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

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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.

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.

Publications

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

Auteurs: 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
Publié dans: European Journal of Medicinal Chemistry, 2021, ISSN 0223-5234
Éditeur: Elsevier BV
DOI: 10.1016/j.ejmech.2021.113664

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

Auteurs: Sjors van Klaveren, Anders P. Sundin, Žiga Jakopin, Marko Anderluh, Hakon Leffler, Ulf J. Nilsson, Tihomir Tomašič
Publié dans: ChemMedChem, 2022, Page(s) 1-8, ISSN 1860-7187
Éditeur: Wiley
DOI: 10.1002/cmdc.202100575

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

Auteurs: Sjors van Klaveren; Jaka Dernovšek; Žiga Jakopin; Marko Anderluh; Hakon Leffler; Ulf J. Nilsson; Tihomir Tomašič
Publié dans: RSC Advances, Numéro 17, 2022, ISSN 2046-2069
Éditeur: Royal Society of Chemistry
DOI: 10.1039/d2ra03163a

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

Auteurs: Tiago Bozzola, Ulf J. Nilsson and Ulf Ellervik
Publié dans: RSC Advances, Numéro 19, 2022, Page(s) 11992–11995, ISSN 2046-2069
Éditeur: Royal Society of Chemistry
DOI: 10.1039/d2ra01576e

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

Auteurs: Dania Martínez-Alarcón, Annabelle Varrot, Elaine Fitches, John A. Gatehouse, Min Cao, Prashant Pyati, Alejandro Blanco-Labra, Teresa Garcia-Gasca
Publié dans: Biomolecules, Numéro 10/4, 2020, Page(s) 654, ISSN 2218-273X
Éditeur: MDPI
DOI: 10.3390/biom10040654

New Quinolinone O-GlcNAc Transferase Inhibitors Based on Fragment Growth

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

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

Auteurs: 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
Publié dans: ACS Chemical Biology, Numéro 19, 2022, ISSN 1554-8929
Éditeur: American Chemical Society
DOI: 10.1021/acschembio.2c00708

Sialic Acid Derivatives Inhibit SiaT Transporters and Delay Bacterial Growth

Auteurs: 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
Publié dans: ACS Chemical Biology, Numéro 6, 2022, Page(s) 1890–1900, ISSN 1554-8929
Éditeur: American Chemical Society
DOI: 10.1021/acschembio.2c00321

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

Auteurs: Nives Hribernik, Fabrizio Chiodo, Roland J. Pieters, Anna Bernardi
Publié dans: Tetrahedron Letters, 2022, ISSN 0040-4039
Éditeur: 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

Auteurs: Rafael Bermeo, Anna Bernardi, Annabelle Varrot
Publié dans: Molecules, Numéro 25/2, 2020, Page(s) 248, ISSN 1420-3049
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25020248

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

Auteurs: Blijke Kroezen, Gabriele Conti, Benedetta Girardi, Jonathan Cramer, Xiaohua Jiang, Said Rabbani, Jennifer Müller, Maja Kokot, Enrico Luisoni, Daniel Ricklin, Oliver Schwardt, Beat Ernst
Publié dans: ChemMedChem, 2020, ISSN 1860-7179
Éditeur: 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

Auteurs: Elena Maria Loi, Matjaž Weiss, Stane Pajk, Martina Gobec, Tihomir Tomašič, Roland J. Pieters, Marko Anderluh
Publié dans: Molecules, Numéro 25/15, 2020, Page(s) 3381, ISSN 1420-3049
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25153381

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

Auteurs: Kanhaya Lal, Rafael Bermeo, Serge Perez
Publié dans: Beilstein Journal of Organic Chemistry, Numéro 16, 2020, Page(s) 2448-2468, ISSN 1860-5397
Éditeur: Beilstein-Institut
DOI: 10.3762/bjoc.16.199

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

Auteurs: Dania Martínez-Alarcón, Viviane Balloy, Jean-Philippe Bouchara, Roland J. Pieters, Annabelle Varrot
Publié dans: Scientific Reports, Numéro 11/1, 2021, ISSN 2045-2322
Éditeur: 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.

