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

Future Med Chem. 2018 Sep 1;10(17):2109-2126. doi: 10.4155/fmc-2018-0103. Epub 2018 Aug 1.

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

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Agents, Immunological / chemistry
  • Antineoplastic Agents, Immunological / pharmacology
  • Antineoplastic Agents, Immunological / therapeutic use*
  • Drug Development / methods
  • Drug Discovery / methods
  • Drug Resistance, Neoplasm
  • Fibroblast Growth Factors / metabolism
  • Humans
  • Molecular Targeted Therapy / methods
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Receptors, Fibroblast Growth Factor / antagonists & inhibitors*
  • Receptors, Fibroblast Growth Factor / metabolism
  • Signal Transduction / drug effects

Substances

  • Antineoplastic Agents
  • Antineoplastic Agents, Immunological
  • Protein Kinase Inhibitors
  • Receptors, Fibroblast Growth Factor
  • Fibroblast Growth Factors