Full Text Journal Articles by
Author Carlo Bertucci

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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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Indole Derivative Interacts with Estrogen Receptor Beta and Inhibits Human Ovarian Cancer Cell Growth.

Laura Verardi, Jessica Fiori, Vincenza Andrisano, Alessandra Locatelli, Rita Morigi, Marina Naldi, Carlo Bertucci, Elena Strocchi, Carla Boga, Gabriele Micheletti, Natalia Calonghi,

Ovarian cancer remains the leading cause of mortality among gynecological tumors. Estrogen receptor beta (ERβ) expression has been suggested to act as a tumor suppressor in epithelial ovarian cancer by reducing both tumor growth and metastasis. ERβ expression abnormalities represent a critical step in the development and progression of ovarian ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2020, 25(19):]

Cited: 0 times

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Unveiling the Biochemistry of the Epigenetic Regulator SMYD3.

Edoardo Fabini, Vladimir O Talibov, Filip Mihalic, Marina Naldi, Manuela Bartolini, Carlo Bertucci, Alberto Del Rio, U Helena Danielson,

SET and MYND domain-containing protein 3 (SMYD3) is a lysine methyltransferase that plays a central role in a variety of cancer diseases, exerting its pro-oncogenic activity by methylation of key proteins, of both nuclear and cytoplasmic nature. However, the role of SMYD3 in the initiation and progression of cancer is ... Read more >>

Biochemistry (Biochemistry)
[2019, 58(35):3634-3645]

Cited: 3 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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Special Issue "Chiroptical Spectroscopy: Instrumentation, Experimental Aspects and Applications" in memory of Ettore Castiglioni.

Sergio Abbate, Carlo Bertucci, Lorenzo Di Bari, Gennaro Pescitelli, Nina Berova, John Caldwell,

Chirality (Chirality)
[2018, 30(3):226]

Cited: 0 times

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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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Albumin Homodimers in Patients with Cirrhosis: Clinical and Prognostic Relevance of a Novel Identified Structural Alteration of the Molecule.

Maurizio Baldassarre, Marco Domenicali, Marina Naldi, Maristella Laggetta, Ferdinando A Giannone, Maurizio Biselli, Daniela Patrono, Carlo Bertucci, Mauro Bernardi, Paolo Caraceni,

Decompensated cirrhosis is associated to extensive post-transcriptional changes of human albumin (HA). This study aims to characterize the occurrence of HA homodimerization in a large cohort of patients with decompensated cirrhosis and to evaluate its association with clinical features and prognosis. HA monomeric and dimeric isoforms were identified in peripheral ... Read more >>

Sci Rep (Scientific reports)
[2016, 6:35987]

Cited: 12 times

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Surface plasmon resonance and isothermal titration calorimetry to monitor the Ni(II)-dependent binding of Helicobacter pylori NikR to DNA.

Edoardo Fabini, Barbara Zambelli, Luca Mazzei, Stefano Ciurli, Carlo Bertucci,

NikR is a transcription factor that regulates the expression of Ni(II)-dependent enzymes and other proteins involved in nickel trafficking. In the human pathogenic bacterium Helicobacter pylori, NikR (HpNikR) controls, among others, the expression of the Ni(II) enzyme urease by binding the double-strand DNA (dsDNA) operator region of the urease promoter ... Read more >>

Anal Bioanal Chem (Analytical and bioanalytical chemistry)
[2016, 408(28):7971-7980]

Cited: 3 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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Mass spectrometry characterization of circulating human serum albumin microheterogeneity in patients with alcoholic hepatitis.

Marina Naldi, Maurizio Baldassarre, Marco Domenicali, Ferdinando Antonino Giannone, Matteo Bossi, Jonathan Montomoli, Thomas Damgaard Sandahl, Emilie Glavind, Hendrik Vilstrup, Paolo Caraceni, Carlo Bertucci,

Human serum albumin (HSA) is the most abundant plasma protein, endowed with several biological properties unrelated to its oncotic power, such as antioxidant and free-radicals scavenging activities, binding and transport of many endogenous and exogenous substances, and regulation of endothelial function and inflammatory response. These non-oncotic activities are closely connected ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2016, 122:141-147]

Cited: 6 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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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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A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth.

