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Your search keyword '"Elisabetta Barresi"' showing total 3 results
Start Over Author "Elisabetta Barresi" Publisher american chemical society (acs)
3 results on '"Elisabetta Barresi"'

1. Targeting TSPO Reduces Inflammation and Apoptosis in an In Vitro Photoreceptor-Like Model of Retinal Degeneration

Author

Francesca Corsi, Emma Baglini, Elisabetta Barresi, Silvia Salerno, Chiara Cerri, Claudia Martini, Federico Da Settimo Passetti, Sabrina Taliani, Claudia Gargini, and Ilaria Piano

Subjects
Lipopolysaccharides, Inflammation, Physiology, Cognitive Neuroscience, Retinal Degeneration, Neurodegenerative Diseases, Apoptosis, Cell Biology, General Medicine, Ligands, Biochemistry, Receptors, GABA, Humans, Carrier Proteins
Abstract

The 18 kDa translocator protein (TSPO) is predominantly located in the mitochondrial outer membrane, playing an important role in steroidogenesis, inflammation, survival, and cell proliferation. Its expression in the CNS, and mainly in glial cells, is upregulated in neuropathologies and brain injury. In this study, the potential of targeting TSPO for the therapeutic treatment of inflammatory-based retinal neurodegeneration was evaluated by means of an in vitro model of lipopolysaccharide (LPS)-induced degeneration in 661 W cells, a photoreceptor-like cell line. After the assessment of the expression of TSPO in 661W cells, which, to the best of our knowledge, was never investigated so far, the anti-inflammatory and cytoprotective effects of a number of known TSPO ligands, belonging to the class of

Published
2022

2. 4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors

Author

Federico Da Settimo, Ciro Milite, Silvia Salerno, Anna Maria Marini, Claudiu T. Supuran, Sandro Cosconati, Ettore Novellino, Giorgio Amendola, Sabrina Taliani, Emanuela Berrino, Elisabetta Barresi, Salerno, Silvia, Barresi, Elisabetta, Amendola, Giorgio, Berrino, Emanuela, Milite, Ciro, Marini, Anna Maria, Da Settimo, Federico, Novellino, Ettore, Supuran, Claudiu T, Cosconati, Sandro, and Taliani, Sabrina

Subjects
Models, Molecular, 0301 basic medicine, Gene isoform, 2-DIMETHYLAMINOMETHYLENE-1, Stereochemistry, Carbonic anhydrase II, Pharmaceutical Science, 3-DIONES, Carbonic Anhydrase II, 01 natural sciences, Isozyme, X-RAY CRYSTALLOGRAPHY, IX, DERIVATIVES, 2-DIMETHYLAMINOMETHYLENE-1,3-DIONES, DINUCLEOPHILES, SYSTEM, 03 medical and health sciences, Catalytic Domain, Drug Discovery, Functional selectivity, Humans, Moiety, Carbonic Anhydrase IX, Carbonic Anhydrase Inhibitors, chemistry.chemical_classification, Sulfonamides, 010405 organic chemistry, Drug discovery, Drug Discovery3003 Pharmaceutical Science, 0104 chemical sciences, Isoenzymes, 030104 developmental biology, chemistry, Drug Design, Molecular Medicine, Selectivity, Tricyclic
Abstract

As a part of our efforts to expand chemical diversity in the carbonic anhydrases inhibitors (CAIs), three small series of polyheterocyclic compounds (4-6) featuring the primary benzenesulfonamide moiety linked to bi/tricyclic scaffolds were investigated. Highly effective inhibitors against the target tumor-associated hCA IX (low nanomolar/ subnanomolar potency levels) showing significant functional selectivity profile toward hCA I, II, and IV isozymes were identified. Molecular docking studies clarified the reasons behind the activity and selectivity of the new compounds.

Published
2018

3. Iminothioethers as Hydrogen Sulfide Donors: From the Gasotransmitter Release to the Vascular Effects

Author

Eugenia Piragine, Valentina Citi, Federico Da Settimo, Maria Cristina Breschi, Claudia Gargini, Lara Testai, Giulia Nesi, Vincenzo Calderone, Elisabetta Barresi, Ilaria Piano, Alma Martelli, Simona Rapposelli, and Sabrina Taliani

Subjects
Male, 0301 basic medicine, Vasodilator Agents, Hydrogen sulfide, Animals, Aorta, Blood Pressure, Cell Line, Drug Discovery, Gasotransmitters, Humans, Hydrogen Sulfide, Imines, Myocytes, Smooth Muscle, Rats, Rats, Wistar, Sulfides, Molecular Medicine, Drug Discovery3003 Pharmaceutical Science, Wistar, Cardiovascular homeostasis, Pharmacology, 01 natural sciences, 03 medical and health sciences, chemistry.chemical_compound, Smooth muscle, Smooth Muscle, medicine.artery, medicine, Myocytes, 010405 organic chemistry, Drug discovery, equipment and supplies, 0104 chemical sciences, 030104 developmental biology, chemistry, Cell culture, Intracellular
Abstract

The gasotransmitter hydrogen sulfide (H2S) is an important tuner of the cardiovascular homeostasis, and its deficiency is etiologically associated with a number of cardiovascular diseases. Therefore, the research of original moieties able to release H2S represents a timely issue for drug discovery. In this work, we developed a collection of iminothioethers (ITEs), exhibiting H2S-releasing properties and producing vasorelaxing effects on rat aortic rings. Derivatives 4 and 11, selected as representative of slow and fast rate H2S donors, respectively, produced a complete recovery of the basal coronary flow, reverting the AngII-induced effects in isolated rat hearts. In addition, studies on human aortic smooth muscle cells (HASMCs) demonstrated membrane hyperpolarizing effects, well related to the intracellular generation of H2S. Taken together, the results obtained support ITEs 4 and 11 as new pharmacological tools, as well as effective and innovative H2S donors for cardiovascular drug discovery.

Published
2017

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