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|Title:||Indirubin and indigo analogues as potential inhibitors of glycogenolysis: structural basis of glycogen phosphorylase inhibition|
|Author/Creator:||Oikonomakos, Nikos G.|
Kosmopoulou, Magda N.
Leonidas, Demetres D.
Chrysina, Evangelia D.
Tsitsanou, Katerina E.
Zographos, Spyros E.
Kostas, Ioannis D.
|Type:||Conference Item (Conference paper)|
|Abstract:||Indirubin and indigo analogues were discovered as novel inhibitors of glycogen phosphorylase, a target to control hyperglycaemia in type 2 diabetes. We give a structural insight into the molecular basis of enzyme inhibition by indirubin-5-sulphonate, indirubin-3'-aminooxy-acetate, and indigo-5,5',7,7'-tetrasulphonate. The inhibitors bind at the inhibitor site, by intercalating between the side chains of Phe285 and Tyr613. In addition, two indirubin-3'-aminooxy-acetate molecules bind at the allosteric binding site and a new sub-site in the vicinity of the allosteric site. Comparative structural analyses indicate residues in the inhibitor and the allosteric sites that can be exploited to obtain more potent inhibitors.|
|Publisher:||Life In Progress Editions|
|Journal/Proceedings Publication:||Indirubin, the Red Shade of Indigo|
|Conference name:||International Meeting on Indirubin, the Red Shade of Indigo|
|Conference location:||Les Eyzies de Tayac, FRANCE|
|Conference Start date:||2003-04-08|
|Conference End date:||2003-04-13|
|Subject Category:||Science::Biology (General)|
Medicine::Pharmacy and materia medica
|Keywords:||glycogenolysis; indirubins; indigos; inhibition; X-ray crystallography; Chemistry, Medicinal|
|Other Identifiers:||ISBN: 2-9518029-0-0|
|Rights holder:||© LIFE IN PROGRESS EDITIONS|