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Author Marina Naldi

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From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects.

Caterina Pont, Tiziana Ginex, Christian Griñán-Ferré, Matthias Scheiner, Alexia Mattellone, Noemí Martínez, Elsa M Arce, Yolanda Soriano-Fernández, Marina Naldi, Angela De Simone, Marta Barenys, Jesús Gómez-Catalán, Belén Pérez, Raimon Sabate, Vincenza Andrisano, María Isabel Loza, José Brea, Manuela Bartolini, Maria Laura Bolognesi, Michael Decker, Mercè Pallàs, F Javier Luque, Diego Muñoz-Torrero,

Starting from six potential hits identified in a virtual screening campaign directed to a cryptic pocket of BACE-1, at the edge of the catalytic cleft, we have synthesized and evaluated six hybrid compounds, designed to simultaneously reach BACE-1 secondary and catalytic sites and to exert additional activities of interest for ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 225:113779]

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Bio-Guided Fractionation of Stem Bark Extracts from Phyllanthus muellarianus: Identification of Phytocomponents with Anti-Cholinesterase Activity.

Marina Naldi, Gloria Brusotti, Gabriella Massolini, Vincenza Andrisano, Caterina Temporini, Manuela Bartolini,

A combination of flash chromatography, solid phase extraction, high-performance liquid chromatography, and in vitro bioassays was used to isolate phytocomponents endowed with anticholinesterase activity in extract from <i>Phyllanthus muellarianus.</i> Phytocomponents responsible for the anti-cholinesterase activity of subfractions PMF1 and PMF4 were identified and re-assayed to confirm their activity. Magnoflorine was ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2021, 26(14):]

Cited: 0 times

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Determination of Effective Albumin in Patients With Decompensated Cirrhosis: Clinical and Prognostic Implications.

Maurizio Baldassarre, Marina Naldi, Giacomo Zaccherini, Michele Bartoletti, Agnese Antognoli, Maristella Laggetta, Martina Gagliardi, Manuel Tufoni, Marco Domenicali, Katja Waterstradt, Paola Paterini, Anna Baldan, Simona Leoni, Manuela Bartolini, Pierluigi Viale, Franco Trevisani, Mauro Bernardi, Paolo Caraceni,

<h4>Background and aims</h4>Circulating albumin in cirrhosis can be dysfunctional because of accumulating structural damages, leading to the concept of effective albumin concentration (eAlb), referring to the albumin portion presenting structural and functional integrity. We aimed to estimate eAlb in patients with decompensated cirrhosis and analyze its relationships with albumin function ... Read more >>

Hepatology (Hepatology (Baltimore, Md.))
[2021, 74(4):2058-2073]

Cited: 3 times

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New Coumarin Derivatives as Cholinergic and Cannabinoid System Modulators.

Serena Montanari, Marco Allarà, Laura Scalvini, Magdalena Kostrzewa, Federica Belluti, Silvia Gobbi, Marina Naldi, Silvia Rivara, Manuela Bartolini, Alessia Ligresti, Alessandra Bisi, Angela Rampa,

In the last years, the connection between the endocannabinoid system (eCS) and neuroprotection has been discovered, and evidence indicates that eCS signaling is involved in the regulation of cognitive processes and in the pathophysiology of Alzheimer's disease (AD). Accordingly, pharmacotherapy targeting eCS could represent a valuable contribution in fighting a ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2021, 26(11):]

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Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties.

