A5061098272- DNA and Nucleic Acid Chemistry
- Advanced biosensing and bioanalysis techniques
- RNA Interference and Gene Delivery
- Click Chemistry and Applications
- Sirtuins and Resveratrol in Medicine
- Metal complexes synthesis and properties
- SARS-CoV-2 and COVID-19 Research
- RNA regulation and disease
- Viral gastroenteritis research and epidemiology
- RNA and protein synthesis mechanisms
- CRISPR and Genetic Engineering
- Biosensors and Analytical Detection
- PARP inhibition in cancer therapy
- Biochemical Acid Research Studies
- Monoclonal and Polyclonal Antibodies Research
- Ferrocene Chemistry and Applications
- Origins and Evolution of Life
- Cholinesterase and Neurodegenerative Diseases
- Viral Infections and Immunology Research
University of Naples Federico II
2016-2025
Istituto Nazionale di Fisica Nucleare, Sezione di Napoli
2016
In the context of developing efficient anticancer therapies aimed at eradicating any sort tumors, G-quadruplexes represent excellent targets. Small molecules able to interact with can interfere cell pathways specific tumors and common all cancers. Naphthalene diimides (NDIs) are among most promising, putative G-quadruplex-targeting drugs, due their ability simultaneously target multiple strong, selective in vitro vivo activity. Here, available biophysical, biological, structural data...
Aiming to identify highly effective and selective G-quadruplex ligands as anticancer candidates, five natural compounds were investigated here, i.e., the alkaloids Canadine, D-Glaucine Dicentrine, well flavonoids Deguelin Millettone, selected analogs of previously identified promising G-quadruplex-targeting ligands. A preliminary screening with on Controlled Pore Glass assay proved that, among compounds, Dicentrine is most ligand telomeric oncogenic G-quadruplexes, also showing good vs....
In the search for new therapeutic strategies to contrast SARS-CoV-2, we here studied interaction of polydatin (PD) and resveratrol (RESV)-two natural stilbene polyphenols with manifold, well known biological activities-with Spike, viral protein essential virus entry into host cells, ACE2, angiotensin-converting enzyme present on surface multiple cell types (including respiratory epithelial cells) which is main receptor Spike binding. Molecular Docking simulations evidenced that both...
Stilbenoids are natural compounds endowed with several biological activities, including cardioprotection and cancer prevention. Among them, (±)-trans-δ-viniferin, deriving from trans-resveratrol dimerization, was investigated in its ability to target DNA duplex G-quadruplex structures by exploiting NMR spectroscopy, circular dichroism, fluorescence spectroscopy molecular docking. (±)-trans-δ-Viniferin proved bind both the minor major grooves of duplexes, whereas it bound 3'- 5'-ends a...
Contrary to what was believed for many years, cis-PtI2(NH3)2, the diiodido analogue of cisplatin, displays high in vitro antiproliferative activity toward a set tumour cell lines, overcoming resistance cisplatin platinum-resistant cancer line. In context general reappraisal iodinated Pt(ii) derivatives, aiming at more systematic evaluation their chemical and biological profiles, here we report on reactivity cis-PtI2(NH3)2 with selected DNA model systems, single, double strand or G-quadruplex...
Naphthalene diimides showed significant anticancer activity in animal models, with therapeutic potential related to their ability strongly interact G-quadruplexes. Recently, a trifunctionalized naphthalene diimide, named NDI-5, was identified as the best analogue of mini-library novel for its high G-quadruplex binding affinity along marked, selective activity, emerging promising candidate drug vivo studies. Here we used NMR, dynamic light scattering, circular dichroism and fluorescence...
A focused library of newly designed monomeric and dimeric naphthalene diimides (NDIs) was analyzed in its ability to recognize specific G-quadruplex (G4) structures discriminating duplex DNA. The best G4 ligands-according an affinity chromatography-based screening method named G4-CPG-were tested on human cancer healthy cells, inducing DNA damage at telomeres, parallel, showing selective antiproliferative activity HeLa cells with IC50 values the low nanomolar range. CD fluorescence...
In the quest for selective G-quadruplex (G4)-targeting chemotypes, natural compounds have been thus far poorly explored, though representing appealing candidates due to high structural diversity of their scaffolds. this regard, a unique in-house library composed ca. one thousand individual products was investigated. The combination molecular docking-based virtual screening and G4-CPG experimental assay proved be useful quickly effectively identify-out many compounds-five hit binders...
Abstract DNA G‐quadruplexes (G4s) are key structures for the development of targeted anticancer therapies. In this context, ligands selectively interacting with G4s can represent valuable drugs. Aiming at speeding up identification G4‐targeting synthetic or natural compounds, we developed an affinity chromatography‐based assay, named G‐quadruplex on Oligo Affinity Support (G4‐OAS), by synthesizing G4‐forming sequences commercially available polystyrene OAS. Then, due to unspecific binding...
In the optimization process of nucleic acid aptamers, increased affinity and/or activity are generally searched by exploring structural analogues lead compound. many cases, promising results have been obtained dimerization starting aptamer. Here we studied a focused set covalent dimers G-quadruplex (G4) forming anti-Vascular Endothelial Growth Factor (VEGF) V7t1 aptamer with aim identifying derivatives improved properties. design these dimers, connecting linkers different chemical nature,...