A5089480666- Histone Deacetylase Inhibitors Research
- Epigenetics and DNA Methylation
- Protein Degradation and Inhibitors
- Sirtuins and Resveratrol in Medicine
- Peptidase Inhibition and Analysis
- Autophagy in Disease and Therapy
- Genetics and Neurodevelopmental Disorders
- Ubiquitin and proteasome pathways
- Biochemical and Structural Characterization
- Pineapple and bromelain studies
- Transgenic Plants and Applications
Martin Luther University Halle-Wittenberg
2020-2025
Luther University
2022-2023
The rapid spread of a novel coronavirus known as SARS-CoV-2 has compelled the entire world to seek ways weaken this virus, prevent its and also eliminate it. However, no drug been approved treat COVID-19. Furthermore, receptor-binding domain (RBD) on viral spike protein, well several other important parts have recently undergone mutations, resulting in new virus variants. While treatment is currently available, naturally derived molecule with antiviral properties could be used potential...
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with pathogenesis cancer neurodegeneration, thus making these two enzymes promising targets for pharmaceutical intervention. Herein, we report design, synthesis, biological characterization first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools inhibition deacetylation. Using biochemical
<title>Abstract</title> Histone deacetylase (HDAC) inhibitors represent a newer class of anti-cancer agents that play key role in both epigenetic and non-epigenetic regulation, leading to cancer cell death, apoptosis, cycle arrest.. These are being tested numerous clinical trials against various diseases, including hematological solid malignancies. In the present study, we synthesized novel bicyclic hydroxamic acid derivatives them vitro I IIb HDACs investigate their inhibitory activity...
Abstract Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, especially cancer. Five HDAC inhibitors have been approved for anticancer therapy and clinical trials. Among the 11 zinc‐dependent HDACs, HDAC10 has received relatively little attention by drug discovery campaigns, despite its involvement, e. g., pathogenesis of neuroblastoma. This is due part to a lack robust enzymatic conversion assays. In contrast protein lysine deacetylase deacylase...
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with pathogenesis cancer neurodegeneration, thus making these two enzymes promising targets for pharmaceutical intervention. Herein, we report design, synthesis, biological characterization first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools inhibition deacetylation. Using biochemical in vitro assays cell-based methods target engagement, identified Mz325 (31) a...
Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, esp. cancer. First HDAC inhibitors have been approved for anticancer therapy and clinical trials. Among the 11 zinc-dependent HDACs, HDAC10 has received relatively little attention by drug discovery campaigns, despite its involvement e.g. pathogenesis of neuroblastoma. This is due part to a lack robust enzymatic conversion assays. In contrast protein lysine deacetylase deacylase activity other...
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with pathogenesis cancer neurodegeneration, thus making these two enzymes promising targets for pharmaceutical intervention. Herein, we report design, synthesis, biological characterization first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools inhibition deacetylation. Using biochemical in vitro assays cell-based methods target engagement, identified Mz325 (31) a...
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with pathogenesis cancer neurodegeneration, thus making these two enzymes promising targets for pharmaceutical intervention. Herein, we report design, synthesis, biological characterization first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools inhibition deacetylation. Using biochemical in vitro assays cell-based methods target engagement, identified Mz325 (33) a...
Histone deacetylases (HDACs) are a family of 18 epigenetic modifiers that fall into 4 classes. deacetylase inhibitors (HDACi) valid tools to assess HDAC functions. HDAC6 and HDAC10 belong the class IIb subgroup family. The targets biological functions ill-defined. This lack knowledge is due specific potent with cellular activity. Here, we have synthesized characterized piperidine-4-acrylhydroxamates as highly selective HDAC10. was achieved by addressing acidic gatekeeper residue Glu274 basic...
Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, especially cancer. Five HDAC inhibitors have been approved for anticancer therapy and clinical trials. Among the 11 zinc-dependent HDACs, HDAC10 has received relatively little attention by drug discovery campaigns, despite its involvement, e.g., pathogenesis of neuroblastoma. This is due part to a lack robust enzymatic conversion assays. In contrast protein lysine deacetylase deacylase activity most...
Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, esp. cancer. First HDAC inhibitors have been approved for anticancer therapy and clinical trials. Among the 11 zinc-dependent HDACs, HDAC10 has received relatively little attention by drug discovery campaigns, despite its involvement e.g. pathogenesis of neuroblastoma. This is due part to a lack robust enzymatic conversion assays. In contrast protein lysine deacetylase deacylase activity other...
Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, esp. cancer. First HDAC inhibitors have been approved for anticancer therapy and clinical trials. Among the 11 zinc-dependent HDACs, HDAC10 has received relatively little attention by drug discovery campaigns, despite its involvement e.g. pathogenesis of neuroblastoma. This is due part to a lack robust enzymatic conversion assays. In contrast protein lysine deacetylase deacylase activity other...
Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, esp. cancer. First HDAC inhibitors have been approved for anticancer therapy and clinical trials. Among the 11 zinc-dependent HDACs, HDAC10 has received relatively little attention by drug discovery campaigns, despite its involvement e.g. pathogenesis of neuroblastoma. This is due part to a lack robust enzymatic conversion assays. In contrast protein lysine deacetylase deacylase activity other...
Histone deacetylases (HDACs) are a family of 18 epigenetic modifiers that fall into 4 classes. deacetylase inhibitors (HDACi) valid tools to assess HDAC functions. HDAC6 and HDAC10 belong the class IIb subgroup family. The targets biological functions ill-defined. This lack knowledge is due specific potent with cellular activity. Here, we have synthesized characterized piperidine-4-acrylhydroxamates as highly selective HDAC10. was achieved by targeting acidic gatekeeper residue Glu274 basic...