ArticleMolecular vision2012
Halofuginone down-regulates Smad3 expression and inhibits the TGFbeta-induced expression of fibrotic markers in human corneal fibroblasts.
Article in Molecular vision, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 39 citations in OpenAlex.
- Review
- Traditional medicine meets modern science: Halofuginone's role in combating autoimmune diseases.Journal of natural medicines · 2025Review
- Analysis of Smad3 in the modulation of stromal extracellular matrix proteins in corneal scarring after alkali injury.Molecular vision · 2024Article
- DWN12088, A Prolyl-tRNA Synthetase Inhibitor, Alleviates Hepatic Injury in Nonalcoholic Steatohepatitis.Diabetes & metabolism journal · 2024Article
- O-GlcNAc transferase regulates collagen deposition and fibrosis resolution in idiopathic pulmonary fibrosis.Frontiers in immunology · 2024Article
- Understanding Drivers of Ocular Fibrosis: Current and Future Therapeutic Perspectives.International journal of molecular sciences · 2021Review
- Halofuginone, a promising drug for treatment of pulmonary hypertension.British journal of pharmacology · 2021Article
- Antifibrotic therapy to normalize the tumor microenvironment.Journal of translational medicine · 2020Review
- Involvement of eIF2α in halofuginone-driven inhibition of TGF-β1-induced EMT.Journal of biosciences · 2020Article
- Antifibrotic Therapy Disrupts Stromal Barriers and Modulates the Immune Landscape in Pancreatic Ductal Adenocarcinoma.Cancer research · 2019Article
- Neuronal Transforming Growth Factor beta Signaling via SMAD3 Contributes to Pain in Animal Models of Chronic Pancreatitis.Gastroenterology · 2018Article
- Adult mouse eIF2Bε Arg191His astrocytes display a normal integrated stress response in vitro.Scientific reports · 2018Article
- BRD4 inhibitor JQ1 inhibits and reverses mechanical injury-induced corneal scarring.Cell death discovery · 2018Article
- Anti-fibrotic effect of rosmarinic acid on inhibition of pterygium epithelial cells.International journal of ophthalmology · 2018Article
- Low‑dose halofuginone inhibits the synthesis of type I collagen without influencing type II collagen in the extracellular matrix of chondrocytes.Molecular medicine reports · 2017Article
- Discovery and pharmacological characterization of a new class of prolyl-tRNA synthetase inhibitor for anti-fibrosis therapy.PloS one · 2017Article
- Single-cell analysis reveals IGF-1 potentiation of inhibition of the TGF-β/Smad pathway of fibrosis in human keratocytes in vitro.Scientific reports · 2016Article
- Halofuginone suppresses growth of human uterine leiomyoma cells in a mouse xenograft model.Human reproduction (Oxford, England) · 2016Article
- Development of a novel in vivo corneal fibrosis model in the dog.Experimental eye research · 2016Article
- Halofuginone - the multifaceted molecule.Molecules (Basel, Switzerland) · 2015Review
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
purposeDue to its ability to disrupt transforming growth factor beta (TGF-β) signaling, halofuginone has been successfully used to treat various fibrotic disorders. Here we investigated the antifibrotic potential of halofuginone in human corneal fibroblasts.
methodsHuman corneal fibroblasts were isolated from human donor corneas for in vitro experiments. TGF-β was used to stimulate pro-fibrotic responses from corneal fibroblasts under halofuginone treatment. The expression of alpha smooth muscle actin (α-SMA) and fibronectin was analyzed by western blots. Phalloidin toxin was used to stain cultures for stress fiber assemblies. Quantitative reverse transcription PCR (qRT-PCR) and immunostaining were used to analyze the expression of type I collagen mRNA and protein, respectively. The expression of Smad2, Smad3, phospho-Smad2, and phospho-Smad3 was determined by western blots.
resultsHalofuginone was well tolerated by human corneal fibroblasts up to 10 ng/ml as demonstrated by a cell viability assay. At this concentration, TGF-β-induced expression of the fibrotic markers α-SMA, fibronectin, and type I collagen was significantly reduced. Interestingly, under our experimental conditions, halofuginone treatment led to reduced protein expression of Smad3, which was both dose- and time-dependent.
conclusionsOur results suggest that halofuginone may exert its antifibrotic effects in the cornea via a novel molecular mechanism and may be used as an antifibrotic agent for corneal fibrosis treatment.
Indexed as
Identifiers
22393274PMC3291522W2096522371What OpenQuestion holds
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.