A5077442406- RNA and protein synthesis mechanisms
- Tuberculosis Research and Epidemiology
- Redox biology and oxidative stress
- Computational Drug Discovery Methods
- Antimicrobial Resistance in Staphylococcus
- Antimicrobial Peptides and Activities
- Bacterial Genetics and Biotechnology
- Cancer therapeutics and mechanisms
- Synthesis and biological activity
- Free Radicals and Antioxidants
- Bacterial biofilms and quorum sensing
- Fibroblast Growth Factor Research
- Biochemical and Structural Characterization
- Synthesis and Reactivity of Heterocycles
- Glioma Diagnosis and Treatment
- Antibiotic Resistance in Bacteria
- Protein Kinase Regulation and GTPase Signaling
- Quinazolinone synthesis and applications
- Cancer Mechanisms and Therapy
- Kruppel-like factors research
- Mycobacterium research and diagnosis
- Biochemical and Molecular Research
- Genomics, phytochemicals, and oxidative stress
- Histone Deacetylase Inhibitors Research
- DNA Repair Mechanisms
Institute of Molecular Biology and Genetics
2014-2024
National Academy of Sciences of Ukraine
2008-2023
National University Zaporizhzhia Polytechnic
2022
Instituto de Biomedicina y Genética Molecular de Valladolid
2019
Institute of Software Systems
2019
Palladin Institute of Biochemistry
2008
Apoptosis signal-regulating kinase 1 (ASK1) has recently emerged as an attractive therapeutic target for the treatment of cardiac and neurodegenerative disorders. The selective inhibitors ASK1 may become important compounds development clinical agents. We have identified inhibitor among 3H-naphtho[1,2,3-de]quinoline-2,7-diones using receptor-based virtual screening. In vitro assay revealed that ethyl 2,7-dioxo-2,7-dihydro-3H-naphtho[1,2,3-de]quinoline-1-carboxylate (NQDI-1) inhibited with a...
In this article, the derivatives of 3-quinoline carboxylic acid were studied as inhibitors protein kinase CK2. Forty-three new compounds synthesized. Among them 22 inhibiting CK2 with IC50 in range from 0.65 to 18.2 μM identified. The most active found among tetrazolo-quinoline-4-carboxylic and 2-aminoquinoline-3-carboxylic derivatives.
A screen of 37 compounds identified four inhibitors that exhibited dual on-target activity against <italic>Mycobacterium tuberculosis</italic> aminoacyl-tRNA synthetases.
The increase of antibiotic resistance amongst Mycobacterium tuberculosis strains has become one the most pressing problems modern medicine. Therefore, search antibiotics against M. with novel mechanisms action is very important. We have identified inhibitors leucyl-tRNA synthetase (LeuRS) among derivatives 5-phenylamino-2H-[1,2,4]triazin-3-one. active compounds 5-(5-chloro-2-hydroxy-phenylamino)-6-methyl-2H-[1,2,4]triazin-3-one and 5-(5-chloro-2-hydroxy-phenylamino)-2H-[1,2,4]triazin-3-one...
Benzothiazole based cyanine dyes with bridged groups in the pentamethine chain were studied as potential far-red fluorescent probes for protein detection. Spectral-luminescent properties characterized unbound and presence of serum albumins (bovine (BSA), human (HSA), equine (ESA)), globular proteins (β-lactoglobulin, ovalbumin). We have observed that addition leads to a significant increase fluorescence intensity. However, response other was notably lower. The value quantum yield dye bearing...
Keywords: O6-methylguanine-DNA methyltransferase (MGMT), new inhibitors, glioma cells, autophagy, alkylating agent
Background: A major focus of tuberculosis drug discovery is aimed at the development novel antibiotics with activity against drug-resistant strains Mycobacterium tuberculosis. Results: We have synthesized ten isoniazid derivatives and investigated for antibacterial toward M. H37Rv isoniazid-resistant strain SRI 1369. It was revealed that only one compound, isonicotinic acid (1-methyl-1H-pyrrol-2-ylmethylene)-hydrazide (1), active minimum inhibitory concentration value 0.14 μM. This compound...
Staphylococcus aureus (S. aureus) is a causative agent of many hospital- and community-acquired infections with the tendency to develop resistance all known antibiotics. Therefore, development novel antistaphylococcal agents urgent need. Sortase A considered promising molecular target for agents. The main aim this study was identify sortase inhibitors. In order find agents, we performed phenotypic screening library containing 15512 compounds against S. ATCC43300. docking hits using DOCK...
Abstract Antibiotic resistance is a major problem of tuberculosis treatment. This provides the stimulus for search novel molecular targets and approaches to reduce or forestall emergence in Mycobacterium . Earlier, we discovered small-molecular inhibitor among 3-phenyl-5-(1-phenyl-1H-[1,2,3]triazol-4-yl)-[1,2,4]oxadiazoles targeting simultaneously two enzymes—mycobacterial leucyl-tRNA synthetase (LeuRS) methionyl-tRNA (MetRS), which are promising antibiotic development. Unfortunately,...
Background: The most serious challenge in the treatment of tuberculosis is multidrug resistance Mycobacterium to existing antibiotics. As a strategy overcome we used multitarget drug design approach. purpose work was discover dual-targeted inhibitors mycobacterial LeuRS and MetRS with machine learning. Methods: artificial neural networks were built using module nnet from R 3.6.1. inhibitory activity compounds toward investigated aminoacylation assays. Results: Using machine-learning...
The purpose of the research is to determine effectiveness practical application social media based on Web 2.0 technologies, aimed at developing students' English-speaking communicative competence. To implement tasks and test hypothesis put forward, following scientific methods were used: empirical (experimental learning using 2.0); diagnostic: observation, testing students; statistical method - mathematical analysis data obtained during experiment; descriptive: description verbal recording...
Apoptosis signal-regulating kinase 1 (ASK1) is serine/threonine of 5 that activates MAP-kinase (MAPKKK5).ASK1 induces apoptosis via the JNK and p38 signaling pathways.This review focused on three main characteristics ASK1: structure , regulatory mechanisms activity physiological role.ASK1 required for induced by oxidative stress, TNF-a, Fas endoplasmic reticulum.It also regulates differentiation death neurons.ASK1 has been shown to be innate immune response.This a critical molecule cardiac...
Bacterial success in colonizing complex environments requires individual response to micro-scale conditions as well community-level cooperation produce large-scale structures such biofilms. Connecting and community responses could be achieved by linking the intracellular sensory regulatory systems mediated bis-(3′-5′)-cyclic dimeric guanosine monophosphate (c-di-GMP) other compounds of individuals with intercellular quorum sensing (QS) regulation controlling populations.There is growing...