1. Home page
  2. Search

Indirubin and indigo analogues as potential inhibitors of glycogenolysis: structural basis of glycogen phosphorylase inhibition

This item is provided by the institution :
National Hellenic Research Foundation (NHRF)   

Repository :
Helios - Repository of the National Hellenic Research Foundation (NHRF)  | repositories EKT   

see the original item page
in the repository's web site and access all digital files if the item*



Indirubin and indigo analogues as potential inhibitors of glycogenolysis: structural basis of glycogen phosphorylase inhibition
Οικονομάκος, Νίκος Γ.
Eisenbrand, Gerhard
Kosmopoulou, Magda N.
Χρυσίνα, Ευαγγελία Δ.
Bischler, Nicolas
Tiraidis, Costas
Λεωνίδας, Δημήτρης Δ.
Ζωγράφος, Σπύρος Ε.
Tsitsanou, Katerina E.
Κώστας, Ιωάννης Δ.
Skaltsounis, L (EN)
Guyard, N (EN)
Eisenbrand, G (EN)
Meijer, L (EN)
Ανακοίνωση σε συνέδριο
2006
ROSCOFF
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.
Βιολογία (Γενικά) (EL)
Χημεία (Γενικά) (EL)
Φαρμακευτική (EL)
Biology (General) (EN)
Pharmacy and materia medica (EN)
Chemistry (General) (EN)
X-ray crystallography
indigos
glycogenolysis
inhibition
indirubins
Chemistry, Medicinal
English
Life In Progress Editions
International Meeting on Indirubin, the Red Shade of Indigo, Les Eyzies de Tayac, FRANCE, Indirubin, the Red Shade of Indigo, 2003-04-08 - 2003-04-13
© LIFE IN PROGRESS EDITIONS
© LIFE IN PROGRESS EDITIONS (EN)
National Hellenic Research Foundation (NHRF)
Helios - Repository of the National Hellenic Research Foundation (NHRF)



*Institutions are responsible for keeping their URLs functional (digital file, item page in repository site)