Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.

@article{Binda2011MolecularII,
  title={Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.},
  author={Claudia Binda and Milagros Aldeco and Werner J Geldenhuys and Marcello Tortorici and Andrea Mattevi and Dale E. Edmondson},
  journal={ACS medicinal chemistry letters},
  year={2011},
  volume={3 1},
  pages={39-42}
}
The widely employed anti-diabetic drug pioglitazone (Actos) is shown to be a specific and reversible inhibitor of human monoamine oxidase B (MAO B). The crystal structure of the enzyme-inhibitor complex shows the R-enantiomer is bound with the thiazolidinedione ring near the flavin. The molecule occupies both substrate and entrance cavities of the active site establishing non-covalent interactions with the surrounding amino acids. These binding properties differentiate pioglitazone from the… CONTINUE READING
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