Multidisciplinary European Joint Doctorate in the Design and Development of Glyco Drugs

Informazioni relative al progetto

PhD4GlycoDrug

ID dell’accordo di sovvenzione: 765581

DOI

10.3030/765581

Progetto chiuso

Data della firma CE 17 Agosto 2017

Data di avvio 1 Ottobre 2017

Data di completamento 31 Gennaio 2022

Finanziato da

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Costo totale

€ 3 080 389,68

Contributo UE

€ 3 080 389,68

Coordinato da

UNIVERZA V LJUBLJANI
Slovenia

CORDIS fornisce collegamenti ai risultati finali pubblici e alle pubblicazioni dei progetti ORIZZONTE.

I link ai risultati e alle pubblicazioni dei progetti del 7° PQ, così come i link ad alcuni tipi di risultati specifici come dataset e software, sono recuperati dinamicamente da .OpenAIRE .

Risultati finali

Documents, reports (2)

Communication and public engagement report

The PhD4GlycoDrug network will assure that its research activities are made known to society at large in such a way that they can be understood by a layperson. Outreach activities will be conducted with the possibility to harvest feedback information from the targeted population, and will include: i) active participation in the Researchers’ Nights for each ESR; ii) communication via consortium website with links to Beneficiaries’ homepages and vice-versa, and link to Glycopedia; iii) social media communication (e.g. Twitter and Facebook); iv) project brochures and flyers distributed at public events (e.g. Information Days for high school students)and visits to high schools; v) Press releases, interviews and popular newspaper articles. To do so, we have made a Communication Plan and will report on its implementation. This deliverable will be updated at month 48.

Report on Dissemination of the results to scientific audience

Results will be published in quality international scientific journals, granting open access to all peer-reviewed scientific publications. The research work is expected to lead to 2-4 scientific publications per ESR, as 2 publications is a minimum requirement for a PhD thesis in some beneficiaries. High impact international journals will be targeted. To support the availability of scientific data and broad scientific community the results will be disseminated via the Network web-site, institutional repositories and networks, like ResearchGate. This deliverable will be updated at month 48.

Websites, patent fillings, videos etc. (1)

Webpage with social media linking options

To support the availability of scientific data and broad scientific community the results will be disseminated via the Network web-site. This will be designed and will be operative shortly after beginning of the project.

Pubblicazioni

Peer reviewed articles (28)

Preventing Influenza A Virus Infection by Mixed Inhibition of Neuraminidase and Hemagglutinin by Divalent Inhibitors

Autori: Xuan Wei, Wenjuan Du, Margherita Duca, Guangyun Yu, Erik de Vries, Cornelis A. M. de Haan, and Roland J. Pieters
Pubblicato in: Journal of Medicinal Chemistry, 2022, Pagina/e 7312–7323, ISSN 0022-2623
Editore: American Chemical Society
DOI: 10.1021/acs.jmedchem.2c00319

Discovery of two non-UDP-mimic inhibitors of O-GlcNAc transferase by screening a DNA-encoded library

Autori: Cyril Balsollier, Simon Bijkerk, Arjan de Smit, Kevin van Eekelen, Krištof Bozovičar, Dirk Husstege, Tihomir Tomašič, Marko Anderluh, Roland J Pieters
Pubblicato in: Bioorganic Chemistry, 2024, Pagina/e 107321, ISSN 0045-2068
Editore: Academic Press
DOI: 10.1016/j.bioorg.2024.107321

Benzimidazole–galactosides bind selectively to the Galectin-8 N-Terminal domain: Structure-based design and optimisation

Autori: Mujtaba Hassan, Sjors van Klaveren, Maria Håkansson, Carl Diehl, Rebeka Kovačič, Floriane Baussière, Anders P. Sundin, Jaka Dernovšek, Björn Walse, Fredrik Zetterberg, Hakon Leffler, Marko Anderluh, Tihomir Tomašič, Žiga Jakopin, Ulf J. Nilsson
Pubblicato in: European Journal of Medicinal Chemistry, 2021, ISSN 0223-5234
Editore: Elsevier BV
DOI: 10.1016/j.ejmech.2021.113664

Targeting a Multidrug-Resistant Pathogen: First Generation Antagonists of Burkholderia cenocepacia's BC2L-C Lectin

Autori: Rafael Bermeo, Kanhaya Lal, Davide Ruggeri, Daniele Lanaro, Sarah Mazzotta, Francesca Vasile, Anne Imberty, Laura Belvisi, Annabelle Varrot, Anna Bernardi
Pubblicato in: ACS Chemical Biology, 2022, Pagina/e 2899-2910, ISSN 1554-8929
Editore: American Chemical Society
DOI: 10.1021/acschembio.2c00532

