19 results on '"Pagano, Alessia"'
Search Results
2. Temporality and consumption in post-modern societies: ontologies, paradoxes
- Author
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Umberto Pagano, Alessia Mangiacasale and Umberto Pagano, Alessia Mangiacasale
- Published
- 2018
3. 1H NMR-based metabolomics study on follicular fluid from patients with Polycystic Ovary Syndrome
- Author
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Iaccarino, Nunzia, Amato, Jussara, Pagano, Bruno, Pagano, Alessia, D'Oriano, Laura, Pelliccia, Sveva, Giustiniano, Mariateresa, Brancaccio, Diego, Merlino, Francesco, Novellino, Ettore, Alviggi, Carlo, Randazzo, Antonio, Iaccarino, Nunzia, Amato, Jussara, Pagano, Bruno, Pagano, Alessia, D'Oriano, Laura, Pelliccia, Sveva, Giustiniano, Mariateresa, Brancaccio, Diego, Merlino, Francesco, Novellino, Ettore, Alviggi, Carlo, and Randazzo, Antonio
- Subjects
Medical Laboratory Technology ,Clinical Biochemistry ,Biochemistry (medical) - Published
- 2018
4. Investigating non-canonical nucleic acid structures and their interaction with potential anticancer drugs
- Author
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Pagano, Alessia
- Abstract
The outstanding structural polymorphism of DNA allows for the formation of non-canonical secondary structures, such as G-quadruplexes (G4s), G-triplexes (G3s) and i-motifs. G4 and i-motif structures are found within important functional genomic regions such as telomeres and gene promoters. In particular, they are localized within the promoter regions of several proto-oncogenes, whose overexpression leads to malignant transformation, where they play a major role in the regulation of transcription. In many cases, the biological consequence of non-canonical secondary structure formation in the promoter element is gene silencing. For this reason, the search for ligands able to bind and stabilize G4s and/or i-motifs is pharmacologically very important to develop new anticancer strategies. In this PhD thesis, a series of studies have been carried out with the aim of investigating these non-canonical nucleic acid structures and their interaction with potential anticancer drugs. Such studies have led to the discovery of new and selective G4 ligands (Chapter 3). Chapter 4 deals with the tandem application of virtual screening along with experimental investigations, that led to discover the first dual G-triplex/G-quadruplex stabilizing compound. In Chapter 5, biophysical techniques have been employed to demonstrate that some well-known G4 ligands are also able to interact with i-motif structure. The last section of this PhD thesis deals with a study conducted in Dr. Vincenzo Abbate’s laboratory at King’s College London (UK). It concerns the design and synthesis of a new class of gallium chelator to be employed in the development of chemically-modified nucleic acid aptamers to be used as theranostics.
- Published
- 2018
5. Common G-Quadruplex Binding Agents Found to Interact With i-Motif-Forming DNA: Unexpected Multi-Target-Directed Compounds
- Author
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Pagano, Alessia, primary, Iaccarino, Nunzia, additional, Abdelhamid, Mahmoud A. S., additional, Brancaccio, Diego, additional, Garzarella, Emanuele U., additional, Di Porzio, Anna, additional, Novellino, Ettore, additional, Waller, Zoë A. E., additional, Pagano, Bruno, additional, Amato, Jussara, additional, and Randazzo, Antonio, additional
- Published
- 2018
- Full Text
- View/download PDF
6. Targeting theBCL2Gene Promoter G-Quadruplex with a New Class of Furopyridazinone-Based Molecules
- Author
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Amato, Jussara, primary, Pagano, Alessia, additional, Capasso, Domenica, additional, Di Gaetano, Sonia, additional, Giustiniano, Mariateresa, additional, Novellino, Ettore, additional, Randazzo, Antonio, additional, and Pagano, Bruno, additional
- Published
- 2018
- Full Text
- View/download PDF
7. Discovery of the first dual G-triplex/G-quadruplex stabilizing compound: a new opportunity in the targeting of G-rich DNA structures?
