ArticleScientific reports2015
Selective targeting of nuclear receptor FXR by avermectin analogues with therapeutic effects on nonalcoholic fatty liver disease.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 45 citations in OpenAlex.
- Farnesoid X receptor‑driven metabolic plasticity: Bridging physiological adaptation and malignant transformation in lipid handling (Review).International journal of molecular medicine · 2025Review
- New High-Throughput Screen Discovers Novel Ligands of Full-Length Nuclear Receptor LRH-1.ACS chemical biology · 2023Article
- Biomimetic Total Synthesis and the Biological Evaluation of Natural Product (-)-Fargesone A as a Novel FXR Agonist.JACS Au · 2022Article
- Natural Product 2-Oxokolavenol Is a Novel FXR Agonist.Molecules (Basel, Switzerland) · 2022Article
- Ivermectin Attenuates CClInternational journal of molecular sciences · 2022Article
- Environmental Chemical Contribution to the Modulation of Bile Acid Homeostasis and Farnesoid X Receptor Signaling.Drug metabolism and disposition: the biological fate of chemicals · 2022Article
- Repositioning Ivermectin for Covid-19 treatment: Molecular mechanisms of action against SARS-CoV-2 replication.Biochimica et biophysica acta. Molecular basis of disease · 2022Review
- Isthmin-1 is an adipokine that promotes glucose uptake and improves glucose tolerance and hepatic steatosis.Cell metabolism · 2021Article
- A Novel Dual Drug Approach That Combines Ivermectin and Dihydromyricetin (DHM) to Reduce Alcohol Drinking and Preference in Mice.Molecules (Basel, Switzerland) · 2021Article
- Ivermectin: An Anthelmintic, an Insecticide, and Much More.Trends in parasitology · 2021Review
- Bile Acids as a New Type of Steroid Hormones Regulating Nonspecific Energy Expenditure of the Body (Review).Sovremennye tekhnologii v meditsine · 2021Review
- Oxidative Stress in NAFLD: Role of Nutrients and Food Contaminants.Biomolecules · 2020Review
- Repositioning an Immunomodulatory Drug Vidofludimus as a Farnesoid X Receptor Modulator With Therapeutic Effects on NAFLD.Frontiers in pharmacology · 2020Article
- Tropifexor-Mediated Abrogation of Steatohepatitis and Fibrosis Is Associated With the Antioxidative Gene Expression Profile in Rodents.Hepatology communications · 2019Article
- Molecular tuning of farnesoid X receptor partial agonism.Nature communications · 2019Article
- Review
- Bile-ology: from bench to bedside.Journal of Zhejiang University. Science. B · 2019Review
- Permethrin and ivermectin modulate lipid metabolism in steatosis-induced HepG2 hepatocyte.Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association · 2019Article
- Identification of FDA-approved drugs targeting the Farnesoid X Receptor.Scientific reports · 2019Article
- The transcription factor NHR-8: A new target to increase ivermectin efficacy in nematodes.PLoS pathogens · 2019Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Non-alcoholic fatty liver disease (NAFLD) has become a predictive factor of death from many diseases. Farnesoid X receptor (FXR) is an ideal target for NAFLD drug development due to its crucial roles in lipid metabolism. The aim of this work is to examine the molecular mechanisms and functional roles of FXR modulation by avermectin analogues in regulating metabolic syndromes like NAFLD. We found that among avermectin analogues studied, the analogues that can bind and activate FXR are effective in regulating metabolic parameters tested, including reducing hepatic lipid accumulation, lowering serum cholesterol and glucose levels, and improving insulin sensitivity, in a FXR dependent manner. Mechanistically, the avermectin analogues that interact with FXR exhibited features as partial agonists, with distinctive properties in modulating coregulator recruitment. Structural features critical for avermectin analogues to selectively bind to FXR were also revealed. This study indicated that in addition to antiparasitic activity, avermectin analogues are promising drug candidates to treat metabolism syndrome including NAFLD by directly targeting FXR. Additionally, the structural features that discriminate the selective binding of FXR by avermectin analogues may provide a unique safe approach to design drugs targeting FXR signaling.
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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.