GCKR
GCKR (glucokinase regulator) encodes the glucokinase regulatory protein, which inhibits glucokinase (GCK) by forming an inactive complex with the enzyme. It acts in liver and pancreatic islet cells and belongs to the GCKR subfamily of the SIS (Sugar ISomerase) family. Browse Assay Genie's current range of GCKR research reagents below, or read on for the biology behind the target.
GCKR regulates glucokinase (GCK) by binding it non-covalently and forming an inactive complex. By promoting GCK recruitment to the nucleus, GCKR may provide a reserve of the enzyme that can be released quickly into the cytoplasm after a meal. The GCKR protein therefore acts as a control point on glucokinase activity in liver and pancreatic islet cells.
The affinity of GCKR for GCK is tuned by fructose metabolites. GCKR with bound fructose 6-phosphate has increased affinity for GCK, whereas GCKR with bound fructose 1-phosphate has strongly decreased affinity for GCK and does not inhibit its activity. This lets the regulator respond to the metabolic state of the cell.
The GCKR gene encodes a member of the GCKR subfamily of the SIS (Sugar ISomerase) family. UniProt records the protein in the cytoplasm, nucleus and mitochondrion. The gene is also known by the previous name glucokinase (hexokinase 4) regulatory protein, and orthologues are annotated in mouse and rat as Gckr.
NCBI Gene describes GCKR as a susceptibility gene candidate for a form of maturity-onset diabetes of the young (MODY), which makes it a point of interest for researchers studying glucose sensing and glycaemic control.
GCKR forms an inactive complex with GCK, making it a central subject for studies of how glucokinase activity is restrained.
GCKR inhibits glucokinase in liver cells and may hold a nuclear reserve of GCK that is released after a meal.
GCKR acts in pancreatic islet cells, where it inhibits glucokinase through formation of an inactive complex.
GCKR is considered a susceptibility gene candidate for a form of maturity-onset diabetes of the young (MODY).
GCKR binds glucokinase (GCK) and forms an inactive complex, inhibiting the enzyme in liver and pancreatic islet cells. It promotes GCK recruitment to the nucleus, possibly creating a reserve that can be quickly released into the cytoplasm after a meal.
Fructose 6-phosphate bound to GCKR increases its affinity for GCK. Fructose 1-phosphate bound to GCKR strongly decreases that affinity, and in this state GCKR does not inhibit GCK activity. This modulation links regulator activity to fructose metabolism.
HGNC lists the previous name glucokinase (hexokinase 4) regulatory protein, and UniProt calls the product glucokinase regulatory protein. No alternative symbols are recorded. Mouse and rat orthologues are both named Gckr; check the datasheet of any product for its validated reactivity.
Glucokinase, other hexokinases and glucose-metabolism targets that sit alongside GCKR in metabolic research.
Gene and protein annotations from HGNC, NCBI Gene and UniProt Q14397; product specifications from Assay Genie datasheets.