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Author Daniele Tedesco

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Harnessing the Role of HDAC6 in Idiopathic Pulmonary Fibrosis: Design, Synthesis, Structural Analysis, and Biological Evaluation of Potent Inhibitors.

Giuseppe Campiani, Caterina Cavella, Jeremy D Osko, Margherita Brindisi, Nicola Relitti, Simone Brogi, A Prasanth Saraswati, Stefano Federico, Giulia Chemi, Samuele Maramai, Gabriele Carullo, Benedikt Jaeger, Alfonso Carleo, Rosaria Benedetti, Federica Sarno, Stefania Lamponi, Paola Rottoli, Elena Bargagli, Carlo Bertucci, Daniele Tedesco, Daniel Herp, Johanna Senger, Giovina Ruberti, Fulvio Saccoccia, Simona Saponara, Beatrice Gorelli, Massimo Valoti, Breándan Kennedy, Husvinee Sundaramurthi, Stefania Butini, Manfred Jung, Katy M Roach, Lucia Altucci, Peter Bradding, David W Christianson, Sandra Gemma, Antje Prasse,

Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities confirmed by our immunohistochemistry studies on HDAC6 overexpression in IPF lung tissues. We herein developed a series of novel <i>h</i>HDAC6 inhibitors, having low inhibitory potency over <i>h</i>HDAC1 and ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2021, 64(14):9960-9988]

Cited: 1 time

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Keratin nanoparticles and photodynamic therapy enhance the anticancer stem cells activity of salinomycin.

Greta Avancini, Andrea Guerrini, Claudia Ferroni, Daniele Tedesco, Marco Ballestri, Marta Columbaro, Luca Menilli, Elena Reddi, Roberto Costa, Luigi Leanza, Greta Varchi, Francesca Moret,

The high rates of aggressiveness, drug resistance and relapse of breast cancer (BC) are mainly attributed to the inability of conventional therapies to equally eradicate bulk differentiated cells and cancer stem cells (CSCs). To improve the effectiveness of BC treatments, we report the in-water synthesis of novel keratin-based nanoformulations, loaded ... Read more >>

Mater Sci Eng C Mater Biol Appl (Materials science & engineering. C, Materials for biological applications)
[2021, 122:111899]

Cited: 2 times

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Structural and functional insights into nitrosoglutathione reductase from Chlamydomonas reinhardtii.

Andrea Tagliani, Jacopo Rossi, Christophe H Marchand, Marcello De Mia, Daniele Tedesco, Libero Gurrieri, Maria Meloni, Giuseppe Falini, Paolo Trost, Stéphane D Lemaire, Simona Fermani, Mirko Zaffagnini,

Protein S-nitrosylation plays a fundamental role in cell signaling and nitrosoglutathione (GSNO) is considered as the main nitrosylating signaling molecule. Enzymatic systems controlling GSNO homeostasis are thus crucial to indirectly control the formation of protein S-nitrosothiols. GSNO reductase (GSNOR) is the key enzyme controlling GSNO levels by catalyzing its degradation ... Read more >>

Redox Biol (Redox biology)
[2021, 38:101806]

Cited: 1 time

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Structural and functional insights into nitrosoglutathione reductase from Chlamydomonas reinhardtii

Andrea Tagliani, Jacopo Rossi, Christophe Marchand, Marcello De Mia, Daniele Tedesco, Gurrieri Libero, Maria Meloni, Giuseppe Falini, Paolo Trost, Stéphane Lemaire, Simona Fermani, Mirko Zaffagnini,

<h4>ABSTRACT</h4> Protein S-nitrosylation plays a fundamental role in cell signaling and nitrosoglutathione (GSNO) is considered as the main nitrosylating signaling molecule. Enzymatic systems controlling GSNO homeostasis are thus crucial to indirectly control the formation of protein S-nitrosothiols. GSNO reductase (GSNOR) is the key enzyme controlling GSNO levels by catalyzing its ... Read more >>

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No G-Quadruplex Structures in the DNA of Parvovirus B19: Experimental Evidence versus Bioinformatic Predictions.

