3,808 research outputs found

    Antiproliferative properties and g-quadruplex-binding of symmetrical naphtho[1,2-b:8,7-b’]dithiophene derivatives

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    Background: G-quadruplex (G4) forming sequences are recurrent in telomeres and promoter regions of several protooncogenes. In normal cells, the transient arrangements of DNA in G-tetrads may regulate replication, transcription, and translation processes. Tumors are character-ized by uncontrolled cell growth and tissue invasiveness and some of them are possibly mediated by gene expression involving G-quadruplexes. The stabilization of G-quadruplex sequences with small molecules is considered a promising strategy in anticancer targeted therapy. Methods: Molecular virtual screening allowed us identifying novel symmetric bifunctionalized naphtho[1,2-b:8,7-b’]dithiophene ligands as interesting candidates targeting h-Telo and c-MYC G-quadruplexes. A set of unexplored naphtho-dithiophene derivatives has been synthesized and biologically tested through in vitro antiproliferative assays and spectroscopic experiments in solution. Results: The analysis of biological and spectroscopic data highlighted noteworthy cytotoxic effects on HeLa cancer cell line (GI50 in the low μM range), but weak interactions with G-quadruplex c-MYC promoter. Conclusions: The new series of naphtho[1,2-b:8,7-b’]dithiophene derivatives, bearing the pharmacophoric assump-tions necessary to stabilize G-quadruplexes, have been designed and successfully synthesized. The interesting antiproliferative results supported by computer aided rational approaches suggest that these studies are a significant starting point for a lead optimization process and the isolation of a more efficacious set of G-quadruplexes stabilizers

    Morfologia e sedimentologia della spiaggia e della piattaforma continentale interna

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    Ricerche sedimentologiche sono state condotte sui sedimenti recenti ed attuali della piattaforma del Lazio. Tali indagini hanno permesso di determinare la variabilità dei sedimenti nella zona più mobile dei fondali e il loro dinamismo nella zona più prossima alla costa, ove maggiormente si risente l’azione del moto ondoso e delle correnti. In particolare, lo studio delle caratteristiche tessiturali dei sedimenti ha consentito la determinazione della distribuzione del sedimento sui fondali nella fascia compresa tra la battigia e -50 m e la caratterizzazione litosedimentologica dei sedimenti più superficiali del sottofondo marino

    Caratteristiche morfosedimentologiche e tendenza evolutiva del Lago Lungo (Lazio meridionale)

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    Sono state analizzate le caratteristiche morfosedimentologiche del Lago Lungo (Lazio Meridionale) integrate da dati batimetri. Il lago risulta costituito da due bacini la cui soglia di separazione è un delta lacustre generato dagli apporti sedimentari da mare attraverso un canale emissario. Il confronto tra Modelli Digitali del Terreno costruiti attraverso le isobate riferite all’anno 2000 e quelle ricostruite prima dell’apertura del canale emissario, portano a stimare in poco meno di 26.000 mc il volume del deposito deltizio

    Clinical Applications of Genome Anthropology Felice Festa, Monica Macrì

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    Evolution is the only weapon that every living species has to survive to the changes of the surrounding environment. The clinical applications of genome anthropological studies has been studied. The goal is to understand with a global approach how certain body districts have changed during the evolution and how these changes have affected the contemporary man. All these researches investigated populations lived thousands of years ago and Tanaka craniofacial and cervical spine fresh cadaver dissective technic has enabled the creation of a comprehensive diagnostic protocol [1]. One of the most important tool of this diagnostic protocol is the use of all-skull CT cone beam which shows the anatomical structures in a real 3D perspective using a specific software. The use of this test has become a standard because the radiation dose administered is lower than the usual radiographs performed for the orthodontic diagnosis [2]. Among the innovative aspects of this protocol there is the evaluation of anatomical structures by means of cone-beam CT which allow us to create a specific therapy for each patient paying attention to gnathological and postural disorders. Patients are evaluated and monitored during the therapy using a clinical record which include a VAS test. VAS is a validated test and is used by patients to determine the effectiveness of the chosen therapy. References [1] FESTA, F., et al. Maxillary and Mandibular Base Size in Ancient Skulls and of Modern Humans from Opi, Abruzzi, Italy: A Cross-Sectional Study. , 0823 2010 Spring. ISBN 1941-6741; 1530-5678. [2] Feragalli, B., Rampado, O., Abate, C., Macrì, M., Festa, F., Stromei, F., ... & Guglielmi, G. (2017). Cone beam computed tomography for dental and maxillofacial imaging: technique improvement and low-dose protocols. La radiologia medic

    Modele morphodynamique: modele de profil d'equilibre

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    L'érosion des plages et des remèdes par des interventions de nourriture artificiell
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