Stimulation of hepatocyte glucose metabolism by novel small molecule glucokinase activators.

@article{Brocklehurst2004StimulationOH,
  title={Stimulation of hepatocyte glucose metabolism by novel small molecule glucokinase activators.},
  author={Katy J. Brocklehurst and Victoria A. Payne and Rick A Davies and Debra Carroll and Helen L Vertigan and Heather J Wightman and Susan Aiston and Ian D Waddell and Brendan Leighton and Matthew P. Coghlan and Loranne Agius},
  journal={Diabetes},
  year={2004},
  volume={53 3},
  pages={535-41}
}
Glucokinase (GK) has a major role in the control of blood glucose homeostasis and is a strong potential target for the pharmacological treatment of type 2 diabetes. We report here the mechanism of action of two novel and potent direct activators of GK: 6-[(3-isobutoxy-5-isopropoxybenzoyl)amino]nicotinic acid(GKA1) and 5-([3-isopropoxy-5-[2-(3-thienyl)ethoxy]benzoyl]amino)-1,3,4-thiadiazole-2-carboxylic acid(GKA2), which increase the affinity of GK for glucose by 4- and 11-fold, respectively… CONTINUE READING

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