ArticleScientific reports2016
A novel fibroblast growth factor receptor 1 inhibitor protects against cartilage degradation in a murine model of osteoarthritis.
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 21 papers.
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Who cites it
21 citing papers in PubMed, 35 citations in OpenAlex.
- Targeting Chondrocyte Hypertrophy as Strategies for the Treatment of Osteoarthritis.Bioengineering (Basel, Switzerland) · 2025Review
- Integrated Transcriptomic and Proteomic Analyses of Antler Growth and Ossification Mechanisms.International journal of molecular sciences · 2024Article
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- Review
- New developments in the biology of fibroblast growth factors.WIREs mechanisms of disease · 2022Review
- The Extracellular Matrix of Articular Cartilage Controls the Bioavailability of Pericellular Matrix-Bound Growth Factors to Drive Tissue Homeostasis and Repair.International journal of molecular sciences · 2022Review
- Fibroblast growth factor receptor 1-bound extracellular vesicle as novel therapy for osteoarthritis.BioMedicine · 2022Review
- Roles of the fibroblast growth factor signal transduction system in tissue injury repair.Burns & trauma · 2022Review
- Article
- Article
- Pathological mechanism of chondrocytes and the surrounding environment during osteoarthritis of temporomandibular joint.Journal of cellular and molecular medicine · 2021Review
- Fibroblast growth factor signalling in osteoarthritis and cartilage repair.Nature reviews. Rheumatology · 2020Review
- Of mice and men: converging on a common molecular understanding of osteoarthritis.The Lancet. Rheumatology · 2020Review
- FGF/FGFR signaling in health and disease.Signal transduction and targeted therapy · 2020Review
- Article
- Design, synthesis and biological evaluation of 4-bromo-N-(3,5-dimethoxyphenyl)benzamide derivatives as novel FGFR1 inhibitors for treatment of non-small cell lung cancer.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Regulation of energy metabolism in the growth plate and osteoarthritic chondrocytes.Rheumatology international · 2018Review
- Loss ofThe Journal of biological chemistry · 2018Article
- Recent Insights into the Contribution of the Changing Hypertrophic Chondrocyte Phenotype in the Development and Progression of Osteoarthritis.Frontiers in bioengineering and biotechnology · 2018Review
- Increased Activity of the Chondrocyte Translational Apparatus Accompanies Osteoarthritic Changes in Human and Rodent Knee Cartilage.Arthritis & rheumatology (Hoboken, N.J.) · 2017Article
Corrections and comments
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Authors and funding
17 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The attenuated degradation of articular cartilage by cartilage-specific deletion of fibroblast growth factor receptor 1 (FGFR1) in adult mice suggests that FGFR1 is a potential target for treating osteoarthritis (OA). The goal of the current study was to investigate the effect of a novel non-ATP-competitive FGFR1 inhibitor, G141, on the catabolic events in human articular chondrocytes and cartilage explants and on the progression of cartilage degradation in a murine model of OA. G141 was screened and identified via cell-free kinase-inhibition assay. In the in vitro study, G141 decreased the mRNA levels of catabolic markers ADAMTS-5 and MMP-13, the phosphorylation of Erk1/2, JNK and p38 MAPK, and the protein level of MMP-13 in human articular chondrocytes. In the ex vivo study, proteoglycan loss was markedly reduced in G141 treated human cartilage explants. For the in vivo study, intra-articular injection of G141 attenuated the surgical destabilization of the medial meniscus (DMM) induced cartilage destruction and chondrocyte hypertrophy and apoptosis in mice. Our data suggest that pharmacologically antagonize FGFR1 using G141 protects articular cartilage from osteoarthritic changes, and intra-articular injection of G141 is potentially an effective therapy to alleviate OA progression.
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