- Author
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Amato, Jussara, primary, Pagano, Alessia, additional, Cosconati, Sandro, additional, Amendola, Giorgio, additional, Fotticchia, Iolanda, additional, Iaccarino, Nunzia, additional, Marinello, Jessica, additional, De Magis, Alessio, additional, Capranico, Giovanni, additional, Novellino, Ettore, additional, Pagano, Bruno, additional, and Randazzo, Antonio, additional
- Published
- 2017
- Full Text
- View/download PDF
8. Characterization of monovarietal extra virgin olive oils from the province of Béjaïa (Algeria)
- Author
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Laincer, Firdousse, primary, Iaccarino, Nunzia, additional, Amato, Jussara, additional, Pagano, Bruno, additional, Pagano, Alessia, additional, Tenore, Giancarlo, additional, Tamendjari, Abderezak, additional, Rovellini, Pierangela, additional, Venturini, Stefania, additional, Bellan, Giorgio, additional, Ritieni, Alberto, additional, Mannina, Luisa, additional, Novellino, Ettore, additional, and Randazzo, Antonio, additional
- Published
- 2016
- Full Text
- View/download PDF
9. Toward the Development of Specific G-Quadruplex Binders: Synthesis, Biophysical, and Biological Studies of New Hydrazone Derivatives
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Amato, Jussara, primary, Morigi, Rita, additional, Pagano, Bruno, additional, Pagano, Alessia, additional, Ohnmacht, Stephan, additional, De Magis, Alessio, additional, Tiang, Yee-Peng, additional, Capranico, Giovanni, additional, Locatelli, Alessandra, additional, Graziadio, Alessandra, additional, Leoni, Alberto, additional, Rambaldi, Mirella, additional, Novellino, Ettore, additional, Neidle, Stephen, additional, and Randazzo, Antonio, additional
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- 2016
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- View/download PDF
10. Targeting the <italic>BCL2</italic> Gene Promoter G‐Quadruplex with a New Class of Furopyridazinone‐Based Molecules.
- Author
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Amato, Jussara, Pagano, Alessia, Capasso, Domenica, Di Gaetano, Sonia, Giustiniano, Mariateresa, Novellino, Ettore, Randazzo, Antonio, and Pagano, Bruno
- Published
- 2018
- Full Text
- View/download PDF
11. Effetto delle somministrazione dietetica di livelli crescenti di arginina sulle principali caratteristiche qualitative delle carni di pollo
- Author
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Pagano, Alessia, thesis supervisor: Petracci, Massimiliano, Pagano, Alessia, and thesis supervisor: Petracci, Massimiliano
- Abstract
Il presente lavoro di tesi ha avuto lo scopo di valutare l’effetto della somministrazione dietetica di livelli crescenti di arginina, corrispondenti ad un incremento del rapporto arginina:lisina del 10% (T10), 20% (T20) e 30% (T30), sulle principali caratteristiche qualitative e proprietà tecnologiche delle carni di pollo tal quali e sottoposte a trattamento di marinatura. La prova è stata condotta su un totale di 48 muscoli Pectoralis major (12 muscoli/gruppo sperimentale) che, previa rimozione dei depositi adiposi superficiali e del tessuto connettivo eventualmente presenti, sono stati destinati all’analisi delle principali caratteristiche qualitative (pH, colore), delle proprietà tecnologiche (drip loss, cooking loss e marinade uptake) e della tenerezza (sforzo di taglio). I rilievi eseguiti durante la fase di allevamento hanno dimostrato che la somministrazione di livelli crescenti di arginina non comporta una variazione significativa nelle performance di crescita e conseguentemente nel peso alla macellazione degli animali. Analogamente, per quanto concerne i principali parametri di qualità della carne (pH e parametri colorimetrici) e le proprietà tecnologiche non è stata individuata alcuna differenza significativa fra i gruppi sperimentali considerati. Per quanto riguarda l’approfondimento realizzato mediante NMR ad alta risoluzione, è inoltre emerso come la somministrazione dietetica di livelli crescenti di arginina non sia in grado di modificare sostanzialmente la concentrazione in amminoacidi liberi, composti istidinici e molecole coinvolte nel metabolismo energetico che si ritrovano nella carne. Pertanto, saranno condotti ulteriori studi volti ad approfondire le conoscenze in merito al metabolismo dell’arginina nelle specie avicole tenendo inoltre in considerazione la relazione di antagonismo che lega questo amminoacido alla lisina che costituisce un nutriente essenziale nella crescita dei muscoli pettorali del pollo da carne.
