ArticleActa pharmacologica Sinica2024
A novel small-molecule PCSK9 inhibitor E28362 ameliorates hyperlipidemia and atherosclerosis.
Article in Acta pharmacologica Sinica, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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Who cites it
36 citing papers in PubMed.
- The effect of empagliflozin on inflammation and oxidative stress in patients undergoing percutaneous coronary intervention, a randomized controlled trial.Scientific reports · 2026Trial
- A whole-animal phenotypic drug screen identifies suppressors of atherogenic lipoproteins.eLife · 2026Article
- The Statin Paradox: Drivers and Consequences of Therapy Discontinuation.Metabolites · 2026Review
- Identification and evaluation of a lipid-lowering small compound as a PCSK9 inhibitor.Journal of advanced research · 2026Article
- Advances in chrysin research for cardiovascular disorders: mechanistic insights and therapeutic prospects.Molecular biology reports · 2026Review
- PROTAC-mediated PCSK9 degradation attenuates atherosclerosis and improves plaque composition via suppression of NF-κB/TNF-α pathway.BMC medicine · 2026Article
- Uric Acid and Uric Acid Index in Predicting Coronary Artery Disease, Cerebrovascular Events, and Mortality: A Sex-Stratified Cohort Study.Clinical cardiology · 2026Article
- Discriminating Breast Cancer Patients by Spectral Analysis of Arterial Pulse Waveforms.Cardiovascular engineering and technology · 2026Article
- Artificial intelligence-driven rational design and optimization of a potent terpenoid-derived PCSK9 inhibitor.Molecular diversity · 2026Article
- Validated RP-HPLC and Chromogenic UV Methods for Quantification of Ranolazine in Bulk, Plasma, and Nanoformulation as per ICH Q2(R2) and M10 Guidelines.Chemistry & biodiversity · 2026Article
- Serum PCSK9 level as a potential biomarker relating to age, cholesterol and predicting major adverse cardiovascular event risk in hemodialysis patients.International urology and nephrology · 2026Article
- Mechanisms and structure-activity relationship of hypolipidemic effects of polysaccharides from natural resources: a review.Archives of pharmacal research · 2026Review
- The role of rivaroxaban in the management of coronary artery disease: an overview of five landmark clinical trials.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- Functionalized graphene quantum dots based non-enzymatic sensor for selective tyrosine detection.RSC advances · 2026Article
- Age Modifies the Association Between Smoking and Carotid Artery Plaque: A Cross-Sectional Study in Non-Diabetic Adults.International journal of general medicine · 2026Article
- Machine learning for prediction of newly diagnosed atrial fibrillation after emergency percutaneous coronary intervention during hospitalization in patients with acute ST-segment elevation myocardial infarction: a multi-center prospective study.Frontiers in medicine · 2026Article
- Protective effects of gypenosides on LDL-induced myocardial injury through the miR-223/NLRP3 axis in hyperlipidemia.Frontiers in nutrition · 2026Article
- Drug-Drug Interaction of Chiglitazar with Empagliflozin, Atorvastatin, and Valsartan: An Open-Label, Single-Center, Self-Control, 3-Period Study.Drug design, development and therapy · 2026Article
- Rodent Models for Atherosclerosis.International journal of molecular sciences · 2025Review
- Gold Nanoparticles in Atherosclerosis: A Dual Approach to Diagnosis and Therapy.Molecular imaging and biology · 2025Review
Corrections and comments
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Authors and funding
17 authors.
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Abstract
Proprotein convertase subtilisin/kexin type 9 (PCSK9) binds to the epidermal growth factor precursor homologous domain A (EGF-A) of low-density lipoprotein receptor (LDLR) in the liver and triggers the degradation of LDLR via the lysosomal pathway, consequently leading to an elevation in plasma LDL-C levels. Inhibiting PCSK9 prolongs the lifespan of LDLR and maintains cholesterol homeostasis in the body. Thus, PCSK9 is an innovative pharmacological target for treating hypercholesterolemia and atherosclerosis. In this study, we discovered that E28362 was a novel small-molecule PCSK9 inhibitor by conducting a virtual screening of a library containing 40,000 compounds. E28362 (5, 10, 20 μM) dose-dependently increased the protein levels of LDLR in both total protein and the membrane fraction in both HepG2 and AML12 cells, and enhanced the uptake of DiI-LDL in AML12 cells. MTT assay showed that E28362 up to 80 μM had no obvious toxicity in HepG2, AML12, and HEK293a cells. The effects of E28362 on hyperlipidemia and atherosclerosis were evaluated in three different animal models. In high-fat diet-fed golden hamsters, administration of E28362 (6.7, 20, 60 mg·kg
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