Tuning Tubulin Dynamics and Interactions to Face Neurotoxicity: a Multidisciplinary Approach for Training and Research

Livrables

Organization of the Training School 3 days Live Cell Imaging providing stateoftheart of advanced imaging application in living cells The training school will be followed by a Seminar Presentations about the new achieved research results 1 day

Workshop 2

Workshop 6 (1 day): “Ethics and Research” providing the main ethic issues

Training School 2

Training School 2 (3 days): “Industrial Property Management” providing the indispensable and fundamental know-how of Industrial Property issues

Workshop 1

Workshop 3 1 day keynotes lecture on Protein aggregation in neuronal diseases with invitation of external scientists

Final Conference

Organization of the Final Conference

Paper Publication 1

Publication of 23 papers acknowledging the project published

Recruitment advertising publication

Recruitment advertising publication has to be avilable and published on the website The advertisement has to be just published also on the social media and on the pages of the specialistic journals

Paper Publication 2

At least 6 papers acknowledging the project published

Flyer

the flyer with the description of the project has to be available

Web Site

Web site has to be online and updated with all the relevant information

Publications

Effect of Clinically Used Microtubule Targeting Drugs on Viral Infection and Transport Function

Auteurs: Ángela Oliva, Carlota Tosat-Bitrián, Lucía Barrado-Gil, Francesca Bonato, Inmaculada Galindo, Urtzi Garaigorta, Beatriz Álvarez-Bernad, Rebeca París-Ogáyar, Daniel Lucena-Agell, Juan Francisco Giménez-Abián, Isabel García-Dorival, Jesús Urquiza, Pablo Gastaminza, José Fernando Díaz, Valle Palomo and Covadonga Alonso
Publié dans: International Journal of Molecular Sciences, 2022, ISSN 1422-0067
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms23073448

Design, Synthesis, and In Vitro Evaluation of Tubulin-targeting Dibenzothiazines with Antiproliferative Activity as Novel Heterocycle Building Block

Auteurs: Guerra, W.D.; Lucena-Agell, D.; Hortigüela, R.; Rossi, R.A.; Díaz, J.F.; Padrón, J.M. and Barolo, S.M.
Publié dans: ChemMedChem, 2021, ISSN 1860-7179
Éditeur: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202100383

α-Synuclein: An All-Inclusive Trip Around its Structure, Influencing Factors and Applied Techniques

Auteurs: Nicolò Bisi, Lucia Feni, Kaliroi Peqini, Helena Pérez-Peña, Sandrine Ongeri, Stefano Pieraccini, Sara Pellegrino
Publié dans: Frontiers in Chemistry, Numéro 9, 2021, ISSN 2296-2646
Éditeur: Frontiers
DOI: 10.3389/fchem.2021.666585

Structural basis of noscapine activation for tubulin binding

Auteurs: Oliva, M.A.; Prota, A.E.; Rodríguez-Salarichs, J.; Gu, W.; Bennani, Y.L.; Jiménez-Barbero, J.; Bargsten, K.; Canales, A.; Steinmetz, M.O.; Díaz, J.F.
Publié dans: Journal of medicinal chemistry, 2020, ISSN 0022-2623
Éditeur: American Chemical Society
DOI: 10.1021/acs.jmedchem.0c00855

Breaking down and building up alpha-synuclein: an insight on its N-terminal domain

Auteurs: Kaliroi Peqini, Simone Attanasio, L. Feni, Graziella Cappelletti, Sara Pellegrino
Publié dans: Journal of peptide science, 2023, ISSN 1099-1387
Éditeur: wiley
DOI: 10.1002/psc.3556

1,3-Benzodioxole-Modified Noscapine Analogues: Synthesis, Antiproliferative Activity, and Tubulin-Bound Structure

Auteurs: Cassandra Yong, Shane M. Devine, Anne-Catherine Abel, Stefan D. Tomlins, Divya Muthiah, Xuexin Gao, Richard Callaghan, Michel O. Steinmetz, Andrea E. Prota, Ben Capuano, and Peter J. Scammells
Publié dans: ChemMedChem, 2021, ISSN 1860-7187
Éditeur: ChemMedChem
DOI: 10.1002/cmdc.202100363

On the Importance of the Thiazole Nitrogen in Epothilones: Semisynthesis and Microtubule-Binding Affinity of Deaza-Epothilone C

Auteurs: Edenharter, A.; Ryckewaert, L.; Cintulová, D., Estévez-Gallego, J.; Díaz, J.F.; Altmann, K.H.
Publié dans: Chemistry, 2020, ISSN 2624-8549
Éditeur: MDPI
DOI: 10.3390/chemistry2020030

Microtubule-modulating Agents in the Fight Against Neurodegeneration: Will it ever Work?

