ArticleScientific reports2016
Lupin Peptides Modulate the Protein-Protein Interaction of PCSK9 with the Low Density Lipoprotein Receptor in HepG2 Cells.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 82 citations in OpenAlex.
- Fraisinib in a Shell: Liposomal Encapsulation of a GARS1 Inhibitor for Controlled Anticancer Delivery.AAPS PharmSciTech · 2026Article
- Repurposed drugs as PCSK9-LDLR disruptors for lipid lowering and cardiovascular disease therapeutics.Molecular diversity · 2025Article
- The Emerging Role of PCSK9 in the Pathogenesis of Alzheimer's Disease: A Possible Target for the Disease Treatment.International journal of molecular sciences · 2024Review
- The contradictory role of febuxostat in ABCG2 expression and potentiating hypericin-mediated photodynamic therapy in colorectal cancers.Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology · 2024Article
- Quantifying Imaging Agent Binding and Dissociation in 3-D Cancer Spheroid Tissue Culture Using Paired-Agent Principles.Annals of biomedical engineering · 2024Article
- Olive (Nutrients · 2024Article
- Computational Design, Synthesis, and Biological Evaluation of Diimidazole Analogues Endowed with Dual PCSK9/HMG-CoAR-Inhibiting Activity.Journal of medicinal chemistry · 2023Article
- Brazilin fromAdvances in pharmacological and pharmaceutical sciences · 2023Article
- Computational Design and Biological Evaluation of Analogs of Lupin Peptide P5 Endowed with Dual PCSK9/HMG-CoAR Inhibiting Activity.Pharmaceutics · 2022Article
- Potential dual inhibitors of PCSK-9 and HMG-R from natural sources in cardiovascular risk management.EXCLI journal · 2022Review
- Article
- Lupin-Derived Bioactive Peptides: Intestinal Transport, Bioavailability and Health Benefits.Nutrients · 2021Review
- The Role of Bioactive Peptides in Diabetes and Obesity.Foods (Basel, Switzerland) · 2021Review
- Beneficial Effects of Soybean-Derived Bioactive Peptides.International journal of molecular sciences · 2021Review
- Nanostructure, Self-Assembly, Mechanical Properties, and Antioxidant Activity of a Lupin-Derived Peptide Hydrogel.Biomedicines · 2021Article
- Article
- Assessment of the Multifunctional Behavior of Lupin Peptide P7 and Its Metabolite Using an Integrated Strategy.Journal of agricultural and food chemistry · 2020Article
- From methylene bridged diindole to carbonyl linked benzimidazoleindole: Development of potent and metabolically stable PCSK9 modulators.European journal of medicinal chemistry · 2020Article
- Analysis of Narrow-Leaf Lupin Proteins in Lupin-Enriched Pasta by Untargeted and Targeted Mass Spectrometry.Foods (Basel, Switzerland) · 2020Article
- In Vitro Assay of Quinoa (Chenopodium quinoa Willd.) and Lupin (Lupinus spp.) Extracts on Human Platelet Aggregation.Plant foods for human nutrition (Dordrecht, Netherlands) · 2020Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Proprotein convertase subtilisin/kexin type 9 (PCSK9) has been recently identified as a new useful target for hypercholesterolemia treatment. This work demonstrates that natural peptides, deriving from the hydrolysis of lupin protein and absorbable at intestinal level, are able to inhibit the protein-protein interaction between PCSK9 and the low density lipoprotein receptor (LDLR). In order to sort out the best potential inhibitors among these peptides, a refined in silico model of the PCSK9/LDLR interaction was developed. Docking, molecular dynamics (MD) simulations and peptide binding energy estimations, by MM-GBSA approach, permitted to select the two best candidates among tested peptides that were synthesized and evaluated for their inhibitory activity. The most active was P5 that induced a concentration dependent inhibition of the PCSK9-LDLR binding, with an IC50 value equal to 1.6 ± 0.33 μM. Tested at a 10 μM concentration, this peptide increased by 66 ± 21.4% the ability of HepG2 cells to take up LDL from the extracellular environment.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.