Recent advances of dual FGFR inhibitors as a novel therapy for cancer
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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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].”
From Combination strategies with PD-1/PD-L1 blockade: current advances and future directions (2022) · cites this paper as [233]
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GZD824 as a FLT3, FGFR1 and PDGFRα Inhibitor Against Leukemia In Vitro and In Vivo
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Up-Regulated FGFR1 Expression as a Mediator of Intrinsic TKI Resistance in EGFR-Mutated NSCLC
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FGFR antagonist induces protective autophagy in FGFR1-amplified breast cancer cell
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Metabolic Chiral Inversion of Brivanib and Its Relevance to Safety and Pharmacology
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Combination strategies with PD-1/PD-L1 blockade: current advances and future directions
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Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R
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NAE modulators: A potential therapy for gastric carcinoma
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Current insights and barriers in FGFR-mediated signaling in lung cancer
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A Review and Update on Therapy of Gastrointestinal Tract Tumors: From the Bench to Clinical Practice
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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
- Licence
- 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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