High impact information on Gckr

• In GKRP-mutant mice, the disruption of this regulation and the subsequent decrease in GK activity leads to altered glucose metabolism and impaired glycemic control [1].
• We propose that GKRP functions as an anchor to sequester and inhibit GK in the hepatocyte nucleus, where it is protected from degradation [1].
• The glucokinase regulatory protein (GKRP) inhibits glucokinase competitively with respect to glucose by forming a protein-protein complex with this enzyme [2].
• The physiological role of GKRP in controlling hepatic glucokinase activity was addressed using gene targeting to disrupt GKRP gene expression [2].
• The genes encoding glucokinase regulatory protein and ketohexokinase co-localize to mouse chromosome 5 [3].

Biological context of Gckr

• Interestingly, when assayed under conditions to promote the association between glucokinase and GKRP, liver glucokinase activity in wild-type and null mice displayed comparable glucose phosphorylation capacities at physiological glucose concentrations (5 mM) [2].

Other interactions of Gckr

• These data suggest both a regulatory and a stabilizing role for GKRP in maintaining adequate glucokinase in the liver [2].

Analytical, diagnostic and therapeutic context of Gckr

• Additionally, introduction of the glucokinase regulatory protein and protein kinase C-zeta have been shown to improve glucose tolerance in non-insulin-dependent diabetes mellitus animal models [4].

References