution in 1 country.
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Abstract
Proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as a novel therapeutic target for the development of cholesterol-lowering drugs. In the discovery of PCSK9/LDLR (low-density lipoprotein receptor) protein-protein interaction (PPI) impairing small molecules, a total of 47 phenylbenzo[d][1,3] dioxole-based compounds were designed and synthesised. The result revealed that the 4-chlorobenzyl substitution in the amino group is important for the PPI disrupting activity. In the hepatocyte-based functional tests, active compounds such as
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