Skaltsounis, LGuyard, NEisenbrand, GMeijer, LΟικονομάκος, Νίκος Γ.Eisenbrand, GerhardKosmopoulou, Magda N.Χρυσίνα, Ευαγγελία Δ.Bischler, NicolasTiraidis, CostasΛεωνίδας, Δημήτρης Δ.Ζωγράφος, Σπύρος Ε.Tsitsanou, Katerina E.Κώστας, Ιωάννης Δ.ROSCOFFIndirubin 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.177-+ISBN: 2-9518029-0-0https://hdl.handle.net/10442/12449engLife In Progress Editions© LIFE IN PROGRESS EDITIONS© LIFE IN PROGRESS EDITIONSInternational Meeting on Indirubin, the Red Shade of Indigo, Les Eyzies de Tayac, FRANCE, Indirubin, the Red Shade of Indigo, 2003-04-08 - 2003-04-13X-ray crystallographyindigosglycogenolysisinhibitionindirubinsChemistry, MedicinalIndirubin and indigo analogues as potential inhibitors of glycogenolysis: structural basis of glycogen phosphorylase inhibitionΑνακοίνωση σε συνέδριο2006ΧημείαChemical sciencesFrascati 42Φαρμακευτική χημείαMedicinal chemistryisi - Chemistry, Medicinal includes resources emphasizing the isolation and study of substances with therapeutic potential. Topics of interest are quantitative structure-function relationships, structural characterization and organic syntheses of naturally occurring compounds, and chemical and analytical techniques used in rational drug design. See also the PHARMACOLOGY & PHARMACY category.Φαρμακολογία και ΦαρμακευτικήPharmacology and Pharmacyisi - Pharmacology & Pharmacy covers resources on the discovery and testing of bioactive substances, including animal research, clinical experience, delivery systems, and dispensing of drugs. This category also includes resources on the biochemistry, metabolism, and toxic or adverse effects of drugs.Άρθρο συνεδρίουConference articleΒιολογίαBiological sciencesFrascati 42Εθνικό Ίδρυμα Ερευνών (ΕΙΕ)Greek Aggregator OpenArchives.gr | National Documentation Centre (EKT)