A5031650006- Epigenetics and DNA Methylation
- Histone Deacetylase Inhibitors Research
- Cancer-related gene regulation
- CRISPR and Genetic Engineering
- Peptidase Inhibition and Analysis
- Pluripotent Stem Cells Research
- Genomics and Chromatin Dynamics
- Protein Degradation and Inhibitors
- RNA modifications and cancer
- Genetics and Neurodevelopmental Disorders
- Diet and metabolism studies
- RNA Interference and Gene Delivery
- Phosphodiesterase function and regulation
- Cholinesterase and Neurodegenerative Diseases
- Sirtuins and Resveratrol in Medicine
- Signaling Pathways in Disease
- Autophagy in Disease and Therapy
- Multiple Myeloma Research and Treatments
- Cancer Immunotherapy and Biomarkers
- Stalking, Cyberstalking, and Harassment
- Microbial Natural Products and Biosynthesis
- Corruption and Economic Development
- Chemical Synthesis and Analysis
- Medical and Biological Ozone Research
- T-cell and Retrovirus Studies
University Medical Center Groningen
2022-2025
University of Groningen
2022-2025
University of Campania "Luigi Vanvitelli"
2017-2024
University of Naples Federico II
2016-2018
Institute of Genetics and Biophysics
2018
Università Cattolica del Sacro Cuore
2013-2015
Joint Research Centre
2013
University of Trento
2013
Vitis vinifera represents an important and renowned source of compounds with significant biological activity. Wines winery bioproducts, such as grape pomace, skins, seeds, are rich in bioactive against a wide range human pathogens, including bacteria, fungi, viruses. However, little is known about the properties vine leaves. The aim this study was evaluation phenolic composition antiviral activity leaf extract two viruses: Herpes simplex virus type 1 (HSV-1) pandemic currently widespread...
Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities confirmed our immunohistochemistry studies on HDAC6 overexpression in tissues. We herein developed series of novel hHDAC6 inhibitors, having low inhibitory potency over hHDAC1 and hHDAC8, as potential pharmacological tools for treatment. Their was combined vitro vivo toxicity. Structural analysis 6h structure–activity...
Several evidence pointed out the role of epigenetics in Alzheimer's disease (AD) revealing strictly relationships between epigenetic and "classical" AD targets. Based on reported connection among histone deacetylases (HDACs) glycogen synthase kinase 3β (GSK-3β), herein we present discovery biochemical characterization first-in-class hit compound able to exert promising anti-AD effects by modulating targeted proteins low micromolar range concentration. Compound 11 induces an increase...
Abstract Background DNA methyltransferases (DNMTs) are epigenetic enzymes involved in embryonic development, cell differentiation, epithelial to mesenchymal transition, and control of gene expression, whose overexpression or enhanced catalytic activity has been widely reported cancer initiation progression. To date, two DNMT inhibitors (DNMTi), 5-azacytidine (5-AZA) 5-aza-2′-deoxycytidine (DAC), approved for the treatment myelodysplastic syndromes acute myeloid leukemia. Nevertheless, they...
Epigenetic modifications are functionally involved in gene expression regulation. In particular, histone posttranslational play a crucial role functional chromatin organization. Several drugs able to inhibit or stimulate some families of proteins epigenetic regulation have been found, number which FDA-approved for the treatment cutaneous T-cell lymphoma phase I/II/III clinical trials solid tumors. Although protein families, such as deacetylases and their inhibitors, well characterized, our...
Histone deacetylase inhibitors (HDACi) have emerged as promising therapeutics for the treatment of neurodegeneration, cancer, and rare disorders. Herein, we report development a series spiroindoline-based HDAC6 isoform-selective based on X-ray crystal studies hit 6a. We identified compound 6j most potent selective hHDAC6 inhibitor series. Biological investigation compounds 6b, 6h, demonstrated their antiproliferative activity against several cancer cell lines. Western blotting indicated that...
