Abstract
The inhibition of glucokinase by rat and Xenopus GKRPs (glucokinase regulatory protein) is well documented. We report a comparison of the effects of human and rat GKRPs on glucokinase activity. Human GKRP is a more potent inhibitor of glucokinase than rat GKRP in the absence of fructose 6-phosphate or sorbitol 6-phosphate, and has a higher affinity for these ligands. However, human and rat GKRPs have similar affinities for fructose 1-phosphate and chloride. Residues that are not conserved between the rodent and human proteins affect both the affinity for fructose 6-phosphate and sorbitol 6-phosphate and the inhibitory potency of GKRP on glucokinase in the absence of these ligands.
Publication types
-
Comparative Study
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Adaptor Proteins, Signal Transducing
-
Animals
-
Carrier Proteins / isolation & purification
-
Carrier Proteins / metabolism
-
Carrier Proteins / pharmacology*
-
Chlorides / pharmacology
-
Enzyme Inhibitors / isolation & purification
-
Enzyme Inhibitors / metabolism
-
Enzyme Inhibitors / pharmacology*
-
Fructosephosphates / metabolism
-
Fructosephosphates / pharmacology
-
Glucokinase / metabolism*
-
Glucose / pharmacology
-
Hexosephosphates / metabolism
-
Hexosephosphates / pharmacology
-
Humans
-
Intracellular Signaling Peptides and Proteins
-
Kinetics
-
Ligands
-
Rats
-
Species Specificity
Substances
-
Adaptor Proteins, Signal Transducing
-
Carrier Proteins
-
Chlorides
-
Enzyme Inhibitors
-
Fructosephosphates
-
GCKR protein, human
-
Gckr protein, rat
-
Hexosephosphates
-
Intracellular Signaling Peptides and Proteins
-
Ligands
-
glucokinase regulatory protein
-
fructose-1-phosphate
-
sorbitol 6-phosphate
-
fructose-6-phosphate
-
Glucokinase
-
Glucose