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Recent developments and advances of FGFR as a potential target in cancer

Wen-Jun Xue1, Ming-Tao Li1, Lin Chen1

  • 1Jiangsu Key Laboratory of Drug Design & Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, PR China.

Future Medicinal Chemistry
|August 2, 2018
PubMed

Insights

Fibroblast Growth Factors (FGFs) and their receptors (FGFRs) are key in healing and regeneration. This review covers FGF/FGFR signaling, inhibitors, and strategies to overcome cancer drug resistance.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Fibroblast Growth Factors (FGFs) and their receptors (FGFRs) are crucial for biological processes like angiogenesis, wound healing, and tissue regeneration.
  • Dysregulation of FGFR signaling is frequently observed in various cancers, positioning FGFRs as significant therapeutic targets for antitumor strategies.

Purpose of the Study:

  • To provide a comprehensive overview of FGF/FGFR signaling pathways.
  • To categorize currently available clinical FGFR inhibitors.
  • To elucidate mechanisms of resistance to FGFR inhibitors and discuss strategies to overcome this drug resistance.

Main Methods:

  • Literature review of FGF/FGFR signaling.
  • Analysis of clinical FGFR inhibitors.
  • Discussion of resistance mechanisms and counter-strategies.

Main Results:

  • FGFRs play a vital role in normal biological functions and cancer development.
  • Several FGFR inhibitors are under clinical investigation for cancer treatment.
  • Emergence of resistance to FGFR inhibitors necessitates understanding underlying mechanisms.

Conclusions:

  • Targeted therapies inhibiting FGFR signaling hold promise for cancer treatment.
  • Understanding and overcoming resistance mechanisms are critical for the effective clinical implementation of FGFR inhibitors.
  • Further research into resistance pathways will guide the development of more effective antitumor strategies.
Keywords:
FGF ligandFGF/FGFR signalingFGFRFGFR inhibitorscancertarget

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