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Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors

Shuyan Dai1, Zhan Zhou2, Zhuchu Chen3

  • 1NHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, China. syandai@hotmail.com.

Cells
|June 21, 2019
PubMed

Insights

Fibroblast growth factor receptors (FGFRs) are crucial in cell development and implicated in various cancers. This review covers FGFR structure and the development of small molecule inhibitors, including the approved drug erdafitinib.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Fibroblast growth factor receptors (FGFRs) are receptor tyrosine kinases vital for cellular functions.
  • FGFR dysregulation is linked to numerous cancers, including urothelial, liver, ovarian, and lung cancers.
  • FGFRs represent significant therapeutic targets in oncology.

Purpose of the Study:

  • To review the structural characteristics of FGFRs, focusing on the kinase domain.
  • To summarize the development of small molecule inhibitors targeting FGFRs.
  • To highlight the therapeutic potential of FGFR inhibition in cancer treatment.

Main Methods:

  • Literature review of FGFR structure and function.
  • Analysis of small molecule inhibitor development pipelines.
  • Examination of clinical trial data and drug approvals.

Main Results:

  • FGFRs possess a kinase domain critical for their signaling.
  • Numerous small molecule FGFR inhibitors have been developed, with several in clinical trials.
  • Erdafitinib, a pan-FGFR inhibitor, is FDA-approved for metastatic urothelial carcinoma.

Conclusions:

  • FGFRs are validated drug targets in oncology.
  • Small molecule inhibitors offer a promising therapeutic strategy for FGFR-driven cancers.
  • Targeted therapies like erdafitinib represent advancements in cancer treatment.
Keywords:
fibroblast growth factor receptorskinase inhibitorstructuretargeted therapy

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