A5073667895- Epigenetics and DNA Methylation
- Lung Cancer Research Studies
- Chemical Reaction Mechanisms
- Cancer-related gene regulation
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer, Stress, Anesthesia, and Immune Response
- Porphyrin and Phthalocyanine Chemistry
- Organic Chemistry Cycloaddition Reactions
- Synthesis and Biological Evaluation
- Pharmacological Effects of Medicinal Plants
- Electrochemical Analysis and Applications
- Porphyrin Metabolism and Disorders
- Curcumin's Biomedical Applications
- Folate and B Vitamins Research
- Cytokine Signaling Pathways and Interactions
- Nanoplatforms for cancer theranostics
- Apelin-related biomedical research
- Luminescence and Fluorescent Materials
- Inflammatory mediators and NSAID effects
- Photodynamic Therapy Research Studies
- Biochemical effects in animals
- COVID-19 Impact on Reproduction
- RNA modifications and cancer
- Cancer Immunotherapy and Biomarkers
- Biochemical and Molecular Research
Charles University
2020-2024
General University Hospital in Prague
2020-2023
National Institute of Standards and Technology
2023
Université de Lorraine
2023
Background: Angiotensin-converting enzyme (ACE) is responsible for the production of angiotensin II, and increased II observed in diabetes. What more, ACE polymorphisms may play a role development diabetic nephropathy. The aim this study was to assess selected (rs4343 rs4646994) risk nephropathy likelihood renal replacement therapy. Methods: were analyzed group 225 patients who divided into three subgroups. rs4343 polymorphism determined using PCR-RFLP, rs4646994 PCR. Molecular docking...
Dysregulation of iron homeostasis is one the important processes in development many oncological diseases, such as pancreatic cancer. Targeting it with specific agents, an chelator, are promising therapeutic methods. In this study, we tested cytotoxicity novel azulene hydrazide-hydrazone-based chelators against cancer cell lines (MIA PaCa-2, PANC-1, AsPC-1). All prepared (compounds 4-6) showed strong and high selectivity for compared to healthy line. Their lower than thiosemicarbazone-based...
Abstract Immune checkpoints regulate the immune system response. Recent studies suggest that flavonoids, known as phytoestrogens, may inhibit PD-1/PD-L1 axis. We explored potential of estrogens and 17 Selective Estrogen Receptor Modulators (SERMs) inhibiting ligands for checkpoint proteins (CTLA-4, PD-L1, PD-1, CD80). Our docking revealed strong binding energy values quinestrol, quercetin, bazedoxifene, indicating their to PD-1 CTLA-4. Quercetin modulate EGFR IL-6R alongside estrogen...
Mitochondria generate energy and building blocks required for cellular growth function. The notion that mitochondria are not involved in the cancer has been challenged recent years together with emerging idea of as a promising therapeutic target oncologic diseases. Pentamethinium salts, cyan dyes positively charged nitrogen on benzothiazole or indole part molecule, were originally designed mitochondrial probes. In this study, we show pentamethinium salts have strong effect mitochondria,...
The study of human protoporphyrinogen oxidase (hPPO) inhibition can contribute significantly to a better understanding some pathogeneses (e.g., porphyria, herbicide exposure) and the development anticancer agents. Therefore, we prepared new potential inhibitors with Schiff base structural motifs (2-hydroxybenzaldehyde-based bases 9–13 chromanone derivatives 17–19) as structurally relevant PPO herbicides. inhibitory activities (represented by half maximal concentration (IC50) values)...
Targeting of epigenetic mechanisms, such as the hydroxymethylation DNA, has been intensively studied, with respect to treatment many serious pathologies, including oncological disorders. Recent studies demonstrated that promising therapeutic strategies could potentially be based on inhibition TET1 protein (ten-eleven translocation methylcytosine dioxygenase 1) by specific iron chelators. Therefore, in present work, we prepared a series pyrrolopyrrole derivatives hydrazide (1) or hydrazone...
Abstract Proton pump inhibitors, such as omeprazole, pantoprazole and lansoprazole, are an important group of clinically used drugs. Generally, they considered safe without direct toxicity. Nevertheless, their long‐term use can be associated with a higher risk some serious pathological states (e.g. amnesia oncological neurodegenerative states). It is well known that dysregulation the metabolism transition metals (especially iron ions) plays significant role in these above drugs form...
IL-6 signaling is involved in the pathogenesis of a number serious diseases, including chronic inflammation and cancer. Targeting receptor (IL-6R) by small molecules therefore an intensively studied strategy cancer treatment. We describe design, synthesis, characteristics two new bis-pentamethinium salts 5 6 (meta para) bearing indole moieties. Molecular docking studies showed that both compounds have potential to bind IL-6R (free energy binding -9.5 -8.1 kcal/mol). The interaction with was...
SARS-CoV-2 is a serious viral pathogen, and agents that inhibit its replication are in high demand. In the present work, we prepared two novel tryptanthrin derivates bearing thiosemicarbazone moiety as potential antiviral agents. Both compounds displayed potent chelation activity against Fe(III/II) ion-associated COVID-19. The molecular docking results suggest can display significant affinity towards papain-like proteases main proteases. addition, administering T8H-TSC repress used model...
The concept of intratumoral microbiota is gaining attention in current research. Tumor-associated can activate oncogenic signaling pathways such as NF-κB, thereby promoting tumor development and progression. Numerous studies have demonstrated that curcumin its analogs possess strong antitumor effects by targeting the NF-κB pathway, along with potent antibacterial properties. In this study, we tested activity two curcuminoids, Py-cPen V-cPen, against Gram-negative bacterial strains
Pentamethinium indolium salts are promising fluorescence probes and anticancer agents with high mitochondrial selectivity. We synthesized two pentamethinium salts: a cyclic form quinoxaline directly incorporated in the chain (cPMS) an open substitution γ-position (oPMS). To better understand their properties, we studied interaction phospholipids (cardiolipin phosphatidylcholine) by spectroscopic methods (UV-Vis, fluorescence, NMR spectroscopy). Both compounds displayed significant affinity...