Auteurs: Ahmed Soliman, Lidia Bakota, Roland Brandt
Publié dans: Current Neuropharmacology, 2022, ISSN 1875-6190
Éditeur: Bentham Science Publisher
DOI: 10.2174/1570159x19666211201101020

Method for the Stereoselective Construction of the Hemiaminal Center in Zampanolides

Auteurs: Brütsch, T.M.; Berardozzi, S.; Rothe, M.L.; Redondo-Horcajo, M;. Díaz, J.F.; Altmann, K.H. A.
Publié dans: organic letters, 2020, ISSN 1523-7060
Éditeur: American Chemical Society
DOI: 10.1021/acs.orglett.0c02974

Super-resolution imaging and quantitative analysis of microtubule arrays in model neurons show that epothilone D increases the density but decreases the length and straightness of microtubules in axon-like processes

Auteurs: Christian Conze, Nataliya I Trushina, Michael Holtmannspötter, Marina Rierola, Simone Attanasio, Lidia Bakota, Jacob Piehler, Roland Brandt
Publié dans: Brain Research Bulletin, 2022, ISSN 1873-2747
Éditeur: Elsevier BV
DOI: 10.1016/j.brainresbull.2022.10.008

Structural insight into the stabilization 1 of microtubules by taxanes

Auteurs: Andrea E Prota, Daniel Lucena-Agell, Yuntao Ma, Juan Estevez-Gallego, Shuo Li, Katja Bargsten, Fernando Josa-Prado, Karl-Heinz Altmann, Natacha Gaillard, Shinji Kamimura, Tobias Mühlethaler, Federico Gago, Maria A Oliva, Michel O Steinmetz, Wei-Shuo Fang, J Fernando Díaz
Publié dans: Structural Biology and Molecular Biophysics, 2023, ISSN 2050-084X
Éditeur: eLife Sciences Publications
DOI: 10.7554/elife.84791

Synthesis of Morpholine-Based Analogs of (-)-Zampanolide and Their Biological Activity

Auteurs: Bold, C. P.; Gut, M.; Schürmann, J.; Lucena-Agell, D.; Gertsch, J.; Díaz; J.F.; Altmann, K.H.
Publié dans: Chemistry a european journal, 2021, ISSN 0947-6539
Éditeur: John Wiley & Sons Ltd.
DOI: 10.1002/chem.202003996

Studies toward the Synthesis of an Oxazole-Based Analog of (-)-Zampanolide

Auteurs: Bold, C.; Klaus, C.; Pfeiffer, B.; Schürmann, J.; Lombardi, R.; Lucena-Agell, D.; Díaz, J.F.; Altmann, K.-H
Publié dans: organic letters, 2021, ISSN 1523-7060
Éditeur: American Chemical Society
DOI: 10.1021/acs.orglett.1c00378

N‑alkylisatin‑based microtubule destabilizers bind to the colchicine site on tubulin and retain efficacy in drug resistant acute lymphoblastic leukemia cell lines with less in vitro neurotoxicity

Auteurs: Keenan, B., Finol‑Urdaneta, R.K.; Hope, A.; Bremner, J.B.; Kavallaris, M., Lucena‑Agell, D.; Oliva, M.A.; Díaz, J.F.; Vine, K.L
Publié dans: Cancer cell international, 2020, ISSN 1475-2867
Éditeur: BioMed Central
DOI: 10.1186/s12935-020-01251-6

The Positive Side of the Alzheimer’s Disease Amyloid Cross-Interactions: The Case of the Aβ 1-42 Peptide with Tau, TTR, CysC, and ApoA1

Auteurs: Lidia Ciccone , Chenghui Shi, Davide di Lorenzo, Anne-Cécile Van Baelen and Nicolo Tonali
Publié dans: Molecules, 2020, ISSN 1420-3049
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25102439

Two Antagonistic Microtubule Targeting Drugs Act Synergistically to Kill Cancer Cells

Auteurs: Peronne, L; Denarier, E.; Rai, A.; Prudent, R.; Vernet, A.; Suzanne, P.; Ramirez-Rios, S.; Michallet, S.; Guidetti, M.; Vollaire, J.; Lucena-Agell, D.; Ribba, A.S.; Josserand, V.; Coll, J.L.; Dallemagne, P.; Díaz, J.F.; Oliva, M.A.; Sadoul, K.; Akhmanova, A.; Andrieux, A.; Lafanechère, L.
Publié dans: Cancers, 2020, ISSN 2072-6694
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cancers12082196

Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site

Auteurs: Matthew, S.; Chen, Q.Y.; Ratnayake, R.; Fermaintt, C.S.; Lucena-Agell, D.; Bonato, F.; Prota, A.E.; Lim, S.T.; Wang, X.; Díaz, J.F.; Risinger, A.L.; Paul, V.J.; Oliva, M.A., Luesch, H.
Publié dans: Proceedings of the National academy of sciences (PNAS), 2021, ISSN 0027-8424
Éditeur: National Academy of Sciences
DOI: 10.1073/pnas.2021847118

Computational Approaches to the Rational Design of Tubulin-Targeting Agents

Auteurs: Helena Pérez-Peña , Anne-Catherine Abel, Maxim Shevelev , Andrea E Prota , Stefano Pieraccini , Dragos Horvath
Publié dans: Biomolecules, 2023, ISSN 2218-273X
Éditeur: MDPI
DOI: 10.3390/biom13020285

