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Targeting FGFRs for tumor therapy: current status and novel strategies

Yunzhou Dong1,2,3, Changyu Ren1, Mengli Zhu3

  • 1Department of Pharmacy, Chengdu Fifth People's Hospital, Chengdu 611130, Sichuan, China.

Future Medicinal Chemistry
|November 30, 2022
PubMed

Insights

Novel small-molecule inhibitors targeting fibroblast growth factor receptors (FGFRs) are crucial for cancer treatment. This review details recent advances in FGFR inhibitors and novel technologies to overcome current clinical challenges in tumor therapy.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Fibroblast growth factor receptors (FGFRs) are receptor tyrosine kinases implicated in tumor cell invasion and angiogenesis.
  • Targeted modulation of FGFRs represents a key strategy in cancer therapy.
  • Current FGFR inhibitors face clinical challenges, necessitating the development of novel therapeutic approaches.

Purpose of the Study:

  • To review recent advancements in small-molecule inhibitors targeting FGFRs.
  • To focus on structure-activity relationships of these inhibitors.
  • To summarize novel technologies for improving FGFR-targeted cancer therapy.

Main Methods:

  • Literature review of recent studies on small-molecule FGFR inhibitors.
  • Analysis of structure-activity relationships.
  • Summary of emerging technologies in FGFR-targeted drug development.

Main Results:

  • Several small-molecule inhibitors targeting FGFRs have been developed, with three approved for clinical use.
  • Understanding structure-activity relationships is key to designing more effective inhibitors.
  • New technologies are emerging to address limitations of current FGFR-targeted therapies.

Conclusions:

  • There is a significant need for novel FGFR inhibitors and technologies to overcome existing clinical limitations.
  • This review provides a reference for the development and application of advanced FGFR-targeted drugs in oncology.
  • Continued research into FGFR inhibitors and related technologies holds promise for improved cancer treatment outcomes.
Keywords:
FGFRscancerinhibitorkinase selectivitynovel strategiesstructure–activity relationship

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