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Author Manuela Bartolini

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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):]

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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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Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.

Michele Rossi, Michela Freschi, Luciana de Camargo Nascente, Alessandra Salerno, Sarah de Melo Viana Teixeira, Florian Nachon, Fabien Chantegreil, Ondrej Soukup, Lukáš Prchal, Marco Malaguti, Christian Bergamini, Manuela Bartolini, Cristina Angeloni, Silvana Hrelia, Luiz Antonio Soares Romeiro, Maria Laura Bolognesi,

The multifactorial nature of Alzheimer's disease (AD) is a reason for the lack of effective drugs as well as a basis for the development of "multi-target-directed ligands" (MTDLs). As cases increase in developing countries, there is a need of new drugs that are not only effective but also accessible. With ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2021, 64(8):4972-4990]

Cited: 2 times

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Phenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer's Disease.

Lukas Gorecki, Elisa Uliassi, Manuela Bartolini, Jana Janockova, Martina Hrabinova, Vendula Hepnarova, Lukas Prchal, Lubica Muckova, Jaroslav Pejchal, Jana Z Karasova, Eva Mezeiova, Marketa Benkova, Tereza Kobrlova, Ondrej Soukup, Sabrina Petralla, Barbara Monti, Jan Korabecny, Maria Laura Bolognesi,

Since 2002, no clinical candidate against Alzheimer's disease has reached the market; hence, an effective therapy is urgently needed. We followed the so-called "multitarget directed ligand" approach and designed 36 novel tacrine-phenothiazine heterodimers which were <i>in vitro</i> evaluated for their anticholinesterase properties. The assessment of the structure-activity relationships of such ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2021, 12(9):1698-1715]

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(±)-BIGI-3h: Pentatarget-Directed Ligand combining Cholinesterase, Monoamine Oxidase, and Glycogen Synthase Kinase 3β Inhibition with Calcium Channel Antagonism and Antiaggregating Properties for Alzheimer's Disease.

Lhassane Ismaili, Julie Monnin, Adeline Etievant, Raquel L Arribas, Lucía Viejo, Bernard Refouvelet, Ondrej Soukup, Jana Janockova, Vendula Hepnarova, Jan Korabecny, Tomas Kucera, Daniel Jun, Rudolf Andrys, Kamil Musilek, Aurelie Baguet, Eva M García-Frutos, Angela De Simone, Vincenza Andrisano, Manuela Bartolini, Cristóbal de Los Ríos, José Marco-Contelles, Emmanuel Haffen,

Multitarget-directed ligands (MTDLs) are considered a promising therapeutic strategy to address the multifactorial nature of Alzheimer's disease (AD). Novel MTDLs have been designed as inhibitors of human acetylcholinesterases/butyrylcholinesterases, monoamine oxidase A/B, and glycogen synthase kinase 3β and as calcium channel antagonists via the Biginelli multicomponent reaction. Among these MTDLs, (±)<b>-BIGI-3h</b> ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2021, 12(8):1328-1342]

Cited: 0 times

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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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Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP/PS1 Mice.

Elisabet Viayna, Nicolas Coquelle, Monika Cieslikiewicz-Bouet, Pedro Cisternas, Carolina A Oliva, Elena Sánchez-López, Miren Ettcheto, Manuela Bartolini, Angela De Simone, Mattia Ricchini, Marisa Rendina, Mégane Pons, Omidreza Firuzi, Belén Pérez, Luciano Saso, Vincenza Andrisano, Florian Nachon, Xavier Brazzolotto, Maria Luisa García, Antoni Camins, Israel Silman, Ludovic Jean, Nibaldo C Inestrosa, Jacques-Philippe Colletier, Pierre-Yves Renard, Diego Muñoz-Torrero,

The combination of the scaffolds of the cholinesterase inhibitor huprine Y and the antioxidant capsaicin results in compounds with nanomolar potencies toward human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) that retain or improve the antioxidant properties of capsaicin. Crystal structures of their complexes with AChE and BChE revealed the molecular basis ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2021, 64(1):812-839]

Cited: 3 times

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Targeting SMYD3 to Sensitize Homologous Recombination-Proficient Tumors to PARP-Mediated Synthetic Lethality.

Paola Sanese, Candida Fasano, Giacomo Buscemi, Cinzia Bottino, Silvia Corbetta, Edoardo Fabini, Valentina Silvestri, Virginia Valentini, Vittoria Disciglio, Giovanna Forte, Martina Lepore Signorile, Katia De Marco, Stefania Bertora, Valentina Grossi, Ummu Guven, Natale Porta, Valeria Di Maio, Elisabetta Manoni, Gianluigi Giannelli, Manuela Bartolini, Alberto Del Rio, Giuseppina Caretti, Laura Ottini, Cristiano Simone,

<i>SMYD3</i> is frequently overexpressed in a wide variety of cancers. Indeed, its inactivation reduces tumor growth in preclinical <i>in vivo</i> animal models. However, extensive characterization <i>in vitro</i> failed to clarify <i>SMYD3</i> function in cancer cells, although confirming its importance in carcinogenesis. Taking advantage of a <i>SMYD3</i> mutant variant identified in a high-risk ... Read more >>

iScience (iScience)
[2020, 23(10):101604]

Cited: 3 times

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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):]

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Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6.

