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6 p, 6.1 MB |
Discovery of Neuroprotective Agents Based on a 5-(4-Pyridinyl)-1,2,4-triazole Scaffold
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Gitto, Rosaria (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Vittorio, Serena (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Bucolo, Federica (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Siracusa, Rosalba (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Cuzzocrea, Salvatore (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Di Paola, Rosanna (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
De Luca, Laura (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences)
Parkinson's disease (PD) is characterized by the death of dopaminergic neurons. The common histopathological hallmark in PD patients is the formation of intracellular proteinaceous accumulations. The main constituent of these inclusions is alpha-synuclein (α-syn), an intrinsically disordered protein that in pathological conditions creates amyloid aggregates that lead to neurotoxicity and neurodegeneration. [...]
2022 - 10.1021/acschemneuro.1c00849
ACS Chemical Neuroscience, Vol. 13, Issue 5 (March 2022) , p. 581-586
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4.
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14 p, 3.0 MB |
Ligand-Based Discovery of a Small Molecule as Inhibitor of α-Synuclein Amyloid Formation
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De Luca, Laura (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Vittorio, Serena (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Pitasi, Giovanna (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Fornt Suñé, Marc (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Bucolo, Federica (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences) ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Gitto, Rosaria (University of Messina. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences)
α-Synuclein (α-Syn) aggregates are implicated in Parkinson's disease (PD), so inhibitors of α-Syn aggregation have been intensively explored. It has been demonstrated that small molecules might be able to reduce α-Syn aggregation in fibrils, thus exerting neuroprotective effects in models of PD. [...]
2022 - 10.3390/ijms232314844
International journal of molecular sciences, Vol. 23, Issue 23 (November 2022) , art. 14844
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5.
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11 p, 2.5 MB |
The small aromatic compound SynuClean-D inhibits the aggregation and seeded polymerization of multiple α-synuclein strains
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Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Pujols Pujol, Jordi (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Vasili, Eftychia (Max Planck Institute for Experimental Medicine) ;
Pinheiro, Francisca (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Santos, Jaime (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Manglano-Artuñedo, Zoe (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Outeiro, Tiago Fleming (Scientific Employee With a Honorary Contract. Deutsches Zentrum für Neurodegenerative Erkrankungen (DZNE)) ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí")
Parkinson's disease is a neurodegenerative disorder characterized by the loss of dopaminergic neurons in the substantia nigra, as well as the accumulation of intraneuronal proteinaceous inclusions known as Lewy bodies and Lewy neurites. [...]
2022 - 10.1016/j.jbc.2022.101902
Journal of biological chemistry, Vol. 298, Issue 5 (May 2022) , art. 101902
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6.
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14 p, 4.4 MB |
α-Helical peptidic scaffolds to target α-synuclein toxic species with nanomolar affinity
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Santos, Jaime (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Gracia González, Pablo (Universidad de Zaragoza. Instituto de Biocomputación y Física de Sistemas Complejos) ;
Navarro, Susanna (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Pujols Pujol, Jordi (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Cremades, Nunilo (Universidad de Zaragoza. Instituto de Biocomputación y Física de Sistemas Complejos) ;
Pallarès i Goitiz, Irantzu (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí")
α-Synuclein aggregation is a key driver of neurodegeneration in Parkinson's disease and related syndromes. Accordingly, obtaining a molecule that targets α-synuclein toxic assemblies with high affinity is a long-pursued objective. [...]
2021 - 10.1038/s41467-021-24039-2
Nature communications, Vol. 12 (June 2021) , art. 3752
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12 p, 2.4 MB |
Inhibition of α-synuclein aggregation and mature fibril disassembling with a minimalistic compound, ZPDm
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Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Pujols Pujol, Jordi (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Pinheiro, Francisca (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Santos, Jaime (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Pallarès i Goitiz, Irantzu (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Navarro, Susanna (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Conde Giménez, María (Universidad de Zaragoza. Instituto Aragonés de Investigaciones Sanitarias) ;
García, Jesús (Institut de Recerca Biomèdica de Lleida) ;
Salvatella, Xavier (Institució Catalana de Recerca i Estudis Avançats) ;
Dalfo, Esther (Universitat Autònoma de Barcelona. Facultat de Medicina) ;
Sancho, Javier (Universidad de Zaragoza. Instituto Aragonés de Investigaciones Sanitarias) ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Universitat Autònoma de Barcelona.