Gloria Bua, Daniele Tedesco, Ilaria Conti, Alessandro Reggiani, Manuela Bartolini, Giorgio Gallinella,

Parvovirus B19 (B19V), an ssDNA virus in the family Parvoviridae, is a human pathogenic virus, responsible for a wide range of clinical manifestations, still in need of effective and specific antivirals. DNA structures, including G-quadruplex (G4), have been recognised as relevant functional features in viral genomes, and small-molecule ligands binding ... Read more >>

Viruses (Viruses)
[2020, 12(9):]

Cited: 1 time

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Advanced analytical methodologies in Alzheimer's disease drug discovery.

Angela De Simone, Marina Naldi, Daniele Tedesco, Manuela Bartolini, Lara Davani, Vincenza Andrisano,

Despite the constant progress in the understanding of the etiopathogenesis of Alzheimer's disease (AD) over the last 50 years, just four long-standing drugs are currently used for AD therapy. This article reviews the analytical methodologies developed and applied in the last five years to address the early-stage tasks of the ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2020, 178:112899]

Cited: 1 time

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Crystal Structure of Chloroplastic Thioredoxin f2 from Chlamydomonas reinhardtii Reveals Distinct Surface Properties.

Stéphane D Lemaire, Daniele Tedesco, Pierre Crozet, Laure Michelet, Simona Fermani, Mirko Zaffagnini, Julien Henri,

Protein disulfide reduction by thioredoxins (TRXs) controls the conformation of enzyme active sites and their multimeric complex formation. TRXs are small oxidoreductases that are broadly conserved in all living organisms. In photosynthetic eukaryotes, TRXs form a large multigenic family, and they have been classified in different types: f, m, x, ... Read more >>

Antioxidants (Basel) (Antioxidants (Basel, Switzerland))
[2018, 7(12):]

Cited: 9 times

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Tau-Centric Multitarget Approach for Alzheimer's Disease: Development of First-in-Class Dual Glycogen Synthase Kinase 3β and Tau-Aggregation Inhibitors.

Annachiara Gandini, Manuela Bartolini, Daniele Tedesco, Loreto Martinez-Gonzalez, Carlos Roca, Nuria E Campillo, Josefa Zaldivar-Diez, Concepción Perez, Giampaolo Zuccheri, Andrea Miti, Alessandra Feoli, Sabrina Castellano, Sabrina Petralla, Barbara Monti, Martina Rossi, Fabio Moda, Giuseppe Legname, Ana Martinez, Maria Laura Bolognesi,

Several findings propose the altered tau protein network as an important target for Alzheimer's disease (AD). Particularly, two points of pharmacological intervention can be envisaged: inhibition of phosphorylating tau kinase GSK-3β and tau aggregation process. On the basis of this consideration and on our interest in multitarget paradigms in AD, ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2018, 61(17):7640-7656]

Cited: 11 times

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New insights into the altered binding capacity of pharmaceutical-grade human serum albumin: site-specific binding studies by induced circular dichroism spectroscopy.

Anna Tramarin, Daniele Tedesco, Marina Naldi, Maurizio Baldassarre, Carlo Bertucci, Manuela Bartolini,

The ADMET profile of drugs is strongly affected by human serum albumin (HSA), due to its leading role as carrier of poorly soluble compounds in plasma; a critical assessment of the binding capacity of HSA and the evaluation of binding competition between drugs are therefore pivotal for a reliable pharmacokinetic ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2019, 162:171-178]

Cited: 1 time

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Structural basis for the magnesium-dependent activation of transketolase from Chlamydomonas reinhardtii.

