A5037618574- Electron Spin Resonance Studies
- Protein purification and stability
- Viral Infectious Diseases and Gene Expression in Insects
- Synthesis and biological activity
- Cholinesterase and Neurodegenerative Diseases
- Computational Drug Discovery Methods
- DNA and Nucleic Acid Chemistry
- Peptidase Inhibition and Analysis
- Carbohydrate Chemistry and Synthesis
- Synthesis and Biological Evaluation
- Chemical Synthesis and Analysis
- Galectins and Cancer Biology
- Phytochemicals and Antioxidant Activities
- Synthesis and Characterization of Heterocyclic Compounds
- RNA Interference and Gene Delivery
- Monoclonal and Polyclonal Antibodies Research
- Nicotinic Acetylcholine Receptors Study
- Chemical Reaction Mechanisms
- Advancements in Transdermal Drug Delivery
- Click Chemistry and Applications
- Glycosylation and Glycoproteins Research
- Drug Solubulity and Delivery Systems
- Ubiquitin and proteasome pathways
- Magnetism in coordination complexes
- Toxin Mechanisms and Immunotoxins
University of Ljubljana
2012-2024
Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques
2009-2011
Université Paris Cité
2009-2011
Centre National de la Recherche Scientifique
2009-2011
Jožef Stefan Institute
2005-2006
National Institute of Chemistry
2006
Jožef Stefan International Postgraduate School
2005-2006
Ljubljana University Medical Centre
2005
Max Delbrück Center
2005
The structural integrity, elasticity, and fluidity of lipid membranes are critical for cellular activities such as communication between cells, exocytosis, endocytosis. Unsaturated lipids, the main components biological membranes, particularly susceptible to oxidative attack reactive oxygen species. peroxidation unsaturated in our case 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), induces reorganization membrane. We have employed a multi-technique approach analyze typical properties...
A novel class of potential antithrombotic compounds with moderate thrombin inhibitory and fibrinogen receptor antagonistic activity is described. Combination anticoagulant antiaggregatory in the same molecular entity presented as a new promising approach search for agents.
A pigment from the edible mushroom Xerocomus badius norbadione A, which is a natural derivative of pulvinic acid, was found to possess antioxidant properties. Since acid represents novel scaffold, several other derivatives were recently synthetized and evaluated experimentally, along with some structurally related coumarine derivatives. The obtained data formed basis for construction quantitative structure-activity pharmacophore models, employed in virtual screening experiments compound...
Quinazolinones represent an important scaffold in medicinal chemistry with diverse biological activities. Here, two series of 2-substituted quinazolin-4(3H)-ones were synthesized and evaluated for their antioxidant properties using three different methods, namely DPPH, ABTS TEACCUPRAC, to obtain key information about the structure–antioxidant activity relationships a set substituents at position 2 main quinazolinone scaffold. Regarding activity, TEACCUPRAC assays more sensitive gave reliable...
Polysorbates, widely used excipients in drug formulations, present a stability challenge due to complex degradation processes. This study investigates the hydrolysis of polysorbate (PS) under temperature stress (50 °C), focusing on impact primary packaging materials (glass vs. plastic vials), buffers (histidine and acetic acid), counterions (chloride malate), pH (4-7). Our findings reveal that leachables from vials inhibit PS both histidine acid buffers. Kinetic parameters derived sigmoidal...
Alkylphospholipid analogues of perifosine and miltefosine bearing a nitroxide moiety at different positions on an alkyl chain were synthesized as electron paramagnetic resonance (EPR) probes. Their amphiphilic properties characterized by determining their critical micelle concentration (cmc) hemolytic activity erythrocytes both in free liposomal form. Spin-labeled membrane components large unilamellar liposomes containing cholesterol dicetyl phosphate or solution evaluated using the MTT...
Proteins are prone to post-translational modifications at specific sites, which can affect their physicochemical properties, and consequently also safety efficacy. Sources of include oxygen reactive species. Additionally, catalytic amounts Fe(II) or Cu(I) promote increased activities species, thus catalyse the production particularly hydroxyl radicals. When oxidative detected in biopharmaceutical industry, it is common practice add chelators formulation. However, resultant complexes with...
Abstract DC‐SIGN, an antigen‐uptake receptor in dendritic cells (DCs), has a clear role the immune response but, conversely, can also facilitate infection by providing entry of pathogens into DCs. The key action both processes is internalization acidic endosomes and lysosomes. Molecular probes that bind to DC‐SIGN could thus provide useful tool study constitute potential antagonists against pathogens. So far, only large molecules have been used directly observe DC‐SIGN‐mediated DCs...
A library of 31 butyrylcholinesterase (BChE) and cathepsin B (CatB) inhibitors was screened in vitro for inhibition deoxyribonuclease I (DNase I). Compounds 22, 8 7 are among the most potent synthetic non-peptide DNase reported to date. Three 8-hydroxyquinoline analogues inhibited both BChE with IC50 values below 35 μM 50 nM, respectively, while two nitroxoline derivatives Cat endopeptidase activity 60 20 μM. Selected were various co-target binding affinities at dopamine D2 D3 , histamine H3...
The immunoproteasome is a multicatalytic protease that predominantly expressed in cells of hematopoietic origin. Its elevated expression has been associated with autoimmune diseases, various types cancer, and inflammatory diseases. development immunoproteasome-selective inhibitors non-peptidic scaffolds remains challenging task. Here, we describe focused series psoralen-based the β5i subunit different substituents placed at position 4'. most promising compound was further evaluated through...
Molecular dynamics simulation has been performed to investigate the structural properties of perifosine and its synthetic spin-labeled alkylphospholipid analogues. The conformations adopted by these compounds in water a dipalmitoylphosphatidylcholine bilayer as function presence position N-oxyl-4',4'-dimethyloxazolidine ring (doxyl group) have investigated all-atom molecular dynamics. No predominant conformation was observed water, but molecules adopt specific orientations lipid bilayer. As...
A convenient and efficient total synthesis of ezetimibe, an intestinal cholesterol absorption inhibitor useful anticholesteremic agent, is described. Based on (Z)-5-(4-fluorophenyl)pent-4-enoic acid as a starting compound, taking the through further Z-configured intermediates, yield remarkably increased, compared with use corresponding E-configured substances or intermediates.
Abstract Galectin‐8 has gained attention as a potential new pharmacological target for the treatment of various diseases, including cancer, inflammation, and disorders associated with bone mass reduction. To that end, molecular probes are needed in order to better understand its role functions. Herein we aimed improve affinity selectivity recently published galectin‐8 ligand, 3‐ O ‐[1‐carboxyethyl]‐β‐ d ‐galactopyranoside, by introducing modifications at positions 1 3 galactose. Affinity...