Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors
Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors
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.
- Central South University China (People's Republic of)
- Henan Normal University China (People's Republic of)
- Henan Normal University China (People's Republic of)
- Yunnan Normal University China (People's Republic of)
- Huainan Normal University China (People's Republic of)
QH573-671, kinase inhibitor, Receptor Protein-Tyrosine Kinases, Review, targeted therapy, Receptors, Fibroblast Growth Factor, Fibroblast Growth Factors, fibroblast growth factor receptors, Quinoxalines, Humans, Pyrazoles, structure, Cytology, Protein Kinase Inhibitors, Signal Transduction
QH573-671, kinase inhibitor, Receptor Protein-Tyrosine Kinases, Review, targeted therapy, Receptors, Fibroblast Growth Factor, Fibroblast Growth Factors, fibroblast growth factor receptors, Quinoxalines, Humans, Pyrazoles, structure, Cytology, Protein Kinase Inhibitors, Signal Transduction
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