Miriam Pasquini, Simona Fermani, Daniele Tedesco, Chiara Sciabolini, Pierre Crozet, Marina Naldi, Julien Henri, Ute Vothknecht, Carlo Bertucci, Stéphane D Lemaire, Mirko Zaffagnini, Francesco Francia,

<h4>Background</h4>In photosynthetic organisms, transketolase (TK) is involved in the Calvin-Benson cycle and participates to the regeneration of ribulose-5-phosphate. Previous studies demonstrated that TK catalysis is strictly dependent on thiamine pyrophosphate (TPP) and divalent ions such as Mg<sup>2+</sup>.<h4>Methods</h4>TK from the unicellular green alga Chlamydomonas reinhardtii (CrTK) was recombinantly produced and purified ... Read more >>

Biochim Biophys Acta Gen Subj (Biochimica et biophysica acta. General subjects)
[2017, 1861(8):2132-2145]

Cited: 3 times

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Human Serum Albumin as Chiral Selector in Enantioselective High-Performance Liquid Chromatography.

Carlo Bertucci, Daniele Tedesco,

Enantioselective high-performance liquid chromatography (eHPLC) using chiral stationary phases (CSPs) is surely the most used technique for the determination of the enantiomeric excess (e.e.) of chiral drugs, a fundamental parameter for reliable studies on the relationship between stereochemistry and pharmacological activity. A key aspect of this enantioseparation technique is the ... Read more >>

Curr Med Chem (Current medicinal chemistry)
[2017, 24(8):743-757]

Cited: 2 times

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Absolute Configuration Assignment of Chiral Resorcin[4]arenes from ECD Spectra.

Gerardo Concilio, Carmen Talotta, Carmine Gaeta, Placido Neri, Guglielmo Monaco, Riccardo Zanasi, Daniele Tedesco, Carlo Bertucci,

Racemates of five chiral resorcin[4]arenes, four tetra-O-substituted and one hepta-O-substituted, have been resolved by enantioselective HPLC, and their ECD spectra have been recorded online by stopped-flow measurements. The absolute configuration has been assigned by comparison of the experimental ECD spectra with DFT and semiempirical calculations. For the four tetra-O-substituted resorcin[4]arenes, ... Read more >>

J Org Chem (The Journal of organic chemistry)
[2017, 82(1):202-210]

Cited: 0 times

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Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain.

Margherita Brindisi, Samuele Maramai, Sandra Gemma, Simone Brogi, Alessandro Grillo, Lorenzo Di Cesare Mannelli, Emanuele Gabellieri, Stefania Lamponi, Simona Saponara, Beatrice Gorelli, Daniele Tedesco, Tommaso Bonfiglio, Christophe Landry, Kwang-Mook Jung, Andrea Armirotti, Livio Luongo, Alessia Ligresti, Fabiana Piscitelli, Carlo Bertucci, Marie-Pierre Dehouck, Giuseppe Campiani, Sabatino Maione, Carla Ghelardini, Anna Pittaluga, Daniele Piomelli, Vincenzo Di Marzo, Stefania Butini,

We report the discovery of compound 4a, a potent β-lactam-based monoacylglycerol lipase (MGL) inhibitor characterized by an irreversible and stereoselective mechanism of action, high membrane permeability, high brain penetration evaluated using a human in vitro blood-brain barrier model, high selectivity in binding and affinity-based proteomic profiling assays, and low in ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2016, 59(6):2612-2632]

Cited: 17 times

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Corrigendum to "Surface plasmon resonance and circular dichroism characterization of cucurbitacins binding to serum albumins for early pharmacokinetic profiling" [J. Pharm. Biomed. Anal. 122 (2016) 166-172].

Edoardo Fabini, Giovana Maria Lanchoti Fiori, Daniele Tedesco, Norberto Peporine Lopes, Carlo Bertucci,

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2016, 125:433]

Cited: 0 times

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Surface plasmon resonance and circular dichroism characterization of cucurbitacins binding to serum albumins for early pharmacokinetic profiling.

