A5015344847- Biopolymer Synthesis and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Amino Acid Enzymes and Metabolism
- Garlic and Onion Studies
- Adenosine and Purinergic Signaling
- Peptidase Inhibition and Analysis
- HIV/AIDS drug development and treatment
- Calcium signaling and nucleotide metabolism
- Cancer Research and Treatments
- Biochemical and Molecular Research
- Histone Deacetylase Inhibitors Research
Engelhardt Institute of Molecular Biology
2021-2025
In recent years, a number of synthetic potentiators antibiotics have been discovered. Their action can significantly enhance the antibacterial effect and limit spread antibiotic resistance through inhibition bacterial cystathionine-γ-lyase. To expand known set potentiators, we developed methods for synthesis five new representatives 6-bromoindole derivatives—potential inhibitors cystathionine-γ-lyase—namely potassium 3-amino-5-((6-bromoindolyl)methyl)thiophene-2-carboxylate (MNS2) its...
Diallyl thiosulfinate (allicin) effectively inhibits the growth of various microorganisms, including antibiotic-resistant strains, so it can be considered to a broad-spectrum antimicrobial compound. However, its instability in bloodstream hinders use as therapeutic agent. We have synthesized number allicin analogues, both natural and synthetic, evaluated vitro their properties against Staphylococcus aureus Candida albicans. The compounds were shown exhibited more pronounced antifungal...
Acute and subchronic toxicity of the pharmacological pair based on encapsulated Citrobacter freundii C115H methionine γ-lyase enzyme/prodrug (methiin) was studied in female ICR mice. The drug showed a weak/moderate dose-dependent hepatotoxic effect. Most changes liver morphology identified were insignificant or mild deviations from norm. Long-term use single therapeutic dose per mouse 1.5 U C. @ (PEG-P(Asp)70/PLL70)-PIC-some/2 mg methiin led to slight decrease weight animals without obvious...
Background: Histone deacetylases (HDACs) are critical epigenetic modulators involved in regulating various molecular mechanisms essential for cell development and growth. Alterations HDAC activity have been linked to the progression of numerous cancers, including lymphoma. Over past decade, FDA has approved several inhibitors lymphoma treatment, leading heightened interest this emerging class drugs. Methods: In our research, we developed a novel inhibitor that exhibits high selectivity I...
The development of anticancer drugs based on zinc-dependent histone deacetylase inhibitors (HDACi) has acquired great practical significance over the past decade. most important HDACi characteristics are selectivity and strength inhibition since they determine mechanisms therapeutic action. For in-cell testing de novo-synthesized HDACi, Western blot analysis level acetylation bona fide protein substrates HDACs each class is usually used. However, high labor intensity this method prevents its...
Recent evidence suggests that fibrotic liver injury in patients with chronic hepatitis C correlates cellular senescence damaged tissue. However, it is still unclear how can affect replication of the virus (HCV). In this work, we report an inhibitor cyclin-dependent kinases 4/6, palbociclib, not only induced hepatoma cells a pre-senescent phenotype, including G1 arrest cell cycle, but also accelerated viral replicon multiplication. Importantly, suppression HCV by direct acting antivirals...