Demetres D. Leonidas

Recognition of Ribonuclease A by 3′–5′-Pyrophosphate-Linked Dinucleotide Inhibitors: A Molecular Dynamics/Continuum Electrostatics Analysis

Polydoridis, Savvas, Leonidas, Demetres D., Oikonomakos, Nikos G., Archontis, Georgios

The proteins of the pancreatic ribonuclease A (RNase A) family catalyze the cleavage of the RNA polymer chain. The development of RNase inhibitors is of significant interest, as some of these...

Crystallographic studies on acyl ureas, a new class of glycogen phosphorylase inhibitors, as potential antidiabetic drugs

Oikonomakos, Nikos G., Kosmopoulou, Magda N., Chrysina, Evangelia D., Leonidas, Demetres D., Kostas, Ioannis D., Wendt, K. Ulrich, ...

Acyl ureas were discovered as a novel class of inhibitors for glycogen phosphorylase, a molecular target to control hyperglycemia in type 2 diabetics. This series is exemplified by 6-{2,6-Dichloro-...

Kinetic and crystallographic studies on 2-(β-D-glucopyranosyl)-5-methyl-1, 3, 4-oxadiazole, -benzothiazole, and -benzimidazole, inhibitors of muscle glycogen phosphorylase b. Evidence for a new binding site

Chrysina, Evangelia D., Kosmopoulou, Magda N., Tiraidis, Constantinos, Kardakaris, Rozina, Bischler, Nicolas, Leonidas, Demetres D., ...

In an attempt to identify leads that would enable the design of inhibitors with enhanced affinity for glycogen phosphorylase (GP), that might control hyperglycaemia in type 2 diabetes, three new...

The binding of β- and γ-cyclodextrins to glycogen phosphorylase b: Kinetic and crystallographic studies

Pinotsis, Nikos, Leonidas, Demetres D., Chrysina, Evangelia D., Oikonomakos, Nikos G., Mavridis, Irene M.

A number of regulatory binding sites of glycogen phosphorylase (GP), such as the catalytic, the inhibitor, and the new allosteric sites are currently under investigation as targets for inhibition of...

High-resolution crystal structures of ribonuclease A complexed with adenylic and uridylic nucleotide inhibitors. Implications for structure-based design of ribonucleolytic inhibitors

Leonidas, Demetres D., Chavali, Gayatri B., Oikonomakos, Nikos G., Chrysina, Evangelia D., Kosmopoulou, Magda N., Vlassi, Metaxia, ...

The crystal structures of bovine pancreatic ribonuclease A (RNase A) in complex with 3′,5′-ADP, 2′,5′-ADP, 5′-ADP, U-2′-p and U-3′-p have been determined at high resolution. The...

Binding of Phosphate and pyrophosphate ions at the active site of human angiogenin as revealed by X-ray crystallography

Leonidas, Demetres D., Chavali, Gayatri B., Jardine, Anwar M., Li, Songlin, Shapiro, Robert, Acharya, K. Ravi

Human angiogenin (Ang) is an unusual homolog of bovine pancreatic RNase A that utilizes its ribonucleolytic activity to induce the formation of new blood vessels. The pyrimidine-binding site of Ang...

FR258900, a potential anti-hyperglycemic drug, binds at the allosteric site of glycogen phosphorylase

Tiraidis, Costas, Alexacou, Kyra-Melinda, Zographos, Spyros E., Leonidas, Demetres D., Gimisis, Thanasis, Oikonomakos, Nikos G.

FR258900 has been discovered as a novel inhibitor of human liver glycogen phosphorylase a and proved to suppress hepatic glycogen breakdown and reduce plasma glucose concentrations in diabetic mice...