12. Effetto delle somministrazione dietetica di livelli crescenti di arginina sulle principali caratteristiche qualitative delle carni di pollo
- Author
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Pagano, Alessia, thesis supervisor: Petracci, Massimiliano, Pagano, Alessia, and thesis supervisor: Petracci, Massimiliano
- Abstract
Il presente lavoro di tesi ha avuto lo scopo di valutare l’effetto della somministrazione dietetica di livelli crescenti di arginina, corrispondenti ad un incremento del rapporto arginina:lisina del 10% (T10), 20% (T20) e 30% (T30), sulle principali caratteristiche qualitative e proprietà tecnologiche delle carni di pollo tal quali e sottoposte a trattamento di marinatura. La prova è stata condotta su un totale di 48 muscoli Pectoralis major (12 muscoli/gruppo sperimentale) che, previa rimozione dei depositi adiposi superficiali e del tessuto connettivo eventualmente presenti, sono stati destinati all’analisi delle principali caratteristiche qualitative (pH, colore), delle proprietà tecnologiche (drip loss, cooking loss e marinade uptake) e della tenerezza (sforzo di taglio). I rilievi eseguiti durante la fase di allevamento hanno dimostrato che la somministrazione di livelli crescenti di arginina non comporta una variazione significativa nelle performance di crescita e conseguentemente nel peso alla macellazione degli animali. Analogamente, per quanto concerne i principali parametri di qualità della carne (pH e parametri colorimetrici) e le proprietà tecnologiche non è stata individuata alcuna differenza significativa fra i gruppi sperimentali considerati. Per quanto riguarda l’approfondimento realizzato mediante NMR ad alta risoluzione, è inoltre emerso come la somministrazione dietetica di livelli crescenti di arginina non sia in grado di modificare sostanzialmente la concentrazione in amminoacidi liberi, composti istidinici e molecole coinvolte nel metabolismo energetico che si ritrovano nella carne. Pertanto, saranno condotti ulteriori studi volti ad approfondire le conoscenze in merito al metabolismo dell’arginina nelle specie avicole tenendo inoltre in considerazione la relazione di antagonismo che lega questo amminoacido alla lisina che costituisce un nutriente essenziale nella crescita dei muscoli pettorali del pollo da carne.
13. Tailoring a lead-like compound targeting multiple G-quadruplex structures
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Pasquale Zizza, Bruno Pagano, Ettore Novellino, Daniela Montesarchio, Annamaria Biroccio, Sandro Cosconati, Jussara Amato, Antonio Randazzo, Domenica Musumeci, Sara Iachettini, Chiara Platella, Alessia Pagano, Amato, Jussara, Platella, Chiara, Iachettini, Sara, Zizza, Pasquale, Musumeci, Domenica, Cosconati, Sandro, Pagano, Alessia, Novellino, Ettore, Biroccio, Annamaria, Randazzo, Antonio, Pagano, Bruno, and Montesarchio, Daniela
- Subjects
Biophysical characterization ,DNA damage ,Stereochemistry ,Pharmaceutical Science ,Affinity chromatography-based screening ,Ligands ,G-quadruplex ,01 natural sciences ,Chromatography, Affinity ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,Affinity chromatography ,In vitro biological assay ,Oxazines ,Drug Discovery ,Humans ,Molecule ,Cell Proliferation ,030304 developmental biology ,Pharmacology ,0303 health sciences ,Binding Sites ,010405 organic chemistry ,Ligand ,Chemistry ,Organic Chemistry ,General Medicine ,Naphthoquinone ,0104 chemical sciences ,G-Quadruplexes ,Duplex (building) ,Drug Design ,Molecular docking ,G-quadruplex ligand ,Selectivity ,DNA Damage ,Naphthoquinones ,Protein Binding - Abstract
A focused library of analogs of a lead-like G-quadruplex (G4) targeting compound (4), sharing a furobenzoxazine naphthoquinone core and differing for the pendant groups on the N-atom of the oxazine ring, has been here analyzed with the aim of developing more potent and selective ligands. These molecules have been tested vs. topologically different G4s by the G4-CPG assay, an affinity chromatography-based method for screening putative G4 ligands. The obtained results showed that all these compounds were able to bind several G4 structures, both telomeric and extra-telomeric, thus behaving as multi-target ligands, and two of them fully discriminated G4 vs. duplex DNA. Biological assays proved that almost all the compounds produced effective DNA damage, showing marked antiproliferative effects on tumor cells