A5087659185- Histone Deacetylase Inhibitors Research
- Acute Myeloid Leukemia Research
- Epigenetics and DNA Methylation
- Protein Degradation and Inhibitors
- Sirtuins and Resveratrol in Medicine
- Student Assessment and Feedback
- Trypanosoma species research and implications
- Educational Assessment and Improvement
- Electrochemical sensors and biosensors
- Macrophage Migration Inhibitory Factor
- Enzyme Production and Characterization
- Advanced Nanomaterials in Catalysis
- Teacher Education and Leadership Studies
- Parasites and Host Interactions
- Autophagy in Disease and Therapy
- Cannabis and Cannabinoid Research
- Neurotransmitter Receptor Influence on Behavior
- Computational Drug Discovery Methods
- Pharmacological Receptor Mechanisms and Effects
- Enzyme-mediated dye degradation
- Signaling Pathways in Disease
- Synthesis and biological activity
Martin Luther University Halle-Wittenberg
2018-2023
Helmholtz-Zentrum Dresden-Rossendorf
2017
Leibniz Association
2014
Twin Cities Orthopedics
2009
University of Minnesota
2009
The versatile oxidase enzyme laccase was immobilized on porous supports such as polymer membranes and cryogels with a view of using biocatalysts in bioreactors aiming at the degradation environmental pollutants wastewater. Besides large surface area for supporting biocatalyst, aforementioned systems also offer possibility simultaneous filtration applications wastewater treatment. Herein "green" water-based, initiator-free, straightforward route to highly reactive membrane cryogel-based is...
Posttranslational modification of proteins by reversible acetylation regulates key biological processes. Histone deacetylases (HDACs) catalyze protein deacetylation and are frequently dysregulated in tumors. This has spurred the development HDAC inhibitors (HDACi). Such epigenetic drugs modulate acetylation, eliminate tumor cells, approved for treatment blood cancers.
The FMS-like tyrosine kinase-3 (FLT3) is mutated in ~30% of acute myeloid leukemia (AML) patients.Common FLT3 mutations are internal tandem duplications (FLT3-ITD) and point its c-terminal kinase domain (FLT3-TKD).The resulting active receptors promote cell proliferation resistance to programmed death (apoptosis) [1].The poor prognosis patients with FLT3-ITD has spurred an intensive search for inhibitors (FLT3i) [2].These include the nanomolar FLT3i quizartinib, which produced promising...
Abstract Schistosomiasis is a neglected parasitic disease that affects more than 265 million people worldwide and for which the control strategy relies on mass treatment with only one drug: praziquantel. Based 3‐chlorobenzothiophene‐2‐hydroxamic acid J1075 , series of hydroxamic acids different scaffolds were prepared as potential inhibitors Schistosoma mansoni histone deacetylase 8 ( Sm HDAC8). The crystal structures HDAC8 four provided insight into binding mode orientation molecules in...
Writing and erasing of posttranslational modifications are crucial to phenotypic plasticity antigenic variation eukaryotic pathogens. Targeting pathogens' modification machineries, thus, represents a valid approach fighting parasitic diseases. However, identification targets the development selective anti-parasitic drugs still represent major bottlenecks. Here, we show that zinc-dependent histone deacetylases (HDACs) protozoan parasite Trypanosoma cruzi key regulators have significantly...
Epigenetic modifiers of the histone deacetylase (HDAC) family are often dysregulated in cancer cells. Experiments with small molecule HDAC inhibitors (HDACi) have proven that HDACs a vulnerability transformed We evaluated novel hydroxamic acid-based HDACi (KH16; termed yanostat) human pancreatic ductal adenocarcinoma (PDAC) cells, short- and long-term cultured colorectal (CRC) retinal pigment epithelial show KH16 induces cell cycle arrest apoptosis, both time dose dependently PDAC CRC This...
Cannabinoid type 2 receptors (CB2 receptors) are involved in various pathological processes, and the visualization of their vivo availability with positron emission tomography (PET) is high interest. The study focuses on introduction fluorine into structure highly affine selective CB2 receptor ligand N-(adamantan-1-yl)-5-ethyl-2-methyl-1-phenyl-1H-imidazole-4-carboxamide (5). A novel series compounds was developed by modifying (i) adamantane-3-position, (ii) imidazole-N-phenyl ring, (iii)...
Abstract Introduction Posttranslational modification of proteins by reversible acetylation regulates key biological processes. Histone deacetylases (HDACs) catalyze protein deacetylation and are frequently dysregulated in tumors. This has spurred the development HDAC inhibitors (HDACi). Such epigenetic drugs modulate acetylation, eliminate tumor cells, approved for treatment blood cancers. Objectives We aimed to identify novel, nanomolar HDACi with increased potency over existing agents...