Cayman Fibroblast Growth Factor Receptor 1c and β-Klotho (FGFR/β-Klotho) for Endocrine FGF Signaling Reporter Assay System

INDIGOs Human Fibroblast Growth Factor Receptor Receptor 1c and β-Klotho (FGFR/β-Klotho) Reporter Assay System utilizes proprietary human cells that have been engineered to provide constitutive expression of the Human Fibroblast Growth Factor Receptor 1c and β-Klotho. FGFR1c and β-Klotho are both single-pass transmembrane proteins. FGFR1c has an extracellular ligand-binding domain, transmembrane domain, and intracellular tyrosine kinase domain. It has been established that FGFR association with the co-receptor β-Klotho generates a scaffold that is essential for endocrine growth factor binding interactions, such as those with FGF-21 and FGF-19. Following growth factor binding, the activated tyrosine kinase activities of the FGFR initiate intracellular signaling cascades that may include RAS-MAPK, PI3-AKT, PLCγ and/or STAT pathways. It is FGFR1c/β-Klotho signal transduction via the RAS-MAPK-ERK1/2 cascade that is exploited by the reporter cells in this assay.

INDIGOs FGFR/β-Klotho Reporter Cells contain the luciferase reporter gene functionally linked to an Elk-1 responsive promoter. Activated Elk-1 binds to the response elements to initiate the formation of a complete transcription complex that drives Luc gene expression. Quantifying relative changes in luciferase activity in the treated reporter cells relative to the untreated cells provides a sensitive, dose-dependent surrogate measure of drug-induced changes in FGFR1c/β-Klotho activity.

The principal application of this reporter assay is in the screening of test materials to quantify any functional interactions, either activating or inhibitory, that they may exert against FGFR1c/β-Klotho or the coupled RAS-MAPK pathway.

FGFR/β-Klotho Reporter Cells are transiently transfected and prepared as frozen stocks using INDIGOs proprietary CryoMite™ process. This cryo-preservation method allows for the immediate dispensing of healthy, division-competent reporter cells into assay plates. There is no need for cumbersome intermediate treatment steps such as spin-and-rinse of cells, viability determinations, or cell titer adjustments prior to assay setup. [INDIGO Catalog Nos. IB2200132, IB22001, IB22002]

WARNING This product is not for human or veterinary use.