Protein / target
Fibroblast growth factor receptor 2
Protein at a glance
Biological role
Fibroblast growth factor receptor activity
Primary system
Nervous system
Strongest disease association
Pfeiffer syndrome
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
11 approved · 16 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an essential role in the regulation of osteoblast differentiation, proliferation and apoptosis, and is required for normal skeleton development. Promotes cell proliferation in keratinocytes and immature osteoblasts, but promotes apoptosis in differentiated osteoblasts. Phosphorylates PLCG1, FRS2 and PAK4. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. FGFR2 signaling is down-regulated by ubiquitination, internalization and degradation. Mutations that lead to constitutive kinase activation or impair normal FGFR2 maturation, internalization and degradation lead to aberrant signaling. Over-expressed FGFR2 promotes activation of STAT1
Subcellular location
Domains and Gene Ontology detail (117)Hide
Domains & features
Gene Ontology
- Ccell cortex
- Ccell surface
- Ccytoplasm
- Ccytoplasmic vesicle
- Cexcitatory synapse
- Cextracellular region
- CGolgi apparatus
- Cmembrane
- Cnucleus
- Cplasma membrane
- Creceptor complex
- FATP binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Kinase signalling
- ·Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth facto…
- ·protein tyrosine kinase activity
- ·peptidyl-tyrosine phosphorylation
- ·protein autophosphorylation
Transcriptional regulation
- ·negative regulation of transcription by RNA polymerase II
- ·positive regulation of transcription by RNA polymerase II
Apoptosis & cell death
- ·apoptotic process
- ·fibroblast growth factor receptor signaling pathway involved in negative regulation of a…
Excitatory neurotransmission
- ·excitatory synapse
Synaptic signalling
- ·excitatory synapse
View underlying pathways (17)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Fibroblast growth factor receptor 2 inhibitor
Appears in clinical studies involving gastric cancer, gastric neoplasm, gastric adenocarcinoma, gastroesophageal junction adenocarcinoma
Fibroblast growth factor receptor 2 inhibitor
Appears in clinical studies involving colorectal cancer, metastatic colorectal cancer, colorectal neoplasm, neoplasm
Fibroblast growth factor receptor inhibitor
Appears in clinical studies involving cancer, urothelial carcinoma, urinary bladder carcinoma, neoplasm
Fibroblast growth factor receptor inhibitor
Appears in clinical studies involving cancer, biliary tract cancer, intrahepatic cholangiocarcinoma, cholangiocarcinoma
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 5,541 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 27 total
urothelial carcinoma · urinary bladder carcinoma · non-small cell lung carcinoma
malignant mesothelioma · bladder transitional cell carcinoma · cholangiocarcinoma
idiopathic pulmonary fibrosis · systemic sclerosis · non-small cell lung carcinoma
biliary tract cancer · cholangiocarcinoma · cancer
breast cancer
small cell lung carcinoma · breast cancer · lung cancer
cancer · urothelial carcinoma · urinary bladder carcinoma
gastric adenocarcinoma · non-small cell lung carcinoma · breast cancer
gastric cancer · breast cancer
colorectal carcinoma · breast carcinoma · exocrine pancreatic carcinoma
Tractability
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 4 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- New publicationEfficacy of pembrolizumab in microsatellite-stable, tumor mutational burden-high metastatic colorectal cancer: genomic signatures and clinical outcomes.
- Regulatory approval
Approval: Balversa (EMA)
- New publicationLenvatinib Plus Pembrolizumab Versus Standard of Care for Previously Treated Metastatic Colorectal Cancer: Final Analysis of the Randomized, Open-Label, Phase III LEAP-017 Study.
- New publicationBemarituzumab as first-line treatment for locally advanced or metastatic gastric/gastroesophageal junction adenocarcinoma: final analysis of the randomized phase 2 FIGHT trial.
- New publicationClinical and Genomic Landscape of FGFR3-Altered Urothelial Carcinoma and Treatment Outcomes with Erdafitinib: A Real-World Experience.
- Regulatory approval
Approval: Lytgobi (EMA)
- New publicationFutibatinib for <i>FGFR2</i>-Rearranged Intrahepatic Cholangiocarcinoma.
- New publicationTargeted therapy for hepatocellular carcinoma.
- New publicationMolecular targeted and immune checkpoint therapy for advanced hepatocellular carcinoma.
- New publicationErdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma.
- New publicationRandomized Double-Blind Phase II Study of Regorafenib in Patients With Metastatic Osteosarcoma.
- New publicationRegorafenib for patients with hepatocellular carcinoma who progressed on sorafenib treatment (RESORCE): a randomised, double-blind, placebo-controlled, phase 3 trial.
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.