Chemical modulation of microtubule structure through the laulimalide/peloruside site

Auteurs: JuanEstévez-Gallego, Beatriz Álvarez-Bernad, Benet Pera, Christoph Wullschleger, Olivier Raes, Dirk Menche, Juan Carlos Martínez, Daniel Lucena-Agell, Andrea E.Prota, Francesca Bonato, Katja Bargsten, Jelle Cornelus, Juan Francisco Giménez-Abián, Peter Northcote, Michel O.Steinmetz, Shinji Kamimura, Karl-Heinz Altmann, Ian Paterson, Federico Gago, Johan Van der Eycke, J Fernando Díaz, Marí
Publié dans: Structure, 2023, ISSN 1878-4186
Éditeur: Elsevier BV
DOI: 10.1016/j.str.2022.11.006

Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders

Auteurs: Paola Marzullo, Zlata Boiarska, Helena Pérez‐Peña, Anne‐Catherine Abel, Beatriz Álvarez‐Bernad, Daniel Lucena‐Agell, Francesca Vasile, Maurizio Sironi, Karl‐Heinz Altmann, Andrea E. Prota, J. Fernando Díaz, Stefano Pieraccini, Daniele Passarella
Publié dans: Chemistry – A European Journal, 2021, ISSN 0947-6539
Éditeur: John Wiley & Sons Ltd.
DOI: 10.1002/chem.202103520

Microtubule-targeting agents and neurodegeneration

Auteurs: Zlata Boiarska, Daniele Passarella
Publié dans: Drug Discovery Today, Numéro 26/2, 2021, Page(s) 604-615, ISSN 1359-6446
Éditeur: Elsevier BV
DOI: 10.1016/j.drudis.2020.11.033

Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: further chemical modifications and potential therapeutic effects against lymphomas

Auteurs: Marilia Barreca; Virginia Spanò; Roberta Rocca; Roberta Bivacqua; Anne-Catherine Abel; Annalisa Maruca; Alessandra Montalbano; Maria Valeria Raimondi; Chiara Tarantelli; Eugenio Gaudio; Luciano Cascione; Andrea Rinaldi; Ruoli Bai; Michel O. Steinmetz; Andrea E. Prota; Stefano Alcaro; Ernest Hamel; Francesco Bertoni; Paola Barraja
Publié dans: European Journal of Medicinal Chemistry, 2022, ISSN 0223-5234
Éditeur: Elsevier BV
DOI: 10.1016/j.ejmech.2022.114744

Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics

Auteurs: Zlata Boiarska, Helena Pérez-Peña, Anne-Catherine Abel, Paola Marzullo, Beatriz Álvarez-Bernad, Francesca Bonato, Benedetta Santini, Dragos Horvath, Daniel Lucena-Agell, Francesca Vasile, Maurizio Sironi, J. Fernando Díaz, Andrea E. Prota, Stefano Pieraccini, Daniele Passarella
Publié dans: Chemistry-A European Journal, 2022, ISSN 1521-3765
Éditeur: Wiley-VCH GmbH
DOI: 10.1002/chem.202203431

CLIP-170S is a novel microtubule +TIP variant that confers resistance to taxanes by impairing drug-target engagement

Auteurs: Thakkar, P.V.; Kita, K.; del Castillo, U.; Galletti, G.; Madhukar; N.; Vila-Navarro, E.; Barasoain, I.; Goodson, H.V.; Sackett, D.; Díaz, J.F.; Lu, Y; RoyChoudhary, A.; Molina, H.; Elemento, O.; Shah, M.A.; Giannakakou, P.
Publié dans: Developmental Cell, 2021, ISSN 1534-5807
Éditeur: Cell Press
DOI: 10.1016/j.devcel.2021.09.023

Structural model for differential cap maturation at growing microtubule ends

Auteurs: Estévez-Gallego, J.; Josa-Prado, F.; Ku, S.; Buey, R.M.; Balaguer, F.A., Prota, A.E.; Lucena-Agell, D.; Kamma-Lorger,C.; Steinmetz, M.O.; Barasoain,I.; Chrétien, D.; Kamimura, S.; Díaz, J.F.; Oliva, M.A.
Publié dans: Structural Biology and Molecular Biophysics, 2020, ISSN 2050-084X
Éditeur: eLife Sciences Publications
DOI: 10.7554/elife.50155

Pathological Pathways and Alpha-Synuclein in Parkinson’s Disease: A View from the Periphery

Auteurs: Milo Jarno Basellini,, Josine Marie Kothuis, Alessandro Comincini, Gianni Pezzoli, Graziella Cappelletti, Samanta Mazzetti Front. Biosci
Publié dans: Frontiers in Bioscience-Landmark, 2023, ISSN 2768-6698
Éditeur: IMR press
DOI: 10.31083/j.fbl2802033

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