Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme.

@article{Freeman2006SensitivityOG,
  title={Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme.},
  author={Susan B Freeman and Jake Blake Bartlett and Gemma Convey and Ian M. Hardern and Joanne L Teague and Susan J G Loxham and Janet M. Allen and S. M. Poucher and Alan Charles},
  journal={British journal of pharmacology},
  year={2006},
  volume={149 6},
  pages={775-85}
}
BACKGROUND AND PURPOSE Inhibition of hepatic glycogen phosphorylase is a potential treatment for glycaemic control in type 2 diabetes. Selective inhibition of the liver phosphorylase isoform could minimize adverse effects in other tissues. We investigated the potential selectivity of two indole site phosphorylase inhibitors, GPi688 and GPi819. EXPERIMENTAL APPROACH The activity of glycogen phosphorylase was modulated using the allosteric effectors glucose or caffeine to promote the less… CONTINUE READING