Πλοήγηση ανά Συγγραφέα "Leonidas, D. D."

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 ...

Anopheles gambiae odorant binding protein crystal complex with the synthetic repellent DEET: implications for structure-based design of novel mosquito repellents

Tsitsanou, K. E.; Thireou, T.; Drakou, C. E.; Koussis, K.; Keramioti, M. V.; Leonidas, D. D.; Eliopoulos, E.; Iatrou, K.; Zographos, S. E. (2012)

Insect odorant binding proteins (OBPs) are the first components of the olfactory system to encounter and bind attractant and repellent odors emanating from various sources for presentation to olfactory receptors, which ...

The binding of beta-D-glucopyranosyl-thiosemicarbazone derivatives to glycogen phosphorylase: A new class of inhibitors

Alexacou, K. M.; Tenchiu, A. C.; Chrysina, E. D.; Charavgi, M. D.; Kostas, I. D.; Zographos, S. E.; Oikonomakos, N. G.; Leonidas, D. D. (2010)

Glycogen phosphorylase (GP) is a promising target for the treatment of type 2 diabetes. In the process of structure based drug design for GP, a group of 15 aromatic aldehyde 4-(beta-D-glucopyranosyl) thiosemicarbazones ...

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 ...

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 ...

Halogen-substituted (C-beta-D-glucopyranosyl)-hydroquinone regioisomers: Synthesis, enzymatic evaluation and their binding to glycogen phosphorylase

Alexacou, K. M.; Zhang, Y. Z.; Praly, J. P.; Zographos, S. E.; Chrysina, E. D.; Oikonomakos, N. G.; Leonidas, D. D. (2011)

Electrophilic halogenation of C-(2,3,4,6-tetra-O-acetyl-b-D-glucopyranosyl) 1,4-dimethoxybenzene (1) afforded regioselectively products halogenated at the para position to the D-glucosyl moiety (8, 9) that were deacetylated ...

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 ...

Inhibitor design for ribonuclease A: the binding of two 5 '-phosphate uridine analogues

Tsirkone, V. G.; Dossi, K.; Drakou, C.; Zographos, S. E.; Kontou, M.; Leonidas, D. D. (2009)

In the quest for the rational design of selective and potent inhibitors for members of the pancreatic ribonuclease A (RNase A) family of biomedical interest, the binding of uridine 5'-phosphate (U5P) and uridine 5'-diphosphate ...

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 ...

Non-contact Current Transfer Induces the Formation and Improves the X-ray Diffraction Quality of Protein Crystals

Boltsis, I.; Lagoumintzis, G.; Chatzileontiadou, D. S. M.; Giastas, P.; Tzartos, S. J.; Leonidas, D. D.; Poulas, K. (2014)

The effect of non-contact current transfer on the crystallization of three model proteins (hen egg white lysozyme, bovine pancreatic ribonuclease A, and human recombinant insulin) was investigated using a prototype ...

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 ...

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 ...