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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
07:32

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library

Published on: September 30, 2019

Small molecule inhibition of fibroblast growth factor receptors in cancer

Guang Liang1, Gaozhi Chen, Xiaoyan Wei

  • 1School of Pharmaceutical Sciences, Wenzhou Medical College, Wenzhou 325035, China.

Cytokine & Growth Factor Reviews
|July 9, 2013
PubMed

Insights

Fibroblast growth factor receptors (FGFRs) are crucial in human development and metabolism. Aberrant FGFR signaling drives developmental disorders and cancers, making FGFRs a key target for novel cancer therapeutics.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Fibroblast growth factors (FGFs) transmit signals via FGF receptors (FGFRs), a receptor tyrosine kinase family.
  • Dysregulated FGF signaling, often due to FGFR gain-of-function mutations, causes developmental disorders and is implicated in various cancers.
  • FGFs promote cell proliferation and tumor angiogenesis, contributing to carcinogenesis.

Purpose of the Study:

  • To review the critical roles of FGFRs in cancer development.
  • To provide an update on clinical trials involving small-molecule FGFR inhibitors.
  • To discuss the application of structural data in designing novel FGFR inhibitors.

Main Methods:

  • Review of existing literature on FGF/FGFR signaling in cancer.
  • Analysis of data from in vivo and in vitro models of FGFR inhibition.
  • Examination of current structural data of FGFR kinases.

Main Results:

  • FGFRs play significant roles in the pathogenesis of cancers like endometrial and bladder cancer.
  • Gene knockout and pharmacological inhibition studies confirm FGFRs as viable therapeutic targets.
  • Ongoing clinical trials are evaluating small-molecule FGFR inhibitors for FGFR-driven cancers.

Conclusions:

  • FGFRs are validated targets for cancer therapy due to their roles in proliferation and angiogenesis.
  • The development of specific small-molecule FGFR inhibitors is a promising area for cancer treatment.
  • Structural insights into FGFR kinases are instrumental in the rational design of new inhibitors.
Keywords:
CancerCancer chemotherapyFibroblast growth factor receptorSmall-molecule inhibitorStructure–activity relationship

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