in the low μM range. Combined analysis of the G4-CPG binding assays and biological data led us to focus on compound S4-5, proved to be less cytotoxic than the parent compound 4 on normal cells. An in-depth biophysical characterization of the binding of S4-5 to different G4s showed that the here identified ligand has higher affinity for the G4s and higher ability to discriminate G4 vs. duplex DNA than 4. Molecular docking studies, in agreement with the NMR data, suggest that S4-5 interacts with the accessible grooves of the target G4 structures, giving clues for its increased G4 vs. duplex selectivity. A focused library of analogs of a lead-like G-quadruplex (G4) targeting compound (4), sharing a furobenzoxazine naphthoquinone core and differing for the pendant groups on the N-atom of the oxazine ring, has been here analyzed with the aim of developing more potent and selective ligands. These molecules have been tested vs. topologically different G4s by the G4-CPG assay, an affinity chromatography-based method for screening putative G4 ligands. The obtained results showed that all these compounds were able to bind several G4 structures, both telomeric and extra-telomeric, thus behaving as multi-target ligands, and two of them fully discriminated G4 vs. duplex DNA. Biological assays proved that almost all the compounds produced effective DNA damage, showing marked antiproliferative effects on tumor cells in the low μM range. Combined analysis of the G4-CPG binding assays and biological data led us to focus on compound S4-5, proved to be less cytotoxic than the parent compound 4 on normal cells. An in-depth biophysical characterization of the binding of S4-5 to different G4s showed that the here identified ligand has higher affinity for the G4s and higher ability to discriminate G4 vs. duplex DNA than 4. Molecular docking studies, in agreement with the NMR data, suggest that S4-5 interacts with the accessible grooves of the target G4 structures, giving clues for its increased G4 vs. duplex selectivity.
- Published
- 2019
14. Toward the Development of Specific G-Quadruplex Binders: Synthesis, Biophysical, and Biological Studies of New Hydrazone Derivatives
- Author
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Alberto Leoni, Stephen Neidle, Stephan A. Ohnmacht, Alessio De Magis, Yee-Peng Tiang, Jussara Amato, Rita Morigi, Antonio Randazzo, Alessandra Locatelli, Mirella Rambaldi, Ettore Novellino, Giovanni Capranico, Alessandra Graziadio, Bruno Pagano, Alessia Pagano, Amato, Jussara, Morigi, Rita, Pagano, Bruno, Pagano, Alessia, Ohnmacht, Stephan, De Magis, Alessio, Tiang, Yee Peng, Capranico, Giovanni, Locatelli, Alessandra, Graziadio, Alessandra, Leoni, Alberto, Rambaldi, Mirella, Novellino, Ettore, Neidle, Stephen, Randazzo, Antonio, De Magis Alessio, and Tiang, Yee-Peng
- Subjects
Circular dichroism ,Hydrazone ,Ligand ,010402 general chemistry ,G-quadruplex ,01 natural sciences ,Structure-Activity Relationship ,Drug Discovery ,Tumor Cells, Cultured ,Telomeric DNA ,Humans ,Cytotoxic T cell ,heterocyclic compounds ,Cell Proliferation ,chemistry.chemical_classification ,Dose-Response Relationship, Drug ,Molecular Structure ,Oncogene ,010405 organic chemistry ,Chemistry ,Hydrazones ,DNA ,Combinatorial chemistry ,In vitro ,0104 chemical sciences ,G-Quadruplexes ,Molecular Docking Simulation ,Folding (chemistry) ,Anticancer ,Cancer cell ,Molecular Medicine ,Oncogene promoters ,DNA, Drug Discovery, G-quadruplex, Anticancer compounds, Telomeric DNA, Hydrazone derivative, Osteosarcoma cells - Abstract
G-Quadruplex-binding compounds are currently perceived as possible anticancer therapeutics. Here, starting from a promising lead, a small series of novel hydrazone-based compounds were synthesized and evaluated as G-quadruplex binders. The in vitro G-quadruplex-binding properties of the synthesized compounds were investigated employing both human telomeric and oncogene promoter G-quadruplexes with different folding topologies as targets. The present investigation led to the identification of potent G-quadruplex stabilizers with high selectivity over duplex DNA and preference for one G-quadruplex topology over others. Among them, selected derivatives have been shown to trap G-quadruplex structures in the nucleus of cancer cells. Interestingly, this behavior correlates with efficient cytotoxic activity in human osteosarcoma and colon carcinoma cells.