Selective Galectin-8N Ligands: The Design and Synthesis of Phthalazinone-d-Galactals

Autori: Sjors van Klaveren, Anders P. Sundin, Žiga Jakopin, Marko Anderluh, Hakon Leffler, Ulf J. Nilsson, Tihomir Tomašič
Pubblicato in: ChemMedChem, 2022, Pagina/e 1-8, ISSN 1860-7187
Editore: Wiley
DOI: 10.1002/cmdc.202100575

Design and synthesis of novel 3-triazolyl-1-thiogalactosides as galectin-1, -3 and -8 inhibitors

Autori: Sjors van Klaveren; Jaka Dernovšek; Žiga Jakopin; Marko Anderluh; Hakon Leffler; Ulf J. Nilsson; Tihomir Tomašič
Pubblicato in: RSC Advances, Numero 17, 2022, ISSN 2046-2069
Editore: Royal Society of Chemistry
DOI: 10.1039/d2ra03163a

Design of OSMI-4 Analogs Using Scaffold Hopping: Investigating the Importance of the Uridine Mimic in the Binding of OGT Inhibitors

Autori: Cyril Balsollier, Dr. Tihomir Tomašič, Daniel Yasini, Simon Bijkerk, Prof. Marko Anderluh, Prof. Roland J. Pieters
Pubblicato in: ChemMedChem, 2023, Pagina/e e202300001, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202300001

Direct sialic acid 4-OAc substitution by nitrogen, sulfur and carbon nucleophiles with retention ofstereochemistry

Autori: Tiago Bozzola, Ulf J. Nilsson and Ulf Ellervik
Pubblicato in: RSC Advances, Numero 19, 2022, Pagina/e 11992–11995, ISSN 2046-2069
Editore: Royal Society of Chemistry
DOI: 10.1039/d2ra01576e

Identification of New L-Fucosyl and L-Galactosyl Amides as Glycomimetic Ligands of TNF Lectin Domain of BC2L-C from Burkholderia cenocepacia

Autori: Sarah Mazzotta; Giulia Antonini; Francesca Vasile; Emilie Gillon; Jon Lundstrøm; Annabelle Varrot; Laura Belvisi; Anna Bernardi
Pubblicato in: Molecules, 2023, Pagina/e 1494, ISSN 1420-3049
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules28031494

Recombinant Lectin from Tepary Bean (Phaseolus acutifolius) with Specific Recognition for Cancer-Associated Glycans: Production, Structural Characterization, and Target Identification

Autori: Dania Martínez-Alarcón, Annabelle Varrot, Elaine Fitches, John A. Gatehouse, Min Cao, Prashant Pyati, Alejandro Blanco-Labra, Teresa Garcia-Gasca
Pubblicato in: Biomolecules, Numero 10/4, 2020, Pagina/e 654, ISSN 2218-273X
Editore: MDPI
DOI: 10.3390/biom10040654

New Quinolinone O-GlcNAc Transferase Inhibitors Based on Fragment Growth

Autori: Weiss Matjaž, Loi Elena M., Sterle Maša, Balsollier Cyril, Tomašič Tihomir, Pieters Roland J., Gobec Martina, Anderluh Marko
Pubblicato in: Frontiers in Chemistry, 2021, ISSN 2296-2646
Editore: Frontiers Media S.A.
DOI: 10.3389/fchem.2021.666122

Multivalent Fucosides Targeting β-Propeller Lectins from Lung Pathogens with Promising Anti-Adhesive Properties

Autori: Duca, Margherita; Haksar, Diksha; van Neer, Jacq; Thies-Weesie, Dominique M E; Martínez-Alarcón, Dania; de Cock, Hans; Varrot, Annabelle; Pieters, Roland J; Molecular Microbiology; Afd Chemical Biology and Drug Discovery; Sub Molecular Microbiology; Sub Physical and Colloid Chemistry; Chemical Biology and Drug Discovery; Chemical Biology and Drug Discovery; Physical and Colloid Chemistry
Pubblicato in: ACS Chemical Biology, Numero 19, 2022, ISSN 1554-8929
Editore: American Chemical Society
DOI: 10.1021/acschembio.2c00708

Sialic Acid Derivatives Inhibit SiaT Transporters and Delay Bacterial Growth

Autori: Tiago Bozzola; Mariafrancesca Scalise; Christer U. Larsson; Michael C. Newton-Vesty; Caterina Rovegno; Ankita Mitra; Jonathan Cramer; Weixiao Yuan Wahlgren; Partha Radhakrishnan Santhakumari; Richard E. Johnsson; Oliver Schwardt; Beat Ernst; Rosmarie Friemann; Renwick C. J. Dobson; Cesare Indiveri; Jenny Schelin; Ulf J. Nilsson; Ulf Ellervik
Pubblicato in: ACS Chemical Biology, Numero 6, 2022, Pagina/e 1890–1900, ISSN 1554-8929
Editore: American Chemical Society
DOI: 10.1021/acschembio.2c00321

