Target intelligence / Profile preview

Basic fibroblast growth factor (FGF2) (FGF2)

Target
FGF2
Molecular classification
Growth factor, Heparin-binding protein, Cytokine, Mitogen
01

Overview

Basic fibroblast growth factor (FGF2) is a potent mitogenic and angiogenic protein that belongs to the fibroblast growth factor family. It plays a fundamental role in physiological processes such as limb and nervous system development, tissue regeneration, and wound repair by stimulating the proliferation and differentiation of various cell types, including fibroblasts and endothelial cells. In pathological contexts, FGF2 is frequently overexpressed in the tumor microenvironment, where it promotes tumor growth, survival, and metastasis by enhancing angiogenesis and activating oncogenic signaling through its high-affinity tyrosine kinase receptors (FGFRs). In drug development, FGF2 is targeted both as an agonist in the form of recombinant proteins (e.g., Trafermin) for chronic wound healing and as part of the FGF/FGFR axis in oncology, where small molecule inhibitors and antibodies aim to block its aberrant signaling in malignancies like urothelial and cholangiocarcinoma. Managing its pathway often involves monitoring for unique side effects like hyperphosphatemia and ocular toxicities.

Other names
bFGFFibroblast growth factor 2Heparin-binding growth factor 2HBGF-2ProstatropinFGF-beta
02

Mechanism of action

FGF2 binds to fibroblast growth factor receptors (FGFR1-4) and heparan sulfate proteoglycans to form a ternary complex, inducing receptor dimerization, autophosphorylation, and activation of the RAS-MAPK, PI3K-AKT, and PLC-gamma signaling pathways.

03

Biological functions

Cell proliferationAngiogenesisWound healingTissue repairEmbryonic developmentCell differentiationMorphogenesis
04

Disease associations

CancerCardiovascular diseaseOsteoarthritisInflammationAngiogenic disordersAtherosclerosis
05

Safety considerations

HyperphosphatemiaRetinal pigment epithelial detachment (RPED)DiarrheaHand-foot syndromeStomatitisNail toxicityRisk of tumor promotion in non-oncology applications
06

Interacting drugs

Trafermin

9 more in the full profile.

07

Biomarkers

Serum FGF2 levelsFGFR1/2/3 gene amplificationFGFR2/3 gene fusionsFGF2 mRNA expression

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