Alessia Peserico, Aldo Germani, Paola Sanese, Armenio Jorge Barbosa, Valeria Di Virgilio, Raffaella Fittipaldi, Edoardo Fabini, Carlo Bertucci, Greta Varchi, Mary Pat Moyer, Giuseppina Caretti, Alberto Del Rio, Cristiano Simone,

SMYD3 is a histone lysine methyltransferase that plays an important role in transcriptional activation as a member of an RNA polymerase complex, and its oncogenic role has been described in different cancer types. We studied the expression and activity of SMYD3 in a preclinical model of colorectal cancer (CRC) and ... Read more >>

J Cell Physiol (Journal of cellular physiology)
[2015, 230(10):2447-2460]

Cited: 46 times

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Ischaemia-modified albumin: a marker of bacterial infection in hospitalized patients with cirrhosis.

Ferdinando A Giannone, Marco Domenicali, Maurizio Baldassarre, Michele Bartoletti, Marina Naldi, Maristella Laggetta, Carlo Bertucci, Antonio Colecchia, Pierluigi Viale, Mauro Bernardi, Paolo Caraceni,

<h4>Background & aims</h4>Patients with cirrhosis present structural changes of human serum albumin (HSA) affecting non-oncotic functions. Ischaemia-modified albumin (IMA), which reflects the capacity to bind cobalt, has been associated to patient mortality during acute-on-chronic liver failure. This study aimed to assess whether circulating IMA is elevated in advanced cirrhosis and ... Read more >>

Liver Int (Liver international : official journal of the International Association for the Study of the Liver)
[2015, 35(11):2425-2432]

Cited: 11 times

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Mass spectrometric characterization of human serum albumin dimer: A new potential biomarker in chronic liver diseases.

Marina Naldi, Maurizio Baldassarre, Marina Nati, Maristella Laggetta, Ferdinando Antonino Giannone, Marco Domenicali, Mauro Bernardi, Paolo Caraceni, Carlo Bertucci,

Human serum albumin (HSA) undergoes several structural alterations affecting its properties in pro-oxidant and pro-inflammatory environments, as it occurs during liver cirrhosis. These modifications include the formation of albumin dimers. Although HSA dimers were reported to be an oxidative stress biomarker, to date nothing is known about their role in ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2015, 112:169-175]

Cited: 10 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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Species-dependent binding of new synthesized bicalutamide analogues to albumin by optical biosensor analysis.

Cecilia Fortugno, Toon van der Gronde, Greta Varchi, Andrea Guerrini, Carlo Bertucci,

The binding of some novel bicalutamide analogues to human serum albumin (HSA) and rat serum albumin (RSA) was investigated by surface plasmon resonance (SPR) based optical biosensor technique. The serum protein binding of the bicalutamide analogues was determined and compared to that of the parent compound. Furthermore, HSA and RSA ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2015, 111:324-332]

Cited: 4 times

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Posttranscriptional changes of serum albumin: clinical and prognostic significance in hospitalized patients with cirrhosis.

Marco Domenicali, Maurizio Baldassarre, Ferdinando A Giannone, Marina Naldi, Marianna Mastroroberto, Maurizio Biselli, Maristella Laggetta, Daniela Patrono, Carlo Bertucci, Mauro Bernardi, Paolo Caraceni,

<h4>Unlabelled</h4>Beside the regulation of fluid distribution, human serum albumin (HSA) carries other activities, such as binding, transport, and detoxification of many molecules. In patients with cirrhosis, HSA exhibits posttranscriptional alterations that likely affect its functions. This study aimed at identifying the structural HSA alterations occurring in cirrhosis and determining their ... Read more >>

Hepatology (Hepatology (Baltimore, Md.))
[2014, 60(6):1851-1860]

Cited: 47 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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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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