A5045416342- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- RNA and protein synthesis mechanisms
- Enzyme function and inhibition
- Peptidase Inhibition and Analysis
- Natural product bioactivities and synthesis
- HIV/AIDS drug development and treatment
- Chemical Synthesis and Analysis
- RNA Research and Splicing
- Medical Imaging Techniques and Applications
- Boron Compounds in Chemistry
- Endoplasmic Reticulum Stress and Disease
- Metal complexes synthesis and properties
- Biological Activity of Diterpenoids and Biflavonoids
- Lanthanide and Transition Metal Complexes
- Pesticide and Herbicide Environmental Studies
- Synthesis and biological activity
- Plant biochemistry and biosynthesis
- Hereditary Neurological Disorders
- RNA Interference and Gene Delivery
- HIV Research and Treatment
- Synthesis and Catalytic Reactions
- Insect and Pesticide Research
- Galectins and Cancer Biology
Institute of Molecular and Translational Medicine
2018-2024
Palacký University Olomouc
2018-2024
Carbonic anhydrase IX (CAIX) is a transmembrane enzyme that regulates pH in hypoxic tumors and promotes tumor cell survival. Its expression associated with the occurrence of metastases poor prognosis. Here, we present nine derivatives cobalt bis(dicarbollide)(1-) anion substituted at boron or carbon sites by alkysulfamide group(s) as highly specific selective inhibitors CAIX. Interactions these compounds active site CAIX were explored on atomic level using protein crystallography. Two...
A set of fifteen triterpenoid pyrazines and pyridines was prepared from parent 3-oxoderivatives (betulonic acid, dihydrobetulonic oleanonic moronic ursonic heterobetulonic allobetulone). Cytotoxicity all compounds tested in eight cancer two non-cancer cell lines. Evaluation the structure-activity relationships revealed that core determined whether final molecule is active or not, while heterocycle able to increase activity modulate specificity. Five (1b, 1c, 2b, 2c, 8) were found be...
Abstract All four isomeric series of novel 4‐substituted pyrido‐fused 7‐deazapurine ribonucleosides possessing the pyridine nitrogen atom at different positions were designed and synthesized. The total synthesis each fused heterocycle through multistep heterocyclization was followed by glycosylation derivatization position 4 cross‐coupling reactions or nucleophilic substitutions. compounds tested for cytostatic antiviral activity. most active pyrido[4′,3′:4,5]pyrimidine nucleosides bearing...
Here, we have identified the interaction site of contraceptive drug gamendazole using computational modeling. The was previously described as a ligand for eukaryotic translation elongation factor 1-α 1 (eEF1A1) and found to be potential target derivatives 2-phenyl-3-hydroxy-4(1 H)-quinolinones (3-HQs), which exhibit anticancer activity. this class 3-HQs with eEF1A1 inside cancer cells confirmed via pull-down assay. We designed synthesized new family subsequently applied isothermal titration...
We present a novel series of radioiodinated tracers and potential theranostics for diseases accompanied by pathological function proteins involved in choline transport. Unlike analogues labeled with 11C or 18F that are currently used the clinic, iodinated compounds described herein applicable positron emission tomography, single-photon computed potentially therapy, depending on iodine isotope selection. Moreover, favorable half-lives isotopes result much less challenging synthesis exchange...
The broad-spectrum herbicide, glyphosate, is considered safe for animals because it selectively affects the shikimate pathway that specific to plants and microorganisms. We sought a previously unknown mechanism explain concerns glyphosate exposure can negatively affect animals, including humans. Computer modeling showed probable interaction between eukaryotic translation elongation factor 1 subunit alpha (eEF1α1), which was confirmed by microcalorimetry. Only restricted, nondisrupted...
The effects of two anticancer active copper(II) mixed-ligand complexes the type [Cu(qui)(mphen)]Y·H2O, where Hqui = 2-phenyl-3-hydroxy- 1H-quinolin-4-one, mphen bathophenanthroline, and Y NO3 (complex 1) or BF4 2) on activities different isoenzymes cytochrome P450 (CYP) have been evaluated. screening revealed significant inhibitory CYP3A4/5 (IC50 values were 2.46 4.88 μM), CYP2C9 16.34 37.25 CYP2C19 61.21 77.07 μM). Further, analysis mechanisms action uncovered a non-competitive inhibition...
ADVERTISEMENT RETURN TO ISSUEPREVExpression of Concer...Expression ConcernNEXTExpression Concern for "Identification Eukaryotic Translation Elongation Factor 1-α 1 Gamendazole-Binding Site Binding 3-Hydroxy-4(1H)-quinolinones as Novel Ligands with Anticancer Activity"Kristyna BurglováKristyna BurglováMore by Kristyna Burglová, Gabriela RylováGabriela RylováMore Rylová, Athanasios MarkosAthanasios MarkosMore Markos, Hana PrichystalovaHana PrichystalovaMore Prichystalova, Miroslav...