Biochemical Pharmacology

HEAD OF DEPARTMENT

RNDr. Magdaléna Májeková, PhD.

T: +421 2/32295709,

@: magdalena.majekova@savba.sk,

W: http://www.biopharm.sav.sk

ABOUT THE DEPARTMENT

The main topics of our research are design, development and testing new multi-target oriented compounds for the treatment and prevention of chronic disorders and diseases (diabetes, neurodegenerative diseases, oxidation and glykation stress related tissue damage).

RESEARCH AREAS

Chemical and enzyme mechanisms of molecular oxygen activation and tissue damage under hypoxic conditions. Toxic effects of reactive oxygen species and glucose under conditions of hyperglycemia with main attention to diabetic complications; enzyme mechanisms of polyol pathway in the ethiology of diabetic complications. Oxidative injury of Ca2+-ATPase from sarcoplasmic reticulum and its consequences in calcium homeostasis. In silico approaches in the study of antioxidant activity, ligand-protein interaction, QSAR and virtual screening.


TECHNIQUES

Chemistry and biochemistry of inhibition, activation, induction and spectral properties of proteins. Chemical and physico-chemical methods of study of structural changes of lipids and proteins initiated by reactive compounds (free radicals, advanced glycation products). Cell culture techniques in studying cellular damage by oxidative, osmotic and glycation stress. Animal models of experimental diabetes and models of hypoxia-ischemia. Quantum chemical and molecular mechanics computational methods, ligand-protein interactions (docking and induced fit), homology modeling, combinatorial databases, QSAR, molecular dynamics.

SELECTED PAPERS

HLAVÁČ, Matúš – KOVÁČIKOVÁ, Lucia – ŠOLTÉSOVÁ PRNOVÁ, Marta – ŠRAMEL, Peter – ADDOVÁ, Gabriela – MÁJEKOVÁ, Magdaléna – HANQUET, Gilles – BOHÁČ, A. – ŠTEFEK, Milan**. Development of Novel Oxotriazinoindole Inhibitors of Aldose Reductase: Isosteric Sulfur/Oxygen Replacement in the Thioxotriazinoindole Cemtirestat Markedly Improved Inhibition Selectivity. In Journal of Medicinal Chemistry, 2020, vol. 63, no. 1, p. 369-381.


KOVÁČIKOVÁ, Lucia – ŠOLTÉSOVÁ PRNOVÁ, Marta – MÁJEKOVÁ, Magdaléna – BOHÁČ, A. – KARASU, Çimen – ŠTEFEK, Milan**. Development of Novel Indole-Based Bifunctional Aldose Reductase Inhibitors/Antioxidants as Promising Drugs for the Treatment of Diabetic Complications. In Molecules, 2021, vol. 26, no. 10, art. no. 2867.


RODRÍGUEZ, Yoel – MÁJEKOVÁ, Magdaléna**. Structural Changes of Sarco/Endoplasmic Reticulum Ca2+-ATPase Induced by Rutin Arachidonate: A Molecular Dynamics Study. In Biomolecules : Open Access Journal, 2020, vol. 10, no. 2, art. no. 214.


HEGER, Vladimír – BENEŠOVÁ, Barbora – VISKUPIČOVÁ, Jana – MÁJEKOVÁ, Magdaléna – ZOOFISHAN, Zoofishan – HUNYADI, Attila – HORÁKOVÁ, Ľubica**. Phenolic Compounds from Morus nigra Regulate Viability and Apoptosis of Pancreatic β-Cells Possibly via SERCA Activity. In ACS Medicinal Chemistry Letters, 2020, vol. 11, no. 5, p. 1006-1013.


ŠOLTÉSOVÁ PRNOVÁ, Marta – ŠVÍK, Karol – BEZEK, Štefan – KOVÁČIKOVÁ, Lucia – KARASU, Çimen – ŠTEFEK, Milan**. 3-Mercapto-5H-1,2,4-Triazino[5,6-b] Indole-5-Acetic Acid (Cemtirestat) Alleviates Symptoms of Peripheral Diabetic Neuropathy in Zucker Diabetic Fatty (ZDF) Rats: A Role of Aldose Reductase. In Neurochemical Research, 2019, vol. 44, no. 5, p. 1056-1064.