Edoardo Fabini, Giovana Maria Lanchoti Fiori, Daniele Tedesco, Norberto Peporine Lopes, Carlo Bertucci,

Cucurbitacins are a group of tetracyclic triterpenoids, known for centuries for their anti-cancer and anti-inflammatory properties, which are being actively investigated over the past decades in order to elucidate their mechanism of action. In perspective of being used as therapeutic molecules, a pharmacokinetic characterization is crucial to assess the affinity ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2016, 122:166-172]

Cited: 8 times

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Stopped-Flow Enantioselective HPLC-CD Analysis and TD-DFT Stereochemical Characterization of Methyl Trans-3-(3,4-Dimethoxyphenyl)Glycidate.

Daniele Tedesco, Edoardo Fabini, Vakhtang Barbakadze, Maia Merlani, Riccardo Zanasi, Bezhan Chankvetadze, Carlo Bertucci,

Caffeic acid-derived polyethers are a class of natural products isolated from the root extracts of comfrey and bugloss, which are endowed with intriguing pharmacological properties as anticancer agents. The synthesis of new polyether derivatives is achieved through ring-opening polymerization of chiral 2,3-disubstituted oxiranes, whose absolute configurations define the overall stereochemistry ... Read more >>

Chirality (Chirality)
[2015, 27(12):914-918]

Cited: 0 times

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Short-range solvation effects on chiroptical properties: a time-dependent density functional theory and ab initio molecular dynamics computational case study on austdiol.

Daniele Tedesco, Riccardo Zanasi, Barbara Kirchner, Carlo Bertucci,

The description of solvation effects on the chiroptical properties of chiral molecules is still a difficult challenge in the field of computational spectroscopy; this issue is critical in stereochemical characterization, since a reliable assessment of absolute configuration requires high accuracy. The present case study reports the huge effect of solvation ... Read more >>

J Phys Chem A (The journal of physical chemistry. A)
[2014, 118(50):11751-11757]

Cited: 1 time

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Induced circular dichroism as a tool to investigate the binding of drugs to carrier proteins: Classic approaches and new trends.

Daniele Tedesco, Carlo Bertucci,

Induced circular dichroism (ICD) is a spectroscopic phenomenon that provides versatile and useful methods for characterizing the structural and dynamic properties of the binding of drugs to target proteins. The understanding of biorecognition processes at the molecular level is essential to discover and validate new pharmacological targets, and to design ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2015, 113:34-42]

Cited: 6 times

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Characterization of the species-dependent ketoprofen/albumin binding modes by induced CD spectroscopy and TD-DFT calculations.

Daniele Tedesco, Marco Pistolozzi, Riccardo Zanasi, Carlo Bertucci,

The stereospecificity of high-affinity biorecognition phenomena at the basis of the activity of drugs is an important topic of active research in medicinal chemistry. The binding of drugs to their targets or to carrier proteins may lead to the onset of an induced circular dichroism (ICD) signal, which can be ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2015, 112:176-180]

Cited: 2 times

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Stereochemical and conformational study on fenoterol by ECD spectroscopy and TD-DFT calculations.

Daniele Tedesco, Riccardo Zanasi, Irving W Wainer, Carlo Bertucci,

Fenoterol and its derivatives are selective β2-adrenergic receptor (β2-AR) agonists whose stereoselective biological activities have been extensively investigated in the past decade; a complete stereochemical characterization of fenoterol derivatives is therefore crucial for a better understanding of the effects of stereochemistry on β2-AR binding. In the present project, the relationship ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2014, 91:92-96]

Cited: 2 times

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Determination of levamisole and tetramisole in seized cocaine samples by enantioselective high-performance liquid chromatography and circular dichroism detection.

