Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling
Keloids are common benign cutaneous pathological fibrous proliferation diseases, which are difficult to cure and easily recur. Studies have shown that fibroblast growth factor receptor-1 (FGFR1) was enhanced in pathological fibrous proliferation diseases, such as cirrhosis and idiopathic pulmonary f...
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MDPI AG
2023-12-01
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| Series: | Biomedicines |
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| Online Access: | https://www.mdpi.com/2227-9059/11/12/3220 |
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| author | Shuqia Xu Yongkang Zhu Peng Wang Shaohai Qi Bin Shu |
| author_facet | Shuqia Xu Yongkang Zhu Peng Wang Shaohai Qi Bin Shu |
| author_sort | Shuqia Xu |
| collection | DOAJ |
| description | Keloids are common benign cutaneous pathological fibrous proliferation diseases, which are difficult to cure and easily recur. Studies have shown that fibroblast growth factor receptor-1 (FGFR1) was enhanced in pathological fibrous proliferation diseases, such as cirrhosis and idiopathic pulmonary fibrosis (IPF), suggesting the FGFR1 pathway has potential for keloid treatment. Derazantinib is a selective FGFR inhibitor with antiproliferative activity in in vitro and in vivo models. The present study determined the effects of derazantinib on human keloid fibroblasts (KFs). Cell viability assay, migration assay, invasion assay, immunofluorescence staining, quantitative polymerase chain reaction, Western blot analysis, HE staining, Masson staining, and immunohistochemical analysis were used to analyze the KFs and keloid xenografts. In this study, we found that derazantinib inhibited the proliferation, migration, invasion, and collagen production of KFs in vitro. The transcription and expression of plasminogen activator inhibitor-1 (PAI-1), which is closely related to collagen deposition and tissue fibrosis, was significantly inhibited. Also, derazantinib inhibited the expression of FGFR1 and PAI-1 and reduced the weight of the implanted keloid from the xenograft mice model. These findings suggest that derazantinib may be a potent therapy for keloids via FGFR signaling. |
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| institution | Directory Open Access Journal |
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| language | English |
| last_indexed | 2024-03-08T20:58:50Z |
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| spelling | doaj.art-9cf44ffef928483cb2a1d38bbc97fe412023-12-22T13:55:00ZengMDPI AGBiomedicines2227-90592023-12-011112322010.3390/biomedicines11123220Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR SignalingShuqia Xu0Yongkang Zhu1Peng Wang2Shaohai Qi3Bin Shu4Department of Plastic Surgery, The First Affiliated Hospital of Sun Yat-sen University, Guangzhou 510080, ChinaDepartment of Burn Surgery, The First Affiliated Hospital of Sun Yat-sen University, Guangzhou 510080, ChinaDepartment of Burn Surgery, The First Affiliated Hospital of Sun Yat-sen University, Guangzhou 510080, ChinaDepartment of Burn Surgery, The First Affiliated Hospital of Sun Yat-sen University, Guangzhou 510080, ChinaDepartment of Burn Surgery, The First Affiliated Hospital of Sun Yat-sen University, Guangzhou 510080, ChinaKeloids are common benign cutaneous pathological fibrous proliferation diseases, which are difficult to cure and easily recur. Studies have shown that fibroblast growth factor receptor-1 (FGFR1) was enhanced in pathological fibrous proliferation diseases, such as cirrhosis and idiopathic pulmonary fibrosis (IPF), suggesting the FGFR1 pathway has potential for keloid treatment. Derazantinib is a selective FGFR inhibitor with antiproliferative activity in in vitro and in vivo models. The present study determined the effects of derazantinib on human keloid fibroblasts (KFs). Cell viability assay, migration assay, invasion assay, immunofluorescence staining, quantitative polymerase chain reaction, Western blot analysis, HE staining, Masson staining, and immunohistochemical analysis were used to analyze the KFs and keloid xenografts. In this study, we found that derazantinib inhibited the proliferation, migration, invasion, and collagen production of KFs in vitro. The transcription and expression of plasminogen activator inhibitor-1 (PAI-1), which is closely related to collagen deposition and tissue fibrosis, was significantly inhibited. Also, derazantinib inhibited the expression of FGFR1 and PAI-1 and reduced the weight of the implanted keloid from the xenograft mice model. These findings suggest that derazantinib may be a potent therapy for keloids via FGFR signaling.https://www.mdpi.com/2227-9059/11/12/3220derazantinibfibroblast growth factor receptorkeloid |
| spellingShingle | Shuqia Xu Yongkang Zhu Peng Wang Shaohai Qi Bin Shu Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling Biomedicines derazantinib fibroblast growth factor receptor keloid |
| title | Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling |
| title_full | Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling |
| title_fullStr | Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling |
| title_full_unstemmed | Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling |
| title_short | Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling |
| title_sort | derazantinib inhibits the bioactivity of keloid fibroblasts via fgfr signaling |
| topic | derazantinib fibroblast growth factor receptor keloid |
| url | https://www.mdpi.com/2227-9059/11/12/3220 |
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