Tetra- and Hexavalent Siglec-8 Ligands Modulate Immune Cell Activation

Autori: Gabriele Conti, Anne Bärenwaldt, Said Rabbani, Tobias Mühlethaler, Mirza Sarcevic, Xiaohua Jiang, Oliver Schwardt, Daniel Ricklin, Roland J Pieters, Heinz Läubli, Beat Ernst
Pubblicato in: Angew Chem Int Ed Engl, 2023, Pagina/e e202314280, ISSN 1433-7851
Editore: John Wiley & Sons Ltd.
DOI: 10.1002/anie.202314280

Rhamnose-based glycomimetic for recruitment of endogenous anti-rhamnose antibodies

Autori: Nives Hribernik, Fabrizio Chiodo, Roland J. Pieters, Anna Bernardi
Pubblicato in: Tetrahedron Letters, 2022, ISSN 0040-4039
Editore: Elsevier BV
DOI: 10.1016/j.tetlet.2022.153843

BC2L-C N-Terminal Lectin Domain Complexed with Histo Blood Group Oligosaccharides Provides New Structural Information

Autori: Rafael Bermeo, Anna Bernardi, Annabelle Varrot
Pubblicato in: Molecules, Numero 25/2, 2020, Pagina/e 248, ISSN 1420-3049
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25020248

A Potent Mimetic of the Siglec‐8 Ligand 6’‐Sulfo‐Sialyl Lewisx

Autori: Blijke Kroezen, Gabriele Conti, Benedetta Girardi, Jonathan Cramer, Xiaohua Jiang, Said Rabbani, Jennifer Müller, Maja Kokot, Enrico Luisoni, Daniel Ricklin, Oliver Schwardt, Beat Ernst
Pubblicato in: ChemMedChem, Numero 15, 2020, Pagina/e 1706-1719, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202000417

Intracellular Hydrolysis of Small-Molecule O-Linked N-Acetylglucosamine Transferase Inhibitors Differs among Cells and Is Not Required for Its Inhibition

Autori: Elena Maria Loi, Matjaž Weiss, Stane Pajk, Martina Gobec, Tihomir Tomašič, Roland J. Pieters, Marko Anderluh
Pubblicato in: Molecules, Numero 25/15, 2020, Pagina/e 3381, ISSN 1420-3049
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25153381

Computational tools for drawing, building and displaying carbohydrates: a visual guide

Autori: Kanhaya Lal, Rafael Bermeo, Serge Perez
Pubblicato in: Beilstein Journal of Organic Chemistry, Numero 16, 2020, Pagina/e 2448-2468, ISSN 1860-5397
Editore: Beilstein-Institut
DOI: 10.3762/bjoc.16.199

Biochemical and structural studies of target lectin SapL1 from the emerging opportunistic microfungus Scedosporium apiospermum

Autori: Dania Martínez-Alarcón, Viviane Balloy, Jean-Philippe Bouchara, Roland J. Pieters, Annabelle Varrot
Pubblicato in: Scientific Reports, Numero 11/1, 2021, ISSN 2045-2322
Editore: Nature Publishing Group
DOI: 10.1038/s41598-021-95008-4

Structure-Guided Design of d-Galactal Derivatives with High Affinity and Selectivity for the Galectin-8 N-Terminal Domain.

Autori: Mujtaba Hassan; Mujtaba Hassan; Floriane Baussière; Samo Guzelj; Anders Sundin; Maria Håkansson; Rebeka Kovačič; Hakon Leffler; Tihomir Tomašič; Marko Anderluh; Žiga Jakopin; Ulf J. Nilsson
Pubblicato in: ACS Medicinal Chemistry Letters, Numero 1, 2021, Pagina/e 1745–1752, ISSN 1948-5875
Editore: American Chemical Society
DOI: 10.1021/acsmedchemlett.1c00371

Glycomimetic antagonists of BC2L-C lectin: insights from molecular dynamics simulations

Autori: Giulia Antonini; Monica Civera; Kanhaya Lal; Kanhaya Lal; Sarah Mazzotta; Annabelle Varrot; Anna Bernardi; Laura Belvisi
Pubblicato in: Frontiers in molecular biosciences, Numero 5, 2023, Pagina/e 1201630, ISSN 2296-889X
Editore: Frontiers Media S.A.
DOI: 10.3389/fmolb.2023.1201630