Departament de Bioquímica i de Biologia Molecular
Synucleinopathies are a group of disorders characterized by the accumulation of α-Synuclein amyloid inclusions in the brain. Preventing α-Synuclein aggregation is challenging because of the disordered nature of the protein and the stochastic nature of fibrillogenesis, but, at the same time, it is a promising approach for therapeutic intervention in these pathologies. [...]
2020 - 10.3389/fbioe.2020.588947
Frontiers in Bioengineering and Biotechnology, Vol. 8 (October 2020) , art. 588947
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10 p, 3.4 MB |
Rational design of small molecules able to inhibit α-synuclein amyloid aggregation for the treatment of Parkinson's disease
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Vittorio, Serena (Università degli Studi di Messina Viale Palatucci. Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche e Ambientali) ;
Adornato, Ilenia (Università degli Studi di Messina Viale Palatucci. Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche e Ambientali) ;
Gitto, Rosaria (Università degli Studi di Messina Viale Palatucci. Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche e Ambientali) ;
Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
De Luca, Laura (Università degli Studi di Messina Viale Palatucci. Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche e Ambientali) ;
Universitat Autònoma de Barcelona.
Departament de Bioquímica i de Biologia Molecular
Parkinson's disease is one of the most common neurodegenerative disorders in elderly age. One of the mechanisms involved in the neurodegeneration appears related to the aggregation of the presynaptic protein alpha synuclein (α-syn) into toxic oligomers and fibrils. [...]
2020 - 10.1080/14756366.2020.1816999
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 35, Issue 1 (September 2020) , p. 1727-1735
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12 p, 3.6 MB |
ZPD-2, a small compound that inhibits α-synuclein amyloid aggregation and its seeded polymerization
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Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Pujols Pujol, Jordi (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Conde Giménez, María (Universidad de Zaragoza. Instituto Universitario de Investigación de Biocomputación y Física de Sistemas Complejos) ;
Carija, Anita (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Dalfo, Esther (Universitat Autònoma de Barcelona. Facultat de Medicina) ;
García, Jesús (Institut de Recerca Biomèdica de Lleida) ;
Navarro, Susanna (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Pinheiro, Francisca (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Santos, Jaime (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Salvatella, Xavier (Institut de Recerca Biomèdica de Lleida) ;
Sancho, Javier (Universidad de Zaragoza. Instituto Universitario de Investigación de Biocomputación y Física de Sistemas Complejos) ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular)
α-Synuclein (α-Syn) forms toxic intracellular protein inclusions and transmissible amyloid structures in Parkinson's disease (PD). Preventing α-Syn self-assembly has become one of the most promising approaches in the search for disease-modifying treatments for this neurodegenerative disorder. [...]
2019 - 10.3389/fnmol.2019.00306
Frontiers in molecular neuroscience, Vol. 12 (Dec. 2019) , art. 306
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12 p, 12.3 MB |
High-throughput screening methodology to identify alpha-synuclein aggregation inhibitors
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Pujols Pujol, Jordi (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Peña Díaz, Samuel (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Conde Giménez, María (Universidad de Zaragoza. Instituto Universitario de Investigación de Biocomputación y Física de Sistemas Complejos) ;
Pinheiro, Francisca (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Navarro, Susanna (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ;
Sancho, Javier (Universidad de Zaragoza. Instituto Universitario de Investigación de Biocomputación y Física de Sistemas Complejos) ;
Ventura, Salvador (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí")
An increasing number of neurodegenerative diseases are being found to be associated with the abnormal accumulation of aggregated proteins in the brain. In Parkinson's disease, this process involves the aggregation of alpha-synuclein (α-syn) into intraneuronal inclusions. [...]
2017 - 10.3390/ijms18030478
International journal of molecular sciences, Vol. 18 (March 2017) , art. 478
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