- Published
- 2016
15. Common G-Quadruplex Binding Agents Found to Interact With i-Motif-Forming DNA: Unexpected Multi-Target-Directed Compounds
- Author
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Alessia Pagano, Nunzia Iaccarino, Mahmoud A. S. Abdelhamid, Diego Brancaccio, Emanuele U. Garzarella, Anna Di Porzio, Ettore Novellino, Zoë A. E. Waller, Bruno Pagano, Jussara Amato, Antonio Randazzo, Pagano, Alessia, Iaccarino, Nunzia, Abdelhamid, Mahmoud A. S., Brancaccio, Diego, Garzarella, Emanuele U., Di Porzio, Anna, Novellino, Ettore, Waller, Zoë A. E., Pagano, Bruno, Amato, Jussara, and Randazzo, Antonio
- Subjects
0301 basic medicine ,Berberine ,Phen-DC3 ,Computational biology ,010402 general chemistry ,G-quadruplex ,01 natural sciences ,lcsh:Chemistry ,03 medical and health sciences ,chemistry.chemical_compound ,Multi target ,BRACO-19 ,Original Research ,G quadruplex binding ,RHPS4 ,Pyridostatin ,Chemistry (all) ,General Chemistry ,Anticancer drug ,In vitro ,0104 chemical sciences ,Chemistry ,030104 developmental biology ,lcsh:QD1-999 ,chemistry ,I-motif ,Nucleic acid ,Motif (music) ,Mitoxantrone ,DNA - Abstract
G-quadruplex (G4) and i-motif (iM) are four-stranded non-canonical nucleic acid structural arrangements. Recent evidences suggest that these DNA structures exist in living cells and could be involved in several cancer-related processes, thus representing an attractive target for anticancer drug discovery. Efforts toward the development of G4 targeting compounds have led to a number of effective bioactive ligands. Herein, employing several biophysical methodologies, we studied the ability of some well-known G4 ligands to interact with iM-forming DNA. The data showed that the investigated compounds are actually able to interact with both DNA in vitro, thus acting de facto as multi-target-directed agents. Interestingly, while all the compounds stabilize the G4, some of them significantly reduce the stability of the iM. The present study highlights the importance, when studying G4-targeting compounds, of evaluating also their behavior toward the i-motif counterpart.
- Published
- 2018
16. Targeting the BCL2 Gene Promoter G-Quadruplex with a New Class of Furopyridazinone-Based Molecules
- Author
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Domenica Capasso, Mariateresa Giustiniano, Bruno Pagano, Alessia Pagano, Antonio Randazzo, Jussara Amato, Sonia Di Gaetano, Ettore Novellino, Amato, Jussara, Pagano, Alessia, Capasso, Domenica, Digaetano, Sonia, Giustiniano, Mariateresa, Novellino, Ettore, Randazzo, Antonio, and Pagano, Bruno
- Subjects
0301 basic medicine ,Models, Molecular ,G-quadruplexes ,antitumor agents ,Ligand ,G-quadruplex ,Biochemistry ,Jurkat cells ,03 medical and health sciences ,chemistry.chemical_compound ,Structure-Activity Relationship ,hemic and lymphatic diseases ,Drug Discovery ,Humans ,heterocyclic compounds ,General Pharmacology, Toxicology and Pharmaceutics ,Cytotoxicity ,Promoter Regions, Genetic ,G-quadruplexe ,Pharmacology ,Bcl-2 transcriptional down-regulation ,Dose-Response Relationship, Drug ,Molecular Structure ,ligands ,gene promoters ,Organic Chemistry ,Antitumor agent ,Promoter ,G-Quadruplexes ,Pyridazines ,030104 developmental biology ,chemistry ,Proto-Oncogene Proteins c-bcl-2 ,Cell culture ,Gene promoter ,Pharmacology, Toxicology and Pharmaceutics (all) ,Molecular Medicine ,Selectivity ,DNA - Abstract
Targeting of G-quadruplex-forming DNA in the BCL2 gene promoter to inhibit the expression of anti-apoptotic Bcl-2 protein is an attractive approach to cancer treatment. So far, efforts made in the discovery of molecules that are able to target the BCL2 G-quadruplex have succeeded mainly in the identification of ligands with poor drug-like properties. Here, a small series of furo[2,3-d]pyridazin-4(5H)-one derivatives were evaluated as a new class of drug-like G-quadruplex-targeting compounds. Biophysical studies showed that two derivatives could effectively bind to BCL2 G-quadruplex with good selectivity. Moreover, one such ligand was found to appreciably inhibit BCL2 gene transcription, with a substantial decrease in protein expression levels, and also showed significant cytotoxicity toward the Jurkat human T-lymphoblastoid cell line.
