Protein / target
Fibroblast growth factor receptor 1
Protein at a glance
Biological role
Fibroblast growth factor receptor activity
Primary system
Nervous system
Strongest disease association
hypogonadotropic hypogonadism 2 with or without anosmia
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
12 approved · 14 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 embryonic development, cell proliferation, differentiation and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (GnRH) neuronal system. Phosphorylates PLCG1, FRS2, GAB1 and SHB. 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. Promotes phosphorylation of SHC1, STAT1 and PTPN11/SHP2. In the nucleus, enhances RPS6KA1 and CREB1 activity and contributes to the regulation of transcription. FGFR1 signaling is down-regulated by IL17RD/SEF, and by FGFR1 ubiquitination, internalization and degradation
Subcellular location
Domains and Gene Ontology detail (56)Hide
Domains & features
Gene Ontology
- Ccytoplasmic vesicle
- Ccytosol
- Cextracellular region
- Cglutamatergic synapse
- Cmembrane
- Cnucleus
- Cplasma membrane
- Cpostsynapse
- Creceptor complex
- FATP binding
- Ffibroblast growth factor binding
- Ffibroblast growth factor receptor activity
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
- ·positive regulation of MAP kinase activity
Transcriptional regulation
- ·Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth facto…
- ·DNA-templated transcription
- ·negative regulation of transcription by RNA polymerase II
Synaptic signalling
- ·glutamatergic synapse
- ·postsynapse
- ·regulation of postsynaptic density assembly
Excitatory neurotransmission
- ·glutamatergic synapse
Metabolic enzyme activity
- ·diphosphate metabolic process
View underlying pathways (22)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 1 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 4,766 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 · 26 total
macular degeneration · age-related macular degeneration
cancer · biliary tract cancer · cholangiocarcinoma
idiopathic pulmonary fibrosis · systemic sclerosis · non-small cell lung carcinoma
renal cell carcinoma · neoplasm · renal cell carcinoma
breast cancer
cholangiocarcinoma · neoplasm · cancer
gastric adenocarcinoma · non-small cell lung carcinoma · breast cancer
neoplasm · neuroendocrine carcinoma · neuroendocrine neoplasm
colorectal carcinoma · breast carcinoma · exocrine pancreatic carcinoma
gastric cancer · non-small cell lung carcinoma · acute myeloid leukemia
Tractability
Safety liabilities
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.
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 3 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 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.
- Regulatory approval
Approval: Stivarga (EMA)
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.