A5075000718- Quinazolinone synthesis and applications
- Phenothiazines and Benzothiazines Synthesis and Activities
- Drug Transport and Resistance Mechanisms
- Synthesis and Characterization of Heterocyclic Compounds
- Drug-Induced Hepatotoxicity and Protection
- Receptor Mechanisms and Signaling
- Enzyme Structure and Function
- Catalytic C–H Functionalization Methods
- Neuroscience and Neuropharmacology Research
- Synthesis and Catalytic Reactions
- Neuropeptides and Animal Physiology
- Protein Structure and Dynamics
- Liver Disease Diagnosis and Treatment
- Neurological Disorders and Treatments
- Advanced Synthetic Organic Chemistry
- Pharmacogenetics and Drug Metabolism
- Congenital Heart Disease Studies
- Peptidase Inhibition and Analysis
- Neurotransmitter Receptor Influence on Behavior
- Pharmacology and Obesity Treatment
- Liver physiology and pathology
- Protease and Inhibitor Mechanisms
- Pharmacological Effects and Toxicity Studies
- Advanced NMR Techniques and Applications
- Chemical Synthesis and Analysis
Monash University
2011-2022
CSIRO Manufacturing
2018-2021
Universitatea de Medicină, Farmacie, Științe și Tehnologie „George Emil Palade” din Târgu Mureș
2016-2020
Semmelweis University
1995-2020
Institute of Cognitive Neuroscience and Psychology
2020
HUN-REN Research Centre for Natural Sciences
2011-2016
Institute of Organic Chemistry
2016
Hungarian Academy of Sciences
2015
Australian Regenerative Medicine Institute
2015
Freie Universität Berlin
1992
Biased agonism at GPCRs highlights the potential for discovery and design of pathway-selective ligands may confer therapeutic advantages to targeting dopamine D2 receptor (D2R). We investigated determinants efficacy, affinity, bias three privileged structures D2R, exploring changes linker length incorporation a heterocyclic unit. Profiling compounds in two signaling assays (cAMP pERK1/2) allowed us identify quantify biased D2R. Substitution on phenylpiperazine (2-methoxy vs 2,3-dichloro)...
Human hepatocytes are the gold standard for toxicological studies but they have several drawbacks, like scarce availability, high inter-individual variability, a short lifetime, which limits their applicability. The aim of our investigations was to determine, whether HepaRG cells could replace human in uptake experiments toxicity studies. is hepatoma cell line with most hepatic functions, including considerable expression transporters contrast other immortalized lines. We compared effect...
Journal Article Elephantiasis nostras verrucosa: beneficial effect of oral etretinate therapy Get access CH.C. ZOUBOULIS, ZOUBOULIS Department Dermatology, University Medical Center Steglitz, The Free Berlin, Germany Dr Ch.C.Zouboulis, Hindenburgdamm 30, W‐l000 Berlin 45, Germany. Search for other works by this author on: Oxford Academic Google Scholar S. BICZÓ, BICZÓ Departments Dermatology H. GOLLNICK, GOLLNICK H.‐J. REUPKE, REUPKE G. RINCK, RINCK M. SZABÓ, SZABÓ J. FEKETE, FEKETE...
Pseudocontact shifts (PCS) generated by paramagnetic lanthanides provide a rich source of long-range structural restraints that can readily be measured nuclear magnetic resonance (NMR) spectroscopy. Many different lanthanide-binding tags have been designed for site-specific tagging proteins, but established routes DNA with single metal ion rely on difficult chemical synthesis. Here we present simple and practical strategy inexpensive phosphorothioate (PT) oligonucleotides. Commercially...
Cathepsin X/Z/P is cysteine cathepsin with unique carboxypeptidase activity. Its expression associated cancer and neurodegenerative diseases, although its roles during normal physiology are still poorly understood. Advances in our understanding of function have been hindered by a lack available tools that can specifically measure the proteolytic activity X. We present series activity-based probes incorporate sulfoxonium ylide warhead, which exhibit improved specificity for X compared to...
SB269652 (1) is a negative allosteric modulator of the dopamine D2 receptor. Herein, we present design, synthesis, and pharmacological evaluation "second generation" analogues 1 whereby subtle modifications to indole-2-carboxamide motif confer dramatic changes in functional affinity (5000-fold increase), cooperativity (100-fold novel action modulate efficacy. Thus, structural this region allows generation set with distinct properties.
Herein we describe the hybridization of a benzoxazinone M1 scaffold with D2 privileged structures derived from putative and clinically relevant antipsychotics to develop designed multiple ligands. The mAChR is an attractive target for cognitive deficits in key CNS disorders. Moreover, activity at 5-HT2A receptors has proven useful antipsychotic efficacy. We identified 9 which retained functional D2R demonstrated high affinity 5-HT2AR.
Several studies have reported that statins occasionally cause impairment of liver functions characterized by elevated serum bilirubin levels, which might be due to altered function the multidrug resistance-associated proteins (Mrp2/3). We aimed study modulation hepatobiliary transport four statin derivatives, atorvastatin, fluvastatin, pravastatin, and rosuvastatin in sandwich-cultured rat hepatocytes. All except pravastatin significantly inhibited uptake bilirubin. The biliary efflux...
Positive allosteric modulators targeting the M<sub>4</sub> muscarinic acetylcholine receptor offer greater sub-type selectivity and unique potential as CNS agents through their novel mode of action to traditional orthosteric ligands.
Abstract. The metallo-β-lactamase IMP-1 features a flexible loop near the active site that assumes different conformations in single crystal structures, which may assist substrate binding and enzymatic activity. To probe position of this loop, we labelled tryptophan residues with 7-13C-indole protein lanthanoid tags at three sites. magnetic susceptibility anisotropy (Δχ) tensors were determined by measuring pseudocontact shifts (PCSs) backbone amide protons. Δχ subsequently used to identify...
Neurotransmitter release depends critically on the neuronal SNARE complex formed by syntaxin-1, SNAP-25 and synaptobrevin, as well other proteins such Munc18-1, Munc13-1 synaptotagmin-1. Although three-dimensional structures are available for these components, it is still unclear how they assembled between synaptic vesicle plasma membranes to trigger fast, Ca2+-dependent membrane fusion. Methyl TROSY NMR experiments provide a powerful tool study complexes proteins, but assignment of methyl...
The aim of this study was to test for the presence prohepcidin in cord blood, gauge its alteration during early postnatal period, and look a possible association with neonatal iron homeostasis. Cord blood venous samples were taken from 20 healthy neonates. In both kinds could be detected. No found between However, an is demonstrated values mean cell hemoglobin concentration (MCHC). Prohepcidin increased postnatally half neonates, indicating active synthesis molecule. Interestingly, neonates...