FGFR = FIBROBLAST GROWTH FACTOR RECEPTOR
The FGFR (Fibroblast Growth Factor Receptor) family includes four receptor tyrosine kinases, known as FGFR 1-4.
On FGF ligand binding, FGFRs dimerize and become capable of activating several downstream pathways, including Ras-MAPK, PI3K-AKT, Phospholipase C gamma-PKC, and STAT, that regulate cellular proliferation, survival, migration, and motility.
Dysregulated signal transduction by genetic alterations in FGFRs or FGFs has been shown to play crucial roles in tumor cell roliferation, angiogenesis, metastatis, and survival.
Examples include activating mutations and translocations of FGFR3 in bladder cancer, gene amplification of FGFR1 in squamous cell lung cancer, and gene amplification of FGFR2 in gastric cancer.
Incyte is developing inhibitors of FGFR.
FGFRs play an important role in tumor cell proliferation and survival, migration, and angiogenesis. Activating mutations, translocations, and gene amplifications in FGFRs are closely correlated with the development of various cancers. FGFRs are important targets for anticancer drug development. Incyte is researching FGFRs in solid tumors.