Giselle de Andrade Ramos, Andressa Souza de Oliveira, Manuela Bartolini, Marina Naldi, Irene Liparulo, Christian Bergamini, Elisa Uliassi, Ling Wu, Paul E Fraser, Monica Abreu, Alessandra Sofia Kiametis, Ricardo Gargano, Edilberto Rocha Silveira, Guilherme D Brand, Lukas Prchal, Ondřej Soukup, Jan Korábečný, Maria Laura Bolognesi, Luiz Antonio Soares Romeiro,

As part of our efforts to develop sustainable drugs for Alzheimer's disease (AD), we have been focusing on the inexpensive and largely available cashew nut shell liquid (CNSL) as a starting material for the identification of new acetylcholinesterase (AChE) inhibitors. Herein, we decided to investigate whether cardanol, a phenolic CNSL ... Read more >>

RSC Med Chem (RSC medicinal chemistry)
[2021, 12(7):1154-1163]

Cited: 1 time

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From Combinations to Single-Molecule Polypharmacology-Cromolyn-Ibuprofen Conjugates for Alzheimer's Disease.

Claudia Albertini, Marina Naldi, Sabrina Petralla, Silvia Strocchi, Daniela Grifoni, Barbara Monti, Manuela Bartolini, Maria Laura Bolognesi,

Despite Alzheimer's disease (AD) incidence being projected to increase worldwide, the drugs currently on the market can only mitigate symptoms. Considering the failures of the classical paradigm "one target-one drug-one disease" in delivering effective medications for AD, polypharmacology appears to be a most viable therapeutic strategy. Polypharmacology can involve combinations ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2021, 26(4):]

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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Functional characterization of multifunctional ligands targeting acetylcholinesterase and alpha 7 nicotinic acetylcholine receptor.

Monika Cieslikiewicz-Bouet, Marina Naldi, Manuela Bartolini, Belén Pérez, Denis Servent, Ludovic Jean, Rómulo Aráoz, Pierre-Yves Renard,

Alzheimer's disease (AD) is a neurodegenerative disorder associated with cholinergic dysfunction, provoking memory loss and cognitive dysfunction in elderly patients. The cholinergic hypothesis provided over the years with molecular targets for developing palliative treatments for AD, acting on the cholinergic system, namely, acetylcholinesterase and α7 nicotinic acetylcholine receptor (α7 nAChR). ... Read more >>

Biochem Pharmacol (Biochemical pharmacology)
[2020, 177:114010]

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Unveiling the molecular mechanisms underpinning biorecognition of early-glycated human serum albumin and receptor for advanced glycation end products.

Anna Tramarin, Marina Naldi, Genny Degani, Loredana Lupu, Pascal Wiegand, Angelica Mazzolari, Alessandra Altomare, Giancarlo Aldini, Laura Popolo, Giulio Vistoli, Michael Przybylski, Manuela Bartolini,

Serum levels of early-glycated albumin are significantly increased in patients with diabetes mellitus and may play a role in worsening inflammatory status and sustaining diabetes-related complications. To investigate possible pathological recognition involving early-glycated albumin and the receptor for advanced glycation end products (RAGE), an early-glycated human serum albumin (HSAgly), with ... Read more >>

Anal Bioanal Chem (Analytical and bioanalytical chemistry)
[2020, 412(18):4245-4259]

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In vitro thrombogenicity of drug-eluting and bare metal stents.

Tullio Palmerini, Chiara Barozzi, Luciana Tomasi, Diego Della Riva, Mario Marengo, Gianfranco Cicoria, Antonio G Bruno, Maria-Letizia Bacchi-Reggiani, Marina Naldi, Manuela Bartolini, Stefano Fanti, Nazzareno Galiè, Gregg W Stone,

<h4>Aims</h4>We sought to investigate the thrombogenicity of different DES and BMS in an in vitro system of stent perfusion.<h4>Material and methods</h4>The experimental model consisted of a peristaltic pump connected to 4 parallel silicone tubes in which different stents were deployed. Blood was drawn from healthy volunteers and the amount of ... Read more >>

Thromb Res (Thrombosis research)
[2020, 185:43-48]

Cited: 0 times

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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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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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Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.

