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Fibroblast growth factor receptor 1; Fibroblast growth factor receptor 2 (FGFR1; FGFR2)

Target
FGFR1; FGFR2
Molecular classification
Receptor tyrosine kinase, Single-pass transmembrane receptor
01

Overview

Fibroblast growth factor receptor 1 (FGFR1) and fibroblast growth factor receptor 2 (FGFR2) are cell-surface tyrosine-protein kinases that act as high-affinity receptors for fibroblast growth factors (FGFs). Structurally, each consists of three extracellular immunoglobulin-like domains (D1-D3), a single transmembrane helix, and an intracellular split tyrosine kinase domain. Ligand binding triggers receptor dimerization and activation of kinase activity, leading to pathways that control cell proliferation, differentiation, migration, and survival. FGFR1/2 play central roles in embryonic development, tissue homeostasis, angiogenesis, and wound repair. Genetic alterations of FGFR1/2 can drive cancers, skeletal disorders, and other diseases, making them prominent drug targets in oncology and regenerative medicine.

Other names
FGFR1 (also known as CD331)FGFR2
02

Mechanism of action

Inhibition of kinase activity (blocking phosphorylation and downstream signal transduction); Disruption of ligand binding; Receptor dimerization blockade

03

Biological functions

Signal transductionCell proliferationCell differentiationMigrationEmbryonic developmentCell survivalAngiogenesisWound healing
04

Disease associations

Cancer (e.g., breast, colon, pancreatic cancer)Developmental disorders (skeletal dysplasia, craniosynostosis)InflammationCardiovascular disease
05

Safety considerations

Hyperphosphatemia (from inhibition of FGF23 signaling)Ocular toxicitySkin toxicitiesGastrointestinal disturbancesRisk of impaired wound healing and developmental toxicity (due to physiological roles of FGFRs)
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Interacting drugs

Erdafitinib

2 more in the full profile.

07

Biomarkers

FGFR gene mutations or amplifications (e.g., FGFR1/FGFR2 fusions)Protein overexpression (immunohistochemistry on tumor biopsies)

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