Auflistung nach Autor "Hayes, J. M."
Anzeige der Dokumente 1-11 von 11
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1-(3-Deoxy-3-fluoro-beta-D-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modelling studies
Tsirkone, V. G.; Tsoukala, E.; Lamprakis, C.; Manta, S.; Hayes, J. M.; Skamnaki, V. T.; Drakou, C.; Zographos, S. E.; Komiotis, D.; Leonidas, D. D. (2010)Design of inhibitors of glycogen phosphorylase (GP) with pharmaceutical applications in improving glycaemic control in type 2 diabetes is a promising therapeutic strategy. The catalytic site of muscle glycogen phosphorylase ... -
3 '-Axial CH2OH Substitution on Glucopyranose does not Increase Glycogen Phosphorylase Inhibitory Potency. QM/MM-PBSA Calculations Suggest Why
Manta, S.; Xipnitou, A.; Kiritsis, C.; Kantsadi, A. L.; Hayes, J. M.; Skamnaki, V. T.; Lamprakis, C.; Kontou, M.; Zoumpoulakis, P.; Zographos, S. E.; Leonidas, D. D.; Komiotis, D. (2012)Glycogen phosphorylase is a molecular target for the design of potential hypoglycemic agents. Structure-based design pinpointed that the 3'-position of glucopyranose equipped with a suitable group has the potential to form ... -
Computation as a Tool for Glycogen Phosphorylase Inhibitor Design
Hayes, J. M.; Leonidas, D. D. (2010)Glycogen phosphorylase is an important therapeutic target for the potential treatment of type 2 diabetes. The importance of computation in the search for potent, selective and drug-like glycogen phosphorylase inhibitors ... -
An evaluation of indirubin analogues as phosphorylase kinase inhibitors
Begum, J.; Skamnaki, V. T.; Moffatt, C.; Bischler, N.; Sarrou, J.; Skaltsounis, A. L.; Leonidas, D. D.; Oikonomakos, N. G.; Hayes, J. M. (2015)Phosphorylase kinase (PhK) has been linked with a number of conditions such as glycogen storage diseases, psoriasis, type 2 diabetes and more recently, cancer (Camus et al., 2012 [6]). However, with few reported structural ... -
Glycogen Phosphorylase as a Target for Type 2 Diabetes: Synthetic, Biochemical, Structural and Computational Evaluation of Novel N-acyl-N '-(beta-D-glucopyranosyl) Urea Inhibitors
Kantsadi, A. L.; Parmenopoulou, V.; Bakalov, D. N.; Snelgrove, L.; Stravodimos, G. A.; Chatzileontiadou, D. S. M.; Manta, S.; Panagiotopoulou, A.; Hayes, J. M.; Komiotis, D.; Leonidas, D. D. (2015)Glycogen phosphorylase (GP), a validated target for the development of anti-hyperglycaemic agents, has been targeted for the design of novel glycopyranosylamine inhibitors. Exploiting the two most potent inhibitors from ... -
Glycogen phosphorylase as a target for type 2 diabetes: Synthetic, biochemical, structural and computational evaluation of novel N-acyl-N´-(β-D-glucopyranosyl) urea inhibitors
Kantsadi, A. L.; Parmenopoulou, V.; Bakalov, D. N.; Snelgrove, L.; Stravodimos, G. A.; Chatzileontiadou, D. S. M.; Manta, S.; Panagiotopoulou, A.; Hayes, J. M.; Komiotis, D.; Leonidas, D. D. (2015)Glycogen phosphorylase (GP), a validated target for the development of anti-hyperglycaemic agents, has been targeted for the design of novel glycopyranosylamine inhibitors. Exploiting the two most potent inhibitors from ... -
hCINAP is an atypical mammalian nuclear adenylate kinase with an ATPase motif: Structural and functional studies
Drakou, C. E.; Malekkou, A.; Hayes, J. M.; Lederer, C. W.; Leonidas, D. D.; Oikonomakos, N. G.; Lamond, A. I.; Santama, N.; Zographos, S. E. (2012)Human coilin interacting nuclear ATPase protein (hCINAP) directly interacts with coilin, a marker protein of Cajal Bodies (CBs), nuclear organelles involved in the maturation of small nuclear ribonucleoproteins UsnRNPs and ... -
Natural products and their derivatives as inhibitors of glycogen phosphorylase: potential treatment for type 2 diabetes
Hayes, J. M.; Kantsadi, A. L.; Leonidas, D. D. (2014)Glycogen phosphorylase (GP) (EC 2.4.1.1) is an important therapeutic target for the potential treatment of type 2 diabetes. The search for potent, selective and drug-like GP inhibitors which may eventually lead to hypoglycaemic ... -
The s-Hole Phenomenon of Halogen Atoms Forms the Structural Basis of the Strong Inhibitory Potency of C5 Halogen Substituted Glucopyranosyl Nucleosides towards Glycogen Phosphorylase b
Kantsadi, A. L.; Hayes, J. M.; Manta, S.; Skamnaki, V. T.; Kiritsis, C.; Psarra, A. M. G.; Koutsogiannis, Z.; Dimopoulou, A.; Theofanous, S.; Nikoleousakos, N.; Zoumpoulakis, P.; Kontou, M.; Papadopoulos, G.; Zographos, S. E.; Komiotis, D.; Leonidas, D. D. (2012)C5 halogen substituted glucopyranosyl nucleosides (1-(beta-D-glucopyranosyl)-5-X-uracil; X=Cl, Br, I) have been discovered as some of the most potent active site inhibitors of glycogen phosphorylase (GP), with respective ... -
Sourcing the affinity of flavonoids for the glycogen phosphorylase inhibitor site via crystallography, kinetics and QM/MM-PBSA binding studies: Comparison of chrysin and flavopiridol
Tsitsanou, K. E.; Hayes, J. M.; Keramioti, M.; Mamais, M.; Oikonomakos, N. G.; Kato, A.; Leonidas, D. D.; Zographos, S. E. (2013)Flavonoids have been discovered as novel inhibitors of glycogen phosphorylase (GP), a target to control hyperglycemia in type 2 diabetes. To elucidate the mechanism of inhibition, we have determined the crystal structure ... -
Structure based inhibitor design targeting glycogen phosphorylase b. Virtual screening, synthesis, biochemical and biological assessment of novel N-acyl-beta-D-glucopyranosylamines
Parmenopoulou, V.; Kantsadi, A. L.; Tsirkone, V. G.; Chatzileontiadou, D. S. M.; Manta, S.; Zographos, S. E.; Molfeta, C.; Archontis, G.; Agius, L.; Hayes, J. M.; Leonidas, D. D.; Komiotis, D. (2014)Glycogen phosphorylase (GP) is a validated target for the development of new type 2 diabetes treatments. Exploiting the Zinc docking database, we report the in silico screening of 1888 N-acyl-beta-D-glucopyranosylamines ...