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Author Sabrina Petralla

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TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy.

Vanesa Nozal, Loreto Martínez-González, Marta Gomez-Almeria, Claudia Gonzalo-Consuegra, Paula Santana, Apirat Chaikuad, Eva Pérez-Cuevas, Stefan Knapp, Daniel Lietha, David Ramírez, Sabrina Petralla, Barbara Monti, Carmen Gil, Angeles Martín-Requero, Valle Palomo, Eva de Lago, Ana Martinez,

Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease without any effective treatment. Protein TDP-43 is a pathological hallmark of ALS in both sporadic and familiar patients. Post-translational modifications of TDP-43 promote its aggregation in the cytoplasm. Tau-Tubulin kinase (TTBK1) phosphorylates TDP-43 in cellular and animal models; thus, TTBK1 inhibitors ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2022, :]

Cited: 0 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]

Cited: 0 times

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Epigenetics and Communication Mechanisms in Microglia Activation with a View on Technological Approaches.

Sabrina Petralla, Francesca De Chirico, Andrea Miti, Ottavia Tartagni, Francesca Massenzio, Eleonora Poeta, Marco Virgili, Giampaolo Zuccheri, Barbara Monti,

Microglial cells, the immune cells of the central nervous system (CNS), play a crucial role for the proper brain development and function and in CNS homeostasis. While in physiological conditions, microglia continuously check the state of brain parenchyma, in pathological conditions, microglia can show different activated phenotypes: In the early ... Read more >>

Biomolecules (Biomolecules)
[2021, 11(2):]

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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Dietary Protein Source Influences Brain Inflammation and Memory in a Male Senescence-Accelerated Mouse Model of Dementia.

Sabrina Petralla, Cristina Parenti, Valentina Ravaioli, Irene Fancello, Francesca Massenzio, Marco Virgili, Barbara Monti, Emiliano Pena-Altamira,

Dementia is a pathological condition characterized by a decline in memory, as well as in other cognitive and social functions. The cellular and molecular mechanisms of brain damage in dementia are not completely understood; however, neuroinflammation is involved. Evidence suggests that chronic inflammation may impair cognitive performance and that dietary ... Read more >>

Mol Neurobiol (Molecular neurobiology)
[2021, 58(4):1312-1329]

Cited: 1 time

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α-Linolenic Acid-Valproic Acid Conjugates: Toward Single-Molecule Polypharmacology for Multiple Sclerosis.

Michele Rossi, Sabrina Petralla, Michele Protti, Monica Baiula, Tereza Kobrlova, Ondrej Soukup, Santi Mario Spampinato, Laura Mercolini, Barbara Monti, Maria Laura Bolognesi,

Multiple sclerosis (MS) is a complex inflammatory, degenerative, and demyelinating disease of the central nervous system. Although treatments exist, MS cannot be cured by available drugs, which primarily target neuroinflammation. Thus, it is feasible that a well concerted polypharmacological approach able to act at multiple points within the intricate network ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2020, 11(12):2406-2413]

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: 2 times

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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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Correction to "Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease".

Angela De Simone, Valeria La Pietra, Nibal Betari, Nicola Petragnani, Mariarosaria Conte, Simona Daniele, Deborah Pietrobono, Claudia Martini, Sabrina Petralla, Raffaella Casadei, Lara Davani, Flavia Frabetti, Pasquale Russomanno, Ettore Novellino, Serena Montanari, Vincenzo Tumiatti, Patrizia Ballerini, Federica Sarno, Angela Nebbioso, Lucia Altucci, Barbara Monti, Vincenza Andrisano, Andrea Milelli,

[This corrects the article DOI: 10.1021/acsmedchemlett.8b00507.]. ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2019, 10(9):1357]

Cited: 0 times

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Deficiency of Mitochondrial Aspartate-Glutamate Carrier 1 Leads to Oligodendrocyte Precursor Cell Proliferation Defects Both In Vitro and In Vivo.

