Parcourir par auteur "Kantsadi, A. L."
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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 ... -
The binding of C5-alkynyl and alkylfurano 2,3-d pyrimidine glucopyranonucleosides to glycogen phosphorylase b: Synthesis, biochemical and biological assessment
Kantsadi, A. L.; Manta, S.; Psarra, A. M. G.; Dimopoulou, A.; Kiritsis, C.; Parmenopoulou, V.; Skamnaki, V. T.; Zoumpoulakis, P.; Zographos, S. E.; Leonidas, D. D.; Komiotis, D. (2012)C5-alkynyl and allcylfurano[2,3-d]pyrimidine glucopyranonucleosides have been synthesized and studied as inhibitors of glycogen phosphorylase b (GPb). Kinetic experiments have shown that most of these compounds were low ... -
Biochemical and biological assessment of the inhibitory potency of extracts from vinification byproducts of Vitis vinifera extracts against glycogen phosphorylase
Kantsadi, A. L.; Apostolou, A.; Theofanous, S.; Stravodimos, G. A.; Kyriakis, E.; Gorgogietas, V. A.; Chatzileontiadou, D. S. M.; Pegiou, K.; Skamnaki, V. T.; Stagos, D.; Kouretas, D.; Psarra, A. M. G.; Haroutounian, S. A.; Leonidas, D. D. (2014)The inhibitory potency of thirteen polyphenolic extracts obtained from vinification byproducts of Greek varieties of Vitis vinifera against glycogen phosphorylase (GP) has been studied by kinetic experiments. GP is an ... -
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 ... -
Molecular Cloning, Carbohydrate Specificity and the Crystal Structure of Two Sclerotium rolfsii Lectin Variants
Peppa, V. I.; Venkat, H.; Kantsadi, A. L.; Inamdar, S. R.; Bhat, G. G.; Eligar, S.; Shivanand, A.; Chachadi, V. B.; Satisha, G. J.; Swamy, B. M.; Skamnaki, V. T.; Zographos, S. E.; Leonidas, D. D. (2015)SRL is a cell wall associated developmental-stage specific lectin secreted by Sclerotium rolfsii, a soil-born pathogenic fungus. SRL displays specificity for TF antigen (Gal13GalNAc--Ser//Thr) expressed in all cancer types ... -
Natural flavonoids as antidiabetic agents. The binding of gallic and ellagic acids to glycogen phosphorylase b
Kyriakis, E.; Stravodimos, G. A.; Kantsadi, A. L.; Chatzileontiadou, D. S. M.; Skamnaki, V. T.; Leonidas, D. D. (2015)We present a study on the binding of gallic acid and its dimer ellagic acid to glycogen phosphorylase (GP). Ellagic acid is a potent inhibitor with K(i)s of 13.4 and 7.5 mu M, in contrast to gallic acid which displays K(i)s ... -
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 ... -
Structural analysis of the Rhizoctoniasolani agglutinin reveals a domain-swapping dimeric assembly
Skamnaki, V. T.; Peumans, W. J.; Kantsadi, A. L.; Cubeta, M. A.; Plas, K.; Pakala, S.; Zographos, S. E.; Smagghe, G.; Nierman, W. C.; Van Damme, E. J. M.; Leonidas, D. D. (2013)Rhizoctoniasolani agglutinin (RSA) is a 15.5-kDa lectin accumulated in the mycelium and sclerotia of the soil born plant pathogenic fungus R.solani. Although it is considered to serve as a storage protein and is implicated ... -
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 ... -
Triazole pyrimidine nucleosides as inhibitors of Ribonuclease A. Synthesis, biochemical, and structural evaluation
Parmenopoulou, V.; Chatzileontiadou, D. S. M.; Manta, S.; Bougiatioti, S.; Maragozidis, P.; Gkaragkouni, D. N.; Kaffesaki, E.; Kantsadi, A. L.; Skamnaki, V. T.; Zographos, S. E.; Zounpoulakis, P.; Balatsos, N. A. A.; Komiotis, D.; Leonidas, D. D. (2012)Five ribofuranosyl pyrimidine nucleosides and their corresponding 1,2,3-triazole derivatives have been synthesized and characterized. Their inhibitory action to Ribonuclease A has been studied by biochemical analysis and ...