Abstract
FGFs and their receptors (FGFRs) are critical for many biologic processes, including angiogenesis, wound healing and tissue regeneration. Aberrations in FGFR signaling are common in cancer, making FGFRs a promising target in antitumor studies. To date, many FGFR inhibitors are being detected in clinical studies, and resistance to some inhibitors has emerged. Understanding the mechanisms of resistance is a fundamental step for further implementation of targeted therapies. In this review, we will describe the basic knowledge regarding FGF/FGFR signaling and categorize the clinical FGFR inhibitors. The mechanisms of resistance to FGFR inhibitors and corresponding strategies of overcoming drug resistance will also be discussed.
Keywords:
FGF ligand; FGF/FGFR signaling; FGFR; FGFR inhibitors; cancer; target.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use*
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Antineoplastic Agents, Immunological / chemistry
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Antineoplastic Agents, Immunological / pharmacology
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Antineoplastic Agents, Immunological / therapeutic use*
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Drug Development / methods
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Drug Discovery / methods
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Drug Resistance, Neoplasm
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Fibroblast Growth Factors / metabolism
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Humans
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Molecular Targeted Therapy / methods
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Neoplasms / drug therapy*
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Neoplasms / metabolism
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology
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Protein Kinase Inhibitors / therapeutic use*
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Receptors, Fibroblast Growth Factor / antagonists & inhibitors*
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Receptors, Fibroblast Growth Factor / metabolism
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Signal Transduction / drug effects
Substances
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Antineoplastic Agents
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Antineoplastic Agents, Immunological
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Protein Kinase Inhibitors
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Receptors, Fibroblast Growth Factor
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Fibroblast Growth Factors