Fibroblast Growth Factor Receptors 1 & 2 Assay for Paracrine FGF Signaling (FGFR1/2)

INDIGO's assay utilizes proprietary human cells that have been engineered to provide constitutive expression of the Human Fibroblast Growth Factors 1 and 2 (FGFR1/2). FGFR1 and FGFR2 are both single-pass transmembrane receptors that contain respective extracellular ligand-binding domains, transmembrane domains, and intracellular tyrosine kinase domains.

INDIGO's Compound Screening Media is supplemented with heparin, thereby enabling the formation of FGF/Heparin complexes that bind with high affinity to FGFR monomers. This binding interaction triggers conformational changes that drive the assembly of homo-dimeric (R1:R1, R2: R2) and/or hetero-dimeric (R1:R2) receptors, and the activation of their respective cytosolic tyrosine kinase domains.

The tyrosine kinase activities of activated FGFR's initiate intracellular signaling cascades that include RAS-MAPK, PI3-AKT, PLCγ, and STAT pathways. For example, activation of the PLCγ pathway leads to an increase of intracellular calcium. One prominent outcome of the FGF/FGFR>PLCγ pathway is that calcineurin, a calcium-dependent phosphatase, dephosphorylates and activates the transcription factor NFAT. It is FGFR signal transduction via the Ca⁺² calcineurin / NFAT cascade that is exploited by the reporter cells in this assay. [INDIGO Catalog Nos. IB21001, IB21001-32, IB21002]

WARNING This product is not for human or veterinary use.