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Target intelligence / Profile preview
Glucokinase Regulatory Protein (GKRP)
- Target
- GKRP
- Molecular classification
- Regulator protein, Enzyme regulator
01
Overview
Glucokinase regulatory protein (GKRP), encoded by the GCKR gene, is a key regulator of glucokinase (GK) activity and intracellular localization in hepatocytes. It controls hepatic glucose uptake, glycogen synthesis, glycolysis, and blood glucose homeostasis. GKRP binds to GK, sequestering it in the nucleus when glucose levels are low and releasing it into the cytoplasm when glucose levels rise. Variants in GCKR are associated with metabolic disorders such as type 2 diabetes and NAFLD, making it a potential drug target. Therapeutic strategies aim to modulate GK-GKRP interaction to restore balanced hepatic carbohydrate/lipid metabolism, avoiding the side effects associated with direct glucokinase activation.
- Other names
- GCKR
02
Mechanism of action
Modulation of GK-GKRP binding, allosteric activation/inhibition of interaction, mimicking physiological regulators like F1P/F6P.
03
Biological functions
Regulation of glucokinase activityRegulation of hepatic glucose uptakeRegulation of glycogen synthesisRegulation of glycolysisMaintenance of blood glucose homeostasisAllosteric regulation of glucokinase
04
Disease associations
Type 2 Diabetes Mellitus (T2D)Non-Alcoholic Fatty Liver Disease (NAFLD)HypertriglyceridemiaNASH/fibrosis progression
05
Safety considerations
Increased plasma triglyceridesPotential for worsening NAFLD if glucokinase is activated directly without considering GKRP regulation
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