Sabrina Petralla, Luis Emiliano Peña-Altamira, Eleonora Poeta, Francesca Massenzio, Marco Virgili, Simona Nicole Barile, Luigi Sbano, Emanuela Profilo, Mariangela Corricelli, Alberto Danese, Carlotta Giorgi, Rita Ostan, Miriam Capri, Paolo Pinton, Ferdinando Palmieri, Francesco Massimo Lasorsa, Barbara Monti,

Aspartate-Glutamate Carrier 1 (AGC1) deficiency is a rare neurological disease caused by mutations in the solute carrier family 25, member 12 (<i>SLC25A12</i>) gene, encoding for the mitochondrial aspartate-glutamate carrier isoform 1 (AGC1), a component of the malate-aspartate NADH shuttle (MAS), expressed in excitable tissues only. AGC1 deficiency patients are children ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2019, 20(18):]

Cited: 6 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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Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.

Angela De Simone, Valeria La Pietra, Nibal Betari, Nicola Petragnani, Mariarosaria Conte, Simona Daniele, Deborah Pietrobono, Claudia Martini, Sabrina Petralla, Raffaella Casadei, Lara Davani, Flavia Frabetti, Pasquale Russomanno, Ettore Novellino, Serena Montanari, Vincenzo Tumiatti, Patrizia Ballerini, Federica Sarno, Angela Nebbioso, Lucia Altucci, Barbara Monti, Vincenza Andrisano, Andrea Milelli,

Several evidence pointed out the role of epigenetics in Alzheimer's disease (AD) revealing strictly relationships between epigenetic and "classical" AD targets. Based on the reported connection among histone deacetylases (HDACs) and glycogen synthase kinase 3β (GSK-3β), herein we present the discovery and the biochemical characterization of the first-in-class hit compound ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2019, 10(4):469-474]

Cited: 9 times

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Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.

Luiz Antonio Soares Romeiro, Jéssica Larissa da Costa Nunes, Camila de Oliveira Miranda, Gabriella Simões Heyn Roth Cardoso, Andressa Souza de Oliveira, Annachiara Gandini, Tereza Kobrlova, Ondrej Soukup, Michele Rossi, Johanna Senger, Manfred Jung, Silvia Gervasoni, Giulio Vistoli, Sabrina Petralla, Francesca Massenzio, Barbara Monti, Maria Laura Bolognesi,

Alzheimer's disease (AD) represents a global problem, with an estimation of the majority of dementia patients in low- and middle-income countries by 2050. Thus, the development of sustainable drugs has attracted much attention in recent years. In light of this, taking inspiration from the HDAC inhibitor vorinostat (<b>1</b>), we develop ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2019, 10(4):671-676]

Cited: 5 times

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Microglial overexpression of fALS-linked mutant SOD1 induces SOD1 processing impairment, activation and neurotoxicity and is counteracted by the autophagy inducer trehalose.

Francesca Massenzio, Emiliano Peña-Altamira, Sabrina Petralla, Marco Virgili, Giampaolo Zuccheri, Andrea Miti, Elisabetta Polazzi, Ilaria Mengoni, Deborah Piffaretti, Barbara Monti,

Amyotrophic lateral sclerosis (ALS) is a fatal motor neuron disease. Mutations in the gene encoding copper/zinc superoxide dismutase-1 (SOD1) are responsible for most familiar cases, but the role of mutant SOD1 protein dysfunction in non-cell autonomous neurodegeneration, especially in relation to microglial activation, is still unclear. Here, we focused our ... Read more >>

Biochim Biophys Acta Mol Basis Dis (Biochimica et biophysica acta. Molecular basis of disease)
[2018, 1864(12):3771-3785]

Cited: 6 times

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A Focused Library of Psychotropic Analogues with Neuroprotective and Neuroregenerative Potential.

