Cited by 34Fibroblast Growth Factor ResearchCancer Mechanisms and TherapyLung Cancer Treatments and Mutations

Recent advances of dual FGFR inhibitors as a novel therapy for cancer

Liang, Qi, Wang, Juelan, Zhao, Liyun, Hou, Jun, Hu, Yonghe, Shi, Jianyou·2021·European Journal of Medicinal Chemistry

Abstract

Fibroblast growth factor receptor (FGFR) includes four highly conserved transmembrane receptor tyrosine kinases (FGFR1-4). FGF and FGFR regulate many biological processes, such as angiogenesis, wound healing and tissue regeneration. The abnormal expression of FGFR is related to the tumorigenesis, tumor progression and drug resistance of anti-tumor treatments in many types of tumors. Nowadays there are many anti-cancer drugs targeting FGFR. However, traditional single-target anti-tumor drugs are easy to acquire drug resistance. The therapeutic effect can be enhanced by simultaneously inhibiting FGFR and another target (such as VEGFR, EGFR, PI3K, CSF-1R, etc.). We know drug combination can bring problems such as drug interactions. Therefore, the development of FGFR dual target inhibitors is an important direction. In this paper, we reviewed the research on dual FGFR inhibitors in recent years and made brief comments on them.

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Crossref · 10.1016/j.ejmech.2021.113205

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  • Dysregulated FGF-FGFR signaling participates in cancer development by activating MAPK, PI3K, and PLC-γ pathways.

    “Dysregulated fibroblast growth factor-fibroblast growth factor receptor (FGF-FGFR) signaling participates in cancer development by activating MAPK, PI3K, and PLC-γ pathways [232, 233].”

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Authors
Liang, Q., Wang, J., Zhao, L., Hou, J., Hu, Y., & Shi, J.
Affiliations
  • Southwest Jiaotong University (CN)
  • University of Electronic Science and Technology of China (CN)
Corresponding author
  • Hou, Jun
  • Hu, Yonghe
  • Shi, Jianyou
Venue
European Journal of Medicinal Chemistry
Publisher
Elsevier BV
Published
2021-03
Volume
214
Pages
113205
ISSN
0223-5234 (ISSN-L)
OpenAlex
W3125511051
Cited by
32
References
115
Citations by year
2026: 3 · 2025: 4 · 2024: 10 · 2023: 7 · 2022: 3 · 2021: 5
FWCI
0.71
Type
journal article
Language
en
Open access
closed
Locations
  • European Journal of Medicinal Chemistry (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Sichuan Provincial Administration of Traditional Chinese Medicine
  • Department of Science and Technology of Sichuan Province
  • Health and Family Planning Commission of Sichuan Province
  • National Natural Science Foundation of China
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Fibroblast Growth Factor Research
  • Health Sciences › Medicine › Pathology and Forensic Medicine › Cancer Mechanisms and Therapy
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Keywords
fibroblast growth factor receptor, FGFR inhibitors, dual inhibitors, receptor tyrosine kinase, cancer therapy, drug resistance, combination therapy, VEGFR, EGFR, phosphatidylinositol 3-kinase, CSF1R, angiogenesis, drug interactions
MeSH terms
Antineoplastic Agents, Humans, Neoplasms, Molecular Structure, Receptors, Fibroblast Growth Factor, Protein Kinase Inhibitors

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