Carlo Bertucci, Daniele Tedesco, Edoardo Fabini, Anna Maria Di Pietra, Francesca Rossi, Marco Garagnani, Elia Del Borrello, Vincenza Andrisano,

Levamisole, an anthelmintic drug, has been increasingly employed as an adulterant of illicit street cocaine over the last decade; recently, the use of tetramisole, the racemic mixture of levamisole and its enantiomer dexamisole, was also occasionally observed. A new enantioselective high-performance liquid chromatography (HPLC) method, performed on cellulose tris(3,5-dimethylphenylcarbamate) chiral ... Read more >>

J Chromatogr A (Journal of chromatography. A)
[2014, 1363:150-154]

Cited: 4 times

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Enantioresolution, stereochemical characterization and biological activity of a chiral large-conductance calcium-activated potassium channel opener.

Roccaldo Sardella, Andrea Carotti, Giuseppe Manfroni, Daniele Tedesco, Alma Martelli, Carlo Bertucci, Violetta Cecchetti, Benedetto Natalini,

A number of large-conductance calcium-activated potassium (BK) channel openers based on the 2-aryl-1,4-benzothiazine scaffold were previously synthesized, and 2-(5-bromo-2-methoxyphenyl)-6-trifluoromethyl-2H-1,4-benzothiazin-3(4H)-one (1) was identified as the most active compound. Since a stereoselective activation of BK channels was demonstrated for arylindolone derivatives, the effect of the absolute configuration at the C-2 position on ... Read more >>

J Chromatogr A (Journal of chromatography. A)
[2014, 1363:162-168]

Cited: 7 times

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Determination of dextromethorphan and levomethorphan in seized heroin samples by enantioselective HPLC and electronic CD.

Daniele Tedesco, Anna Maria Di Pietra, Francesca Rossi, Marco Garagnani, Elia Del Borrello, Carlo Bertucci, Vincenza Andrisano,

A new enantioselective HPLC method was developed for the resolution and determination of the enantiomers of methorphan, dextromethorphan (DXM) and levomethorphan (LVM), on a Chiralcel OJ column (250 mm × 4.6mm I.D.). The resolution of DXM and LVM was obtained using a mobile phase consisting of (n-hexane)-(2-propanol)-diethylamine (70:30:0.1, v/v/v) at ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2013, 81-82:76-79]

Cited: 4 times

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Mycoleptones A-C and polyketides from the endophyte Mycoleptodiscus indicus.

Willian J Andrioli, Raphael Conti, Magali J Araújo, Riccardo Zanasi, Bruno C Cavalcanti, Viviane Manfrim, Juliano S Toledo, Daniele Tedesco, Manoel O de Moraes, Cláudia Pessoa, Angela K Cruz, Carlo Bertucci, José Sabino, Dhammika N P Nanayakkara, Mônica T Pupo, Jairo K Bastos,

Three new azaphilones with an unusual methylene bridge, named mycoleptones A, B, and C (2, 4, and 5), were isolated from cultures of Mycoleptodiscus indicus, a fungus associated with the South American medicinal plant Borreria verticillata. Additionally, four known polyketides, austdiol (1), eugenitin (3), 6-methoxyeugenin (6), and 9-hydroxyeugenin (7), were ... Read more >>

J Nat Prod (Journal of natural products)
[2014, 77(1):70-78]

Cited: 7 times

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Chiral triazole fungicide difenoconazole: absolute stereochemistry, stereoselective bioactivity, aquatic toxicity, and environmental behavior in vegetables and soil.

Fengshou Dong, Jing Li, Bezhan Chankvetadze, Yongpu Cheng, Jun Xu, Xingang Liu, Yuanbo Li, Xiu Chen, Carlo Bertucci, Daniele Tedesco, Riccardo Zanasi, Yongquan Zheng,

In this study, the systemic assessments of the stereoisomers of triazole fungicide difenoconazole are reported for the first time, including absolute stereochemistry, stereoselective bioactivity toward pathogens (Alternaria sonali, Fulvia fulva, Botrytis cinerea, and Rhizoctonia solani), and toxicity toward aquatic organisms (Scenedesmus obliquus, Daphnia magna, and Danio rerio). Moreover, the stereoselective ... Read more >>

Environ Sci Technol (Environmental science & technology)
[2013, 47(7):3386-3394]

Cited: 35 times

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