- Published
- 2017
17. Discovery of the first dual G-triplex/G-quadruplex stabilizing compound: a new opportunity in the targeting of G-rich DNA structures?
- Author
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Jessica Marinello, Alessio De Magis, Giorgio Amendola, Giovanni Capranico, Bruno Pagano, Jussara Amato, Ettore Novellino, Alessia Pagano, Sandro Cosconati, Nunzia Iaccarino, Antonio Randazzo, Iolanda Fotticchia, Amato, Jussara, Pagano, Alessia, Cosconati, Sandro, Amendola, Giorgio, Fotticchia, Iolanda, Iaccarino, Nunzia, Marinello, Jessica, De Magis, Alessio, Capranico, Giovanni, Novellino, Ettore, Pagano, Bruno, and Randazzo, Antonio
- Subjects
0301 basic medicine ,Magnetic Resonance Spectroscopy ,Time Factors ,Molecular model ,Biophysics ,Antineoplastic Agents ,Ligand ,Ligands ,G-quadruplex ,Antiparallel (biochemistry) ,Biochemistry ,Inhibitory Concentration 50 ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,Cell Line, Tumor ,Humans ,Structure–activity relationship ,Binding site ,Molecular Biology ,Cell Proliferation ,Osteosarcoma ,Virtual screening ,Binding Sites ,Calorimetry, Differential Scanning ,Dose-Response Relationship, Drug ,Guanosine ,Drug discovery ,Circular Dichroism ,DNA, Neoplasm ,Combinatorial chemistry ,G-Quadruplexes ,Molecular Docking Simulation ,Native Polyacrylamide Gel Electrophoresis ,G-triplex ,030104 developmental biology ,Anticancer agent ,chemistry ,Drug Design ,Anticancer agents ,G-triplex, G-quadruplex, Ligand, Anticancer agents, Drug discovery, DNA, Virtual screening, Spectroscopy, Noncanonical DNA structures, Thermostability ,DNA - Abstract
Background Guanine-rich DNA motifs can form non-canonical structures known as G-quadruplexes, whose role in tumorigenic processes makes them attractive drug-target candidates for cancer therapy. Recent studies revealed that the folding and unfolding pathways of G-quadruplexes proceed through a quite stable intermediate named G-triplex. Methods Virtual screening was employed to identify a small set of putative G-triplex ligands. The G-triplex stabilizing properties of these compounds were analyzed by CD melting assay. DSC, non-denaturing gel electrophoresis, NMR and molecular modeling studies were performed to investigate the interaction between the selected compound 1 and G-rich DNA structures. Cytotoxic activity of 1 was evaluated by MTT cell proliferation assay. Results The experiments led to the identification of a promising hit that was shown to bind preferentially to G-triplex and parallel-stranded G-quadruplexes over duplex and antiparallel G-quadruplexes. Molecular modeling results suggested a partial end-stacking of 1 to the external G-triad/G-tetrads as a binding mode. Biological assays showed that 1 is endowed with cytotoxic effect on human osteosarcoma cells. Conclusions A tandem application of virtual screening along with the experimental investigation was employed to discover a G-triplex-targeting ligand. Experiments revealed that the selected compound actually acts as a dual G-triplex/G-quadruplex stabilizer, thus stimulating further studies aimed at its optimization. General significance The discovery of molecules able to bind and stabilize G-triplex structures is highly appealing, but their transient state makes challenging their recognition. These findings suggest that the identification of ligands with dual G-triplex/G-quadruplex stabilizing properties may represent a new route for the design of anticancer agents targeting the G-rich DNA structures. This article is part of a Special Issue entitled "G-quadruplex" Guest Editor: Dr. Concetta Giancola and Dr. Daniela Montesarchio.
