2. Academic Validation
  3. Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors

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

  • Cells. 2019 Jun 18;8(6):614. doi: 10.3390/cells8060614.
Shuyan Dai 1,  Zhan Zhou 2,  Zhuchu Chen 3,  Guangyu Xu 4,  Yongheng Chen 5
Affiliations

Affiliations

  • 1 NHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, China. [email protected].
  • 2 NHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, China. [email protected].
  • 3 NHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, China. [email protected].
  • 4 Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education), College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha 410081, Hunan, China. [email protected].
  • 5 NHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, China. [email protected].
PMID: 31216761 DOI: 10.3390/cells8060614
Abstract

Fibroblast Growth Factor receptors (FGFRs) are a family of Receptor Tyrosine Kinases expressed on the cell membrane that play crucial roles in both developmental and adult cells. Dysregulation of FGFRs has been implicated in a wide variety of cancers, such as urothelial carcinoma, hepatocellular carcinoma, ovarian Cancer and lung adenocarcinoma. Due to their functional importance, FGFRs have been considered as promising drug targets for the therapy of various cancers. Multiple small molecule inhibitors targeting this family of kinases have been developed, and some of them are in clinical trials. Furthermore, the pan-FGFR inhibitor erdafitinib (JNJ-42756493) has recently been approved by the U.S. Food and Drug Administration (FDA) for the treatment of metastatic or unresectable urothelial carcinoma (mUC). This review summarizes the structure of FGFR, especially its kinase domain, and the development of small molecule FGFR inhibitors.

Keywords

fibroblast growth factor receptors; kinase inhibitor; structure; targeted therapy.

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