F Javier Pérez-Areales, María Garrido, Ester Aso, Manuela Bartolini, Angela De Simone, Alba Espargaró, Tiziana Ginex, Raimon Sabate, Belén Pérez, Vincenza Andrisano, Dolors Puigoriol-Illamola, Mercè Pallàs, F Javier Luque, María Isabel Loza, José Brea, Isidro Ferrer, Francisco Ciruela, Angel Messeguer, Diego Muñoz-Torrero,

Oxidative stress is a major pathogenic factor in Alzheimer's disease, but it should not be tackled alone rather together with other key targets to derive effective treatments. The combination of the scaffold of the polar antioxidant lead 7-methoxy-2,2-dimethylchroman-6-ol (CR-6) with that of the lipophilic cholinesterase inhibitor 6-chlorotacrine results in compounds ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2020, 63(17):9360-9390]

Cited: 2 times

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Turning Donepezil into a Multi-Target-Directed Ligand through a Merging Strategy.

Rosaria Perone, Claudia Albertini, Elisa Uliassi, Flaminia Di Pietri, Pedro de Sena Murteira Pinheiro, Sabrina Petralla, Nicola Rizzardi, Romana Fato, Lenka Pulkrabkova, Ondrej Soukup, Anna Tramarin, Manuela Bartolini, Maria Laura Bolognesi,

Thanks to the widespread use and safety profile of donepezil (1) in the treatment of Alzheimer's disease (AD), one of the most widely adopted multi-target-directed ligand (MTDL) design strategies is to modify its molecular structure by linking a second fragment carrying an additional AD-relevant biological property. Herein, supported by a ... Read more >>

ChemMedChem (ChemMedChem)
[2021, 16(1):187-198]

Cited: 1 time

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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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N-1,2,3-triazole-isatin derivatives for cholinesterase and β-amyloid aggregation inhibition: A comprehensive bioassay study.

Carolina S Marques, Óscar López, Donatella Bagetta, Elisabete P Carreiro, Sabrina Petralla, Manuela Bartolini, Matthias Hoffmann, Stefano Alcaro, Barbara Monti, Maria Laura Bolognesi, Michael Decker, José G Fernández-Bolaños, Anthony J Burke,

Our goal was the evaluation of a series of N-1,2,3-triazole-isatin derivatives for multi-target activity which included cholinesterase (ChE) inhibition and β-amyloid (Aβ) peptide anti-aggregation. The compounds have shown considerable promise as butyrylcholinesterase (BuChE) inhibitors. Although the inhibition of eel acetylcholinesterase (eeAChE) was weak, the inhibitions against equine BuChE (eqBuChE) and ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2020, 98:103753]

Cited: 1 time

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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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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]

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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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A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.

F Javier Pérez-Areales, Andreea L Turcu, Marta Barniol-Xicota, Caterina Pont, Deborah Pivetta, Alba Espargaró, Manuela Bartolini, Angela De Simone, Vincenza Andrisano, Belén Pérez, Raimon Sabate, Francesc X Sureda, Santiago Vázquez, Diego Muñoz-Torrero,

The development of multitarget compounds against multifactorial diseases, such as Alzheimer's disease, is an area of very intensive research, due to the expected superior therapeutic efficacy that should arise from the simultaneous modulation of several key targets of the complex pathological network. Here we describe the synthesis and multitarget biological ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 180:613-626]

Cited: 4 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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Small-molecule inhibitors of lysine methyltransferases SMYD2 and SMYD3: current trends.

Edoardo Fabini, Elisabetta Manoni, Claudia Ferroni, Alberto Del Rio, Manuela Bartolini,

Lysine methyltransferases SMYD2 and SMYD3 are involved in the epigenetic regulation of cell differentiation and functioning. Overexpression and deregulation of these enzymes have been correlated to the insurgence and progression of different tumors, making them promising molecular targets in cancer therapy even if their role in tumors is not yet ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2019, 11(8):901-921]

Cited: 9 times

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QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer's Disease Therapy.

Eva Ramos, Alejandra Palomino-Antolín, Manuela Bartolini, Isabel Iriepa, Ignacio Moraleda, Daniel Diez-Iriepa, Abdelouahid Samadi, Carol V Cortina, Mourad Chioua, Javier Egea, Alejandro Romero, José Marco-Contelles,

We report the synthesis and relevant pharmacological properties of the quinoxalinetacrine (QT) hybrid <b>QT78</b> in a project targeted to identify new non-hepatotoxic tacrine derivatives for Alzheimer's disease therapy. We have found that <b>QT78</b> is less toxic than tacrine at high concentrations (from 100 μM to 1 mM), less potent than ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2019, 24(8):]

Cited: 3 times

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