Jesús M Roldán-Peña, Valle Romero-Real, Javier Hicke, Inés Maya, Antonio Franconetti, Irene Lagunes, José M Padrón, José M Padrón, Sabrina Petralla, Eleonora Poeta, Marina Naldi, Manuela Bartolini, Barbara Monti, Maria L Bolognesi, Óscar López, José G Fernández-Bolaños,

Concerned by the devastating effects of Alzheimer's disease, and the lack of effective drugs, we have carried out the design of a series of tacrine-phenolic heterodimers in order to tackle the multifactorial nature of the disease. Hybridization of both pharmacophores involved the modification of the nature (imino, amino, ether) and ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 181:111550]

Cited: 5 times

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Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.

Serena Montanari, Ali Mokhtar Mahmoud, Letizia Pruccoli, Alessandro Rabbito, Marina Naldi, Sabrina Petralla, Ignacio Moraleda, Manuela Bartolini, Barbara Monti, Isabel Iriepa, Federica Belluti, Silvia Gobbi, Vincenzo Di Marzo, Alessandra Bisi, Andrea Tarozzi, Alessia Ligresti, Angela Rampa,

To address the multifactorial nature of Alzheimer's Disease (AD), a multi-target-directed ligand approach was herein developed. As a follow-up of our previous studies, a small library of newly designed 2-arylbenzofuran derivatives was evaluated towards cholinesterases and cannabinoid receptors. The two most promising compounds, 8 and 10, were then assessed for ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 178:243-258]

Cited: 3 times

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Polycyclic Maleimide-based Scaffold as New Privileged Structure for Navigating the Cannabinoid System Opportunities.

Alessandra Bisi, Alì Mokhtar Mahmoud, Marco Allará, Marina Naldi, Federica Belluti, Silvia Gobbi, Alessia Ligresti, Angela Rampa,

The discovery of the relevant role played by a dysregulation of the endogenous cannabinoid system in several pathological conditions has prompted an extensive research in this field. In this Letter, a series of cannabinoid receptor ligands bearing a previously unexplored polycyclic scaffold was designed and synthesized, in order to evaluate ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2019, 10(4):596-600]

Cited: 2 times

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Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.

Killian Oukoloff, Nicolas Coquelle, Manuela Bartolini, Marina Naldi, Rémy Le Guevel, Stéphane Bach, Béatrice Josselin, Sandrine Ruchaud, Marco Catto, Leonardo Pisani, Nunzio Denora, Rosa Maria Iacobazzi, Israel Silman, Joel L Sussman, Frédéric Buron, Jacques-Philippe Colletier, Ludovic Jean, Sylvain Routier, Pierre-Yves Renard,

Both cholinesterases (AChE and BChE) and kinases, such as GSK-3α/β, are associated with the pathology of Alzheimer's disease. Two scaffolds, targeting AChE (tacrine) and GSK-3α/β (valmerin) simultaneously, were assembled, using copper(I)-catalysed azide alkyne cycloaddition (CuAAC), to generate a new series of multifunctional ligands. A series of eight multi-target directed ligands ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 168:58-77]

Cited: 7 times

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Exploiting the Chalcone Scaffold to Develop Multifunctional Agents for Alzheimer's Disease.

Angela Rampa, Manuela Bartolini, Letizia Pruccoli, Marina Naldi, Isabel Iriepa, Ignacio Moraleda, Federica Belluti, Silvia Gobbi, Andrea Tarozzi, Alessandra Bisi,

Alzheimer's disease still represents an untreated multifaceted pathology, and drugs able to stop or reverse its progression are urgently needed. In this paper, a series of naturally inspired chalcone-based derivatives were designed as structural simplification of our previously reported benzofuran lead compound, aiming at targeting both acetyl (AChE)- and butyryl ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2018, 23(8):]

Cited: 6 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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Immobilized enzyme-based analytical tools in the -omics era: Recent advances.

