A5030176459- Neuroblastoma Research and Treatments
- Cancer, Hypoxia, and Metabolism
- Virus-based gene therapy research
- Histone Deacetylase Inhibitors Research
- Protein Degradation and Inhibitors
- Parasites and Host Interactions
- Peptidase Inhibition and Analysis
- Cholinesterase and Neurodegenerative Diseases
- Cancer-related gene regulation
- PARP inhibition in cancer therapy
- Pneumocystis jirovecii pneumonia detection and treatment
- Phytochemical compounds biological activities
- Lung Cancer Research Studies
- Research on Leishmaniasis Studies
- Ubiquitin and proteasome pathways
- Hippo pathway signaling and YAP/TAZ
- Parasitic infections in humans and animals
- Calcium signaling and nucleotide metabolism
- Synthetic Organic Chemistry Methods
- Click Chemistry and Applications
- RNA Research and Splicing
- Trypanosoma species research and implications
- HIV/AIDS drug development and treatment
- Sirtuins and Resveratrol in Medicine
Martin Luther University Halle-Wittenberg
2017-2025
Luther University
2022-2023
Alexandria University
2022
Abstract Background Neuroblastoma is the most common solid tumor in infants accounting for approximately 15% of all cancer-related deaths. Over 50% high-risk neuroblastoma relapse, emphasizing need novel drug targets and therapeutic strategies. In neuroblastoma, chromosomal gains at chromosome 17q, including IGF2BP1 , MYCN amplification 2p are associated with adverse outcome. Recent, pre-clinical evidence indicates feasibility direct indirect targeting cancer treatment. Methods Candidate...
Histone deacetylases (HDACs) are important modulators of epigenetic gene regulation and additionally control the activity non-histone protein substrates. While for HDACs 1–3 6 many potent selective inhibitors have been obtained, other subtypes much less is known on consequences their inhibition. The present report describes development substituted benzhydroxamic acids as HDAC8 inhibitors. Docking studies using available crystal structures used structure-based optimization this series...
In addition to involvement in epigenetic gene regulation, histone deacetylases (HDACs) regulate multiple cellular processes through mediating the activity of non-histone protein substrates. The knockdown HDAC8 isozyme is associated with inhibition cell proliferation and apoptosis enhancement several cancer lines. As shown studies, can be considered a potential target treatment forms such as childhood neuroblastoma. present work describes development proteolysis targeting chimeras (PROTACs)...
Abstract The Hippo/YAP1 signaling pathway regulates normal development by controlling contact inhibition of growth. In cancer, YAP1 activation is often dysregulated, leading to excessive tumor growth and metastasis. SRC kinase can cross talk Hippo disrupting adherens junctions, repressing the cascade, or activating promote proliferation. Here, we demonstrate that IGF2 messenger RNA-binding protein 1 (IGF2BP1) impedes repression in carcinomas. IGF2BP1 stabilizes RNA (mRNA) enhances synthesis...
We developed a one-step direct assay for the determination of histone deacylase (HDAC) activity by substituting carbonyl oxygen acyl moiety with sulfur, resulting in thioacylated lysine side chains. This modification is recognized class I HDACs different efficiencies ranging from not accepted HDAC1 to kinetic constants similar that parent oxo substrate HDAC8. Class II can hydrolyze substrates approximately 5–10-fold reduced kcat values, which resembles effect thioamide substitution...
Histone-modifying proteins have been identified as promising targets to treat several diseases including cancer and parasitic ailments. In silico methods incorporated within a variety of drug discovery programs facilitate the identification development novel lead compounds. this study, we explore binding modes series benzhydroxamates derivatives developed histone deacetylase inhibitors Schistosoma mansoni (smHDAC) using molecular docking free energy (BFE) calculations. The protocol was able...
Background Echinococcosis and cysticercosis are neglected tropical diseases caused by cestode parasites (family Taeniidae). Not only there is a small number of approved anthelmintics for the treatment these cestodiases, but also some them not highly effective against larval stages, such that identifying novel drug targets their associated compounds critical. Histone deacetylase (HDAC) enzymes validated in cancers other diseases, have been gaining relevance developing new potential...
In addition to involvement in epigenetic gene regulation, histone deacetylases (HDACs) regulate multiple cellular processes through mediating the activity of non-histone protein substrates. The knockdown HDAC8 isozyme is associated with inhibition cell proliferation and apoptosis enhancement several cancer lines. As shown studies, can be considered a potential target treatment forms such as childhood neuroblastoma. present work describes development proteolysis targeting chimeras (PROTACs)...
While histone deacetylases (HDACs) are known as modulators of epigenetic gene regulation, they also control the activity non-histone protein substrates. The isozyme HDAC8 plays a role in inhibiting apoptosis and increasing cancer cell proliferation. As result, is considered potential target treatment forms such T-cell lymphoma, gastric adenocarcinoma, hepatocellular carcinoma, childhood neuroblastoma. present work describes development proteolysis targeting chimera (PROTAC) based on...
Abstract Background Neuroblastoma is the most common solid tumor in infants accounting for approximately 15% of all cancer-related deaths. Over 50% high-risk neuroblastoma relapse, emphasizing need novel drug targets and therapeutic strategies. In neuroblastoma, chromosomal gains at chromosome 17q, including IGF2BP1 , MYCN amplification 2p are associated with adverse outcome. Recent, pre-clinical evidence indicates feasibility direct indirect targeting cancer treatment. Methods Candidate...