One pot synthesis of thio -glycosides via aziridine opening reactions

Autori: Nives Hribernik, Alice Tamburrini, Ermelinda Falletta, Anna Bernardi
Pubblicato in: Organic & Biomolecular Chemistry, Numero 19/1, 2021, Pagina/e 233-247, ISSN 1477-0520
Editore: Royal Society of Chemistry
DOI: 10.1039/d0ob01956a

Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside

Autori: Benedetta Girardi, Martina Manna, Sjors Van Klaveren, Tihomir Tomašič, Žiga Jakopin, Hakon Leffler, Ulf J. Nilsson, Daniel Ricklin, Janez Mravljak, Oliver Schwardt, Marko Anderluh
Pubblicato in: ChemMedChem, 2021, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202100514

Discovery of a New Drug-like Series of OGT Inhibitors by Virtual Screening

Autori: Loi, Elena M., Tihomir Tomašič, Cyril Balsollier, Kevin van Eekelen, Matjaž Weiss, Martina Gobec, Matthew G. Alteen, David J. Vocadlo, Roland J. Pieters, and Marko Anderluh
Pubblicato in: Molecules, 2022, Pagina/e 1-21, ISSN 1420-3049
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules27061996

Prediction and Validation of a Druggable Site on Virulence Factor of Drug Resistant Burkholderia cenocepacia

Autori: Kanhaya Lal, Rafael Bermeo, Jonathan Cramer, Francesca Vasile, Beat Ernst, Anne Imberty, Anna Bernardi, Annabelle Varrot, Laura Belvisi
Pubblicato in: Chemistry - A European Journal, 2021, Pagina/e 10341-10348, ISSN 1521-3765
Editore: Wiley-VCH Verlag
DOI: 10.1002/chem.202100252

Druggable Allosteric Sites in β-Propeller Lectins

Autori: Shanina E, Kuhaudomlarp S, Lal K, Seeberger PH, Imberty A, Rademacher C
Pubblicato in: Angewandte Chemie International Edition, Numero 52, 2022, Pagina/e 1-9, ISSN 1433-7851
Editore: John Wiley & Sons Ltd.
DOI: 10.1002/anie.202109339

Overview of the Assays to Probe O-Linked β-N-Acetylglucosamine Transferase Binding and Activity

Autori: Cyril Balsollier, Roland J. Pieters, Marko Anderluh
Pubblicato in: Molecules, Numero 26/4, 2021, Pagina/e 1037, ISSN 1420-3049
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules26041037

Thesis and dissertations (5)

DECOYS FOR DISRUPTING CARBOHYDRATE-LECTIN INTERACTIONS

Autori: Nives Hribernik
Pubblicato in: 2021
Editore: Universita' degli Studi di Milano

Novel glycomimetic inhibitors and proteolysis-targeting chimeras for human galectins

Autori: Hassan, Mujtaba
Pubblicato in: Numero 13, 2022, ISBN 978-91-7422-915-8
Editore: Lund University

DESIGN, SYNTHESIS AND EVALUATION OF ANTAGONISTS TOWARDS BC2L-C

Autori: Rafael Bermeo Malo
Pubblicato in: 2021
Editore: Universita' degli Studi di Milano
DOI: 10.13130/bermeo-malo-rafael_phd2021-06-18

A step forward in the anti-adhesive treatment of lung infections

Autori: Duca, Margherita; Faculteit Betawetenschappen
Pubblicato in: "Biochemistry [q-bio.BM]. Université Grenoble Alpes [2020-..]; Universiteit Utrecht (Utrecht, Nederland), 2023. English. ⟨NNT : 2023GRALV028⟩", Numero 17, 2023
Editore: Utrecht University
DOI: 10.33540/1692

STRUCTURE-BASED DESIGN OF GLYCOMIMETIC LIGANDS FOR THE N-TERMINAL DOMAIN OF BC2L-C LECTIN

Autori: Kanhaya Lal
Pubblicato in: 2021
Editore: Universita' degli Studi di Milano
DOI: 10.13130/lal-kanhaya_phd2021-12-15

Other (2)

Measuring Carbohydrate-Lectin Interactions : A Guide for Beginners

Autori: Margherita Duca
Pubblicato in: GlycoPedia, Numero e-chapter, 2020
Editore: GlycoPedia (https://www.glycopedia.eu/)

The Fascinating World of SigLec Proteins: A Primer

Autori: Benedetta Girardi, Serge Perez
Pubblicato in: GlycoPedia, Numero e-chapter, 2022
Editore: GlvcoPedia (https://www.glvcopedia.eu/)