Marina Naldi, Anna Tramarin, Manuela Bartolini,

Protein analysis is a field under rapid development mainly thanks to technological advances which have granted miniaturization of analytical devices, automation and higher detection sensitivity. The interest in the field has paralleled the expansion of the -omics era, laying down the bases for the current applications in proteomics and glycomics. ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2018, 160:222-237]

Cited: 1 time

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A patent review of butyrylcholinesterase inhibitors and reactivators 2010-2017.

Vincenza Andrisano, Marina Naldi, Angela De Simone, Manuela Bartolini,

INTRODUCTION:Butyrylcholinesterase (BuChE) has obtained a renewed interest as therapeutic target in Alzheimer's disease (AD), when changes in BuChE activity and expression along disease progression were highlighted as well as correlation between BuChE levels and cognitive function. AREAS COVERED:During the last eight years, fourteen patents on BuChE inhibitors (BuChEI) have been ... Read more >>

Expert Opin Ther Pat (Expert opinion on therapeutic patents)
[2018, 28(6):455-465]

Cited: 3 times

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Isolation and Characterization of Wheat Derived Nonspecific Lipid Transfer Protein 2 (nsLTP2).

Sara Bosi, Jessica Fiori, Giovanni Dinelli, Neil Rigby, Emanuela Leoncini, Cecilia Prata, Valeria Bregola, Ilaria Marotti, Roberto Gotti, Marina Naldi, Luca Massaccesi, Marco Malaguti, Paul Kroon, Silvana Hrelia,

Numerous studies support the protective role of bioactive peptides against cardiovascular diseases. Cereals represent the primary source of carbohydrates, but they also contain substantial amounts of proteins, therefore representing a potential dietary source of bioactive peptides with nutraceutical activities. The analysis of wheat extracts purified by chromatographic techniques by means ... Read more >>

J Food Sci (Journal of food science)
[2018, 83(6):1516-1521]

Cited: 2 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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Structural and functional integrity of human serum albumin: Analytical approaches and clinical relevance in patients with liver cirrhosis.

Marina Naldi, Maurizio Baldassarre, Marco Domenicali, Manuela Bartolini, Paolo Caraceni,

Human serum albumin (HSA) is the most abundant circulating plasma protein. Besides a significant contribution to the osmotic pressure, it is also involved in the fine regulation of many other physiological processes, including the balance of the redox state, the inflammatory and/or immunological responses, and the pharmacokinetic and pharmacodynamics of ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2017, 144:138-153]

Cited: 10 times

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Simple and rapid LC-MS method for the determination of circulating albumin microheterogeneity in veal calves exposed to heat stress.

Maurizio Baldassarre, Marina Naldi, Marco Domenicali, Sabrina Volo, Marco Pietra, Francesco Dondi, Paolo Caraceni, Angelo Peli,

Heat stress has a major impact on veal calves welfare and productivity. Prolonged exposure to warm temperature is associated with several alterations of physiologic processes and increased systemic inflammation and oxidative stress. Bovine serum albumin (BSA) is the most abundant plasma protein and, besides the regulation of osmotic pressure, carries ... Read more >>

J Pharm Biomed Anal (Journal of pharmaceutical and biomedical analysis)
[2017, 144:263-268]

Cited: 1 time

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Quinazoline based α1-adrenoreceptor antagonists with potent antiproliferative activity in human prostate cancer cell lines.

Valentina Maestri, Andrea Tarozzi, Elena Simoni, Antonio Cilia, Elena Poggesi, Marina Naldi, Benedetta Nicolini, Letizia Pruccoli, Michela Rosini, Anna Minarini,

New α<sub>1</sub>-adrenoreceptor (α<sub>1</sub>-AR) antagonists related to prazosin and doxazosin were synthesized by replacing piperazine ring with (S)- or (R)-3-aminopiperidine. Binding studies indicated that the S configuration at the 3-C position of the piperidine ring is crucial for an optimal interaction of the compounds at all three α<sub>1</sub>-AR subtypes. Quinazolines 9 ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2017, 136:259-269]

Cited: 2 times

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