- Published
- 2017
18. Characterization of monovarietal extra virgin olive oils from the province of Béjaïa (Algeria)
- Author
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Ettore Novellino, Abderezak Tamendjari, Nunzia Iaccarino, Alberto Ritieni, Jussara Amato, Gian Carlo Tenore, Stefania Venturini, Firdousse Laincer, P. Rovellini, Bruno Pagano, Antonio Randazzo, Alessia Pagano, Giorgio Bellan, Luisa Mannina, Laincer, Firdousse, Iaccarino, Nunzia, Amato, Jussara, Pagano, Bruno, Pagano, Alessia, Tenore, GIAN CARLO, Tamendjari, Abderezak, Rovellini, Pierangela, Venturini, Stefania, Bellan, Giorgio, Ritieni, Alberto, Mannina, Luisa, Novellino, Ettore, and Randazzo, Antonio
- Subjects
Béjaïa ,Statistical analysi ,01 natural sciences ,chemistry.chemical_compound ,0404 agricultural biotechnology ,statistical analysis ,Food science ,Tocopherol ,Carotenoid ,chemistry.chemical_classification ,Olive oil quality ,Content determination ,010401 analytical chemistry ,04 agricultural and veterinary sciences ,olive oils ,NMR ,Algeria ,040401 food science ,Terpenoid ,0104 chemical sciences ,Oleic acid ,chemistry ,Composition (visual arts) ,Food quality ,Olive oil ,Food Science - Abstract
Olive fruits from 19 varieties and different areas of Bejaia province (Algeria) were used to produce monovarietal olive oils in laboratory. The olive oils were analyzed using both traditional chemical analyses and nuclear magnetic resonance (NMR) methodology. The investigation involved pigment content determination, tocopherol analysis, fatty acid composition, and chromatographic determination of phenolic compounds. Chlorophyll, carotenoids, tocopherols and the content of oleic acid turned out to be variety dependent. The extra-virgin olive oils (EVOOs) were analyzed as a whole and as phenolic extract by NMR. The study gave general indication on olive oil quality and information about geographical origin of the samples. Overall, the results obtained in the present work reveal that Algerian monovarietal olive oils produced in Bejaia province have the potential to produce blends that may compete with other Mediterranean products.
- Published
- 2016
19. Targeting the BCL2 Gene Promoter G-Quadruplex with a New Class of Furopyridazinone-Based Molecules.
- Author
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Amato J, Pagano A, Capasso D, Di Gaetano S, Giustiniano M, Novellino E, Randazzo A, and Pagano B
- Subjects
- Dose-Response Relationship, Drug, Humans, Models, Molecular, Molecular Structure, Pyridazines chemistry, Structure-Activity Relationship, G-Quadruplexes drug effects, Promoter Regions, Genetic genetics, Proto-Oncogene Proteins c-bcl-2 antagonists & inhibitors, Pyridazines pharmacology
- Abstract
Targeting of G-quadruplex-forming DNA in the BCL2 gene promoter to inhibit the expression of anti-apoptotic Bcl-2 protein is an attractive approach to cancer treatment. So far, efforts made in the discovery of molecules that are able to target the BCL2 G-quadruplex have succeeded mainly in the identification of ligands with poor drug-like properties. Here, a small series of furo[2,3-d]pyridazin-4(5H)-one derivatives were evaluated as a new class of drug-like G-quadruplex-targeting compounds. Biophysical studies showed that two derivatives could effectively bind to BCL2 G-quadruplex with good selectivity. Moreover, one such ligand was found to appreciably inhibit BCL2 gene transcription, with a substantial decrease in protein expression levels, and also showed significant cytotoxicity toward the Jurkat human T-lymphoblastoid cell line., (© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2018
- Full Text
- View/download PDF
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