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

Deliverables

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

Author(s): 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
Published in: International Journal of Molecular Sciences, 2022, ISSN 1422-0067
Publisher: 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

Author(s): Guerra, W.D.; Lucena-Agell, D.; Hortigüela, R.; Rossi, R.A.; Díaz, J.F.; Padrón, J.M. and Barolo, S.M.
Published in: ChemMedChem, 2021, ISSN 1860-7179
Publisher: 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

Author(s): Nicolò Bisi, Lucia Feni, Kaliroi Peqini, Helena Pérez-Peña, Sandrine Ongeri, Stefano Pieraccini, Sara Pellegrino
Published in: Frontiers in Chemistry, Issue 9, 2021, ISSN 2296-2646
Publisher: Frontiers
DOI: 10.3389/fchem.2021.666585

Structural basis of noscapine activation for tubulin binding

Author(s): 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.
Published in: Journal of medicinal chemistry, 2020, ISSN 0022-2623
Publisher: American Chemical Society
DOI: 10.1021/acs.jmedchem.0c00855

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

Author(s): Kaliroi Peqini, Simone Attanasio, L. Feni, Graziella Cappelletti, Sara Pellegrino
Published in: Journal of peptide science, 2023, ISSN 1099-1387
Publisher: wiley
DOI: 10.1002/psc.3556

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

Author(s): 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
Published in: ChemMedChem, 2021, ISSN 1860-7187
Publisher: ChemMedChem
DOI: 10.1002/cmdc.202100363

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

Author(s): Edenharter, A.; Ryckewaert, L.; Cintulová, D., Estévez-Gallego, J.; Díaz, J.F.; Altmann, K.H.
Published in: Chemistry, 2020, ISSN 2624-8549
Publisher: MDPI
DOI: 10.3390/chemistry2020030

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

Author(s): Ahmed Soliman, Lidia Bakota, Roland Brandt
Published in: Current Neuropharmacology, 2022, ISSN 1875-6190
Publisher: Bentham Science Publisher
DOI: 10.2174/1570159x19666211201101020

Method for the Stereoselective Construction of the Hemiaminal Center in Zampanolides

Author(s): Brütsch, T.M.; Berardozzi, S.; Rothe, M.L.; Redondo-Horcajo, M;. Díaz, J.F.; Altmann, K.H. A.
Published in: organic letters, 2020, ISSN 1523-7060
Publisher: 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

Author(s): Christian Conze, Nataliya I Trushina, Michael Holtmannspötter, Marina Rierola, Simone Attanasio, Lidia Bakota, Jacob Piehler, Roland Brandt
Published in: Brain Research Bulletin, 2022, ISSN 1873-2747
Publisher: Elsevier BV
DOI: 10.1016/j.brainresbull.2022.10.008

Structural insight into the stabilization 1 of microtubules by taxanes

Author(s): 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
Published in: Structural Biology and Molecular Biophysics, 2023, ISSN 2050-084X
Publisher: eLife Sciences Publications
DOI: 10.7554/elife.84791

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

Author(s): Bold, C. P.; Gut, M.; Schürmann, J.; Lucena-Agell, D.; Gertsch, J.; Díaz; J.F.; Altmann, K.H.
Published in: Chemistry a european journal, 2021, ISSN 0947-6539
Publisher: John Wiley & Sons Ltd.
DOI: 10.1002/chem.202003996

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

Author(s): Bold, C.; Klaus, C.; Pfeiffer, B.; Schürmann, J.; Lombardi, R.; Lucena-Agell, D.; Díaz, J.F.; Altmann, K.-H
Published in: organic letters, 2021, ISSN 1523-7060
Publisher: 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

Author(s): 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
Published in: Cancer cell international, 2020, ISSN 1475-2867
Publisher: 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

Author(s): Lidia Ciccone , Chenghui Shi, Davide di Lorenzo, Anne-Cécile Van Baelen and Nicolo Tonali
Published in: Molecules, 2020, ISSN 1420-3049
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25102439

Two Antagonistic Microtubule Targeting Drugs Act Synergistically to Kill Cancer Cells

Author(s): 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.
Published in: Cancers, 2020, ISSN 2072-6694
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cancers12082196

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

Author(s): 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.
Published in: Proceedings of the National academy of sciences (PNAS), 2021, ISSN 0027-8424
Publisher: National Academy of Sciences
DOI: 10.1073/pnas.2021847118

Computational Approaches to the Rational Design of Tubulin-Targeting Agents

Author(s): Helena Pérez-Peña , Anne-Catherine Abel, Maxim Shevelev , Andrea E Prota , Stefano Pieraccini , Dragos Horvath
Published in: Biomolecules, 2023, ISSN 2218-273X
Publisher: MDPI
DOI: 10.3390/biom13020285

Chemical modulation of microtubule structure through the laulimalide/peloruside site

Author(s): 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
Published in: Structure, 2023, ISSN 1878-4186
Publisher: Elsevier BV
DOI: 10.1016/j.str.2022.11.006

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

Author(s): 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
Published in: Chemistry – A European Journal, 2021, ISSN 0947-6539
Publisher: John Wiley & Sons Ltd.
DOI: 10.1002/chem.202103520

Microtubule-targeting agents and neurodegeneration

Author(s): Zlata Boiarska, Daniele Passarella
Published in: Drug Discovery Today, Issue 26/2, 2021, Page(s) 604-615, ISSN 1359-6446
Publisher: 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

Author(s): 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
Published in: European Journal of Medicinal Chemistry, 2022, ISSN 0223-5234
Publisher: Elsevier BV
DOI: 10.1016/j.ejmech.2022.114744

Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics

Author(s): 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
Published in: Chemistry-A European Journal, 2022, ISSN 1521-3765
Publisher: 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

Author(s): 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.
Published in: Developmental Cell, 2021, ISSN 1534-5807
Publisher: Cell Press
DOI: 10.1016/j.devcel.2021.09.023

Structural model for differential cap maturation at growing microtubule ends

Author(s): 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.
Published in: Structural Biology and Molecular Biophysics, 2020, ISSN 2050-084X
Publisher: eLife Sciences Publications
DOI: 10.7554/elife.50155

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

Author(s): Milo Jarno Basellini,, Josine Marie Kothuis, Alessandro Comincini, Gianni Pezzoli, Graziella Cappelletti, Samanta Mazzetti Front. Biosci
Published in: Frontiers in Bioscience-Landmark, 2023, ISSN 2768-6698
Publisher: IMR press
DOI: 10.31083/j.fbl2802033

Deliverables

Publications

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