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Application: Screen or characterize FGF-21 analogs or antagonists.
Background: Fibroblast growth factor 21 (FGF-21) is a member of the FGF family that lacks the heparin-binding ability and can be released into circulation to act as an endocrine factor. It is found in the liver, adipose tissue, central nervous system and other tissues, with circulating FGF-21 being expressed in the liver. It is a stress-inducible hormone that plays a key role in regulating energy balance, as well as glucose and lipid homeostasis, through a heterodimeric receptor complex composed of FGF receptor 1 (FGFR1), which is a tyrosine kinase, and co-receptor β-Klotho. In the liver, the effects of transcription factor PPARα (Peroxisome proliferator-activated receptor alpha) are mediated by increased production of FGF-21. FGF-21 regulates sugar intake and insulin sensitivity. Mutations in FGF-21 have been linked to obesity and type-2 diabetes (T2D) risk, therefore FGF-21 has attracted attention as a therapeutic target for those disorders. Further studies are required to elucidate the detailed mechanisms of action of FGF-21 and the benefits of drugs targeting this hepatokine.
Description: The FGF-21 Responsive Luciferase Reporter HEK293 Cell Line is a HEK293 cell line engineered to express firefly luciferase under the control of the GAL4 upstream activation sequence (UAS). It overexpresses human β-Klotho (KLB, NM_175737.4) and human Elk-1 (ETS Like-1 protein) transactivation domain (Elk1-TA, amino acids 205-end) fused to the DNA binding domain (DBD) of GAL4 (GAL4 DBD, amino acid 1-147). This allows for quantitative measurement of FGF-21 (Fibroblast growth factor 21) activity through its cognate receptors and downstream signaling networks. This cell line has been validated by stimulation with recombinant human FGF-21 and inhibition by a pan-FGFR inhibitor, Futibatinib. Figure 1: Illustration of the mechanism leading to luciferase expression in response to FGF-21 treatment in FGF-21 Responsive Luciferase Reporter HEK293 Cell Line.Interested in having us perform the screening and profiling of inhibitors or blocking antibodies? Visit our Immunotherapy Cell-Based Screening Services.
Host Cell Line: HEK293, Human Embryonic Kidney, epithelial-like cells, adherent.
Mycoplasma Testing: The cell line has been screened to confirm the absence of Mycoplasma species.
Storage Stability: Cells are shipped in dry ice and should immediately be thawed or stored in liquid nitrogen upon receipt. Do not use a -80°C freezer for long term storage.
Supplied As: Each vial contains ≥1 x 106 cells in 1 ml of Cell Freezing Medium (BPS Bioscience #79796)
Target: FGF21
Uniprot: Q86Z14
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: BSL-2
References: Geng L., et al., 2020 Nature Review Endocrinology 16: 654-667.Lin X., et al., 2017 Biomedical Reports 6(5):495-502.Yie J., et. al., 2008 FEBS Letter 583 (1): 19-24.
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