SIRT1, a NAD+-dependent deacetylase, is the most well-studied member of class III histone deacetylases. Due to its wide range activities and substrate targets, this enzyme has emerged as major regulator different physiological processes. However, SIRT1-mediated alterations are also implicated in pathogenesis several conditions, including metabolic neurodegenerative disorders, cancer. Current evidence highlights potential role SIRT1 an attractive therapeutic target for disease prevention...
Abstract The impact of multi-drug resistant bacterial strains on human health is reaching worrisome levels. Over 2 million people are infected by bacteria, and more than 700,000 die each year because the continuous spread strains. development new antibiotics prudent use existing ones to prolong their lifespan require a constant effort drug industries healthcare workers. re-purposing drugs for as antimicrobial agents would streamline antibacterial strategies. As part this effort, we screened...
Aberrant epigenetic modifications are involved in cancer development. Jumonji C domain-containing histone lysine demethylases (KDMs) found mainly up-regulated breast, prostate, and colon cancer. Currently, growing interest is focusing on the identification development of new inhibitors able to block activity KDMs thus reduce tumor progression. KDM4A known play a role several cellular physiological processes, was recently overexpressed number pathological states, including In this work,...
The 7th International Conference on Epigenetics & Bioengineering held in Amsterdam, Netherlands was a successful event covering cutting-edge research utilizing innovative technologies from multidisciplinary international scientists the fields of epigenetics and bioengineering, with an emphasis development disease. This conference report highlights outstanding presented engaging discussions that took place. Throughout sessions, leading experts demonstrated novel to explore epigenetic...
Some species of clover are reported to have beneficial effects in human diseases. However, little is known about the activity forage plant Trifolium repens, or white clover, which has been recently found exert a hepatoprotective action. Scientific interest increasingly focused on identifying new drugs, especially natural products and their derivatives, treat diseases including cancer. We analyzed anticancer T. repens several cancer cell lines. The phytochemical components were first...
Effect of the ozonated oil in liposomes: they act against Staphylococcus aureus and Pseudomonas aeruginosa is among most frequent eye pathogens causes acute chronic infections ocular surface. were tested this study. The bacterial suspension was diluted to obtain 150 CFU/ml. 15 Various volumes liposome-vehiculated added (400 μl, 200 100 μl 50 μl) suspension; both are incubated at 37?C for 10 minutes. cytotoxicity analysed University Campania "Luigi Vanvitelli", Department Precision Medicine....
The involvement of sirtuins (SIRTs) in modulating metabolic and stress response pathways is attracting growing scientific interest. Some SIRT family members are located mitochondria, dynamic organelles that perform several crucial functions essential for eukaryotic life. Mitochondrial dysfunction has emerged as having a key role number human diseases, including cancer. Here, we investigated mitochondrial damage resulting from treatment with recently characterized pan-SIRT inhibitor, MC2494....
Abstract In recent years there has been a clear consensus that neurodegenerative conditions can be better treated through concurrent modulation of different targets. Herein we report combined inhibition transglutaminase 2 (TG2) and histone deacetylases (HDACs) synergistically protects against toxic stimuli mediated by glutamate. Based on these findings, designed synthesized series novel dual TG2–HDAC binding agents. Compound 3 [( E )‐ N...
Abstract The natural product tripartin has been reported to inhibit the N ‐methyl‐lysine histone demethylase KDM4A. A synthesis of starting from 3,5‐dimethoxyphenylacrylic acid was developed, and enantiomers were separated by chiral HPLC. We observed that both manifested an apparent increase in H3K9me3 levels when dosed cells, as measured western blot analysis. Thus, there is no enantiomeric discrimination toward this terms its effects on cellular methylation status. Interestingly, did not...
Despite the discovery and development of novel therapies, cancer is still a leading cause death worldwide. In order to grow, tumor cells require large quantities nutrients involved in metabolic processes, an increase iron levels known contribute proliferation. Iron plays important role active site number proteins energy metabolism, DNA synthesis repair, such as ribonucleotide reductase, which induce G0/S phase arrest exert marked antineoplastic effect, particularly leukemia neuroblastoma....