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Target intelligence / Profile preview
Fibroblast Growth Factor 21 Receptor Complex (FGF21 Receptor)
- Target
- FGF21 Receptor
- Molecular classification
- Receptor Tyrosine Kinase Complex, Growth Factor Receptor, Single-pass transmembrane protein, Type I membrane protein
01
Overview
The Fibroblast Growth Factor 21 Receptor complex is a heterodimeric cell-surface receptor consisting of FGFR1 (primarily the FGFR1c isoform) and the co-receptor β-Klotho. It mediates the systemic metabolic effects of Fibroblast Growth Factor 21 (FGF21), an endocrine hormone involved in glucose and lipid metabolism, insulin sensitivity, and energy homeostasis. Activation of this receptor complex regulates key metabolic processes in tissues like the liver, adipose tissue, and pancreas, making it a therapeutic target for obesity, type II diabetes, and related metabolic disorders.
- Other names
- FGF21 ReceptorFGFR1/β-Klotho complex
02
Mechanism of action
FGF21 binding to the FGFR1/β-Klotho complex induces receptor dimerization and autophosphorylation of intracellular tyrosine kinase domains. This activates downstream signaling cascades including MAPK/ERK and AMPK/SIRT1/PGC‑1α pathways, leading to increased glucose uptake, improved lipid metabolism, and enhanced energy expenditure.
03
Biological functions
Signal transductionGlucose uptake regulationLipid metabolism regulationInsulin sensitivity regulationEnergy homeostasisRegulation of food preferenceMitochondrial function regulation
04
Disease associations
ObesityType II Diabetes MellitusDyslipidemiaNon-alcoholic Fatty Liver Disease (NAFLD)AtherosclerosisMetabolic Syndrome
05
Safety considerations
Potential for off-target effects due to FGFR promiscuityImmunogenicity of FGF21 analogsLong-term effects on growth hormone signalingPossible cardiovascular effects
06
Interacting drugs
FGF21 analogs (e.g., pegbelfermin)
1 more in the full profile.
07
Biomarkers
FGF21 (circulating levels)Glucose levelsLipid profile (triglycerides, cholesterol)Insulin sensitivity markers (e.g., HOMA-IR)
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