Elisa Uliassi, Luis Emiliano Peña-Altamira, Aixa V Morales, Francesca Massenzio, Sabrina Petralla, Michele Rossi, Marinella Roberti, Loreto Martinez Gonzalez, Ana Martinez, Barbara Monti, Maria Laura Bolognesi,

Overcoming the lack of effective treatments and the continuous clinical trial failures in neurodegenerative drug discovery might require a shift from the prevailing paradigm targeting pathogenesis to the one targeting simultaneously neuroprotection and neuroregeneration. In the studies reported herein, we sought to identify small molecules that might exert neuroprotective and ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2019, 10(1):279-294]

Cited: 4 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: 12 times

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Nutritional and Pharmacological Strategies to Regulate Microglial Polarization in Cognitive Aging and Alzheimer's Disease.

Emiliano Peña-Altamira, Sabrina Petralla, Francesca Massenzio, Marco Virgili, Maria L Bolognesi, Barbara Monti,

The study of microglia, the immune cells of the brain, has experienced a renaissance after the discovery of microglia polarization. In fact, the concept that activated microglia can shift into the M1 pro-inflammatory or M2 neuroprotective phenotypes, depending on brain microenvironment, has completely changed the understanding of microglia in brain ... Read more >>

Front Aging Neurosci (Frontiers in aging neuroscience)
[2017, 9:175]

Cited: 16 times

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Down-regulation of the mitochondrial aspartate-glutamate carrier isoform 1 AGC1 inhibits proliferation and N-acetylaspartate synthesis in Neuro2A cells.

Emanuela Profilo, Luis Emiliano Peña-Altamira, Mariangela Corricelli, Alessandra Castegna, Alberto Danese, Gennaro Agrimi, Sabrina Petralla, Giulia Giannuzzi, Vito Porcelli, Luigi Sbano, Carlo Viscomi, Francesca Massenzio, Erika Mariana Palmieri, Carlotta Giorgi, Giuseppe Fiermonte, Marco Virgili, Luigi Palmieri, Massimo Zeviani, Paolo Pinton, Barbara Monti, Ferdinando Palmieri, Francesco Massimo Lasorsa,

The mitochondrial aspartate-glutamate carrier isoform 1 (AGC1) catalyzes a Ca<sup>2+</sup>-stimulated export of aspartate to the cytosol in exchange for glutamate, and is a key component of the malate-aspartate shuttle which transfers NADH reducing equivalents from the cytosol to mitochondria. By sustaining the complete glucose oxidation, AGC1 is thought to be ... Read more >>

Biochim Biophys Acta Mol Basis Dis (Biochimica et biophysica acta. Molecular basis of disease)
[2017, 1863(6):1422-1435]

Cited: 10 times

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Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease.

Jakub Jeřábek, Elisa Uliassi, Laura Guidotti, Jan Korábečný, Ondřej Soukup, Vendula Sepsova, Martina Hrabinova, Kamil Kuča, Manuela Bartolini, Luis Emiliano Peña-Altamira, Sabrina Petralla, Barbara Monti, Marinella Roberti, Maria Laura Bolognesi,

Multi-target drug discovery is one of the most followed approaches in the active central nervous system (CNS) therapeutic area, especially in the search for new drugs against Alzheimer's disease (AD). This is because innovative multi-target-directed ligands (MTDLs) could more adequately address the complexity of this pathological condition. In a continuation ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2017, 127:250-262]

Cited: 18 times

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Neuronal Regulation of Neuroprotective Microglial Apolipoprotein E Secretion in Rat In Vitro Models of Brain Pathophysiology.

Elisabetta Polazzi, Ilaria Mengoni, Emiliano Peña-Altamira, Francesca Massenzio, Marco Virgili, Sabrina Petralla, Barbara Monti,

Apolipoprotein E (ApoE) is mainly secreted by glial cells and is involved in many brain functions, including neuronal plasticity, β-amyloid clearance, and neuroprotection. Microglia--the main immune cells of the brain--are one source of ApoE, but little is known about the physiologic regulation of microglial ApoE secretion by neurons and whether ... Read more >>

J Neuropathol Exp Neurol (Journal of neuropathology and experimental neurology)
[2015, 74(8):818-834]

Cited: 5 times

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