Auteurs: 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
Publié dans: ACS Medicinal Chemistry Letters, Numéro 1, 2021, Page(s) 1745–1752, ISSN 1948-5875
Éditeur: American Chemical Society
DOI: 10.1021/acsmedchemlett.1c00371

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

Auteurs: Giulia Antonini; Monica Civera; Kanhaya Lal; Kanhaya Lal; Sarah Mazzotta; Annabelle Varrot; Anna Bernardi; Laura Belvisi
Publié dans: Frontiers in molecular biosciences, Numéro 5, 2023, Page(s) 1201630, ISSN 2296-889X
Éditeur: Frontiers Media S.A.
DOI: 10.3389/fmolb.2023.1201630

One pot synthesis of thio -glycosides via aziridine opening reactions

Auteurs: Nives Hribernik, Alice Tamburrini, Ermelinda Falletta, Anna Bernardi
Publié dans: Organic & Biomolecular Chemistry, Numéro 19/1, 2021, Page(s) 233-247, ISSN 1477-0520
Éditeur: Royal Society of Chemistry
DOI: 10.1039/d0ob01956a

Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside

Auteurs: Benedetta Girardi, Martina Manna, Sjors Van Klaveren, Tihomir Tomašič, Žiga Jakopin, Hakon Leffler, Ulf J. Nilsson, Daniel Ricklin, Janez Mravljak, Oliver Schwardt, Marko Anderluh
Publié dans: ChemMedChem, 2021, ISSN 1860-7179
Éditeur: 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

Auteurs: 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
Publié dans: Molecules, 2022, Page(s) 1-21, ISSN 1420-3049
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules27061996

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

Auteurs: Kanhaya Lal, Rafael Bermeo, Jonathan Cramer, Francesca Vasile, Beat Ernst, Anne Imberty, Anna Bernardi, Annabelle Varrot, Laura Belvisi
Publié dans: Chemistry - A European Journal, 2021, Page(s) 10341-10348, ISSN 1521-3765
Éditeur: Wiley-VCH Verlag
DOI: 10.1002/chem.202100252

Druggable Allosteric Sites in β-Propeller Lectins

Auteurs: Shanina E, Kuhaudomlarp S, Lal K, Seeberger PH, Imberty A, Rademacher C
Publié dans: Angewandte Chemie International Edition, Numéro 52, 2022, Page(s) 1-9, ISSN 1433-7851
Éditeur: John Wiley & Sons Ltd.
DOI: 10.1002/anie.202109339

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

Auteurs: Cyril Balsollier, Roland J. Pieters, Marko Anderluh
Publié dans: Molecules, Numéro 26/4, 2021, Page(s) 1037, ISSN 1420-3049
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules26041037

DECOYS FOR DISRUPTING CARBOHYDRATE-LECTIN INTERACTIONS

Auteurs: Nives Hribernik
Publié dans: 2021
Éditeur: Universita' degli Studi di Milano

DESIGN, SYNTHESIS AND EVALUATION OF ANTAGONISTS TOWARDS BC2L-C

Auteurs: Rafael Bermeo Malo
Publié dans: 2021
Éditeur: 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

Auteurs: Duca, Margherita; Faculteit Betawetenschappen
Publié dans: "Biochemistry [q-bio.BM]. Université Grenoble Alpes [2020-..]; Universiteit Utrecht (Utrecht, Nederland), 2023. English. ⟨NNT : 2023GRALV028⟩", Numéro 17, 2023
Éditeur: Utrecht University
DOI: 10.33540/1692

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

Auteurs: Kanhaya Lal
Publié dans: 2021
Éditeur: Universita' degli Studi di Milano
DOI: 10.13130/lal-kanhaya_phd2021-12-15

Measuring Carbohydrate-Lectin Interactions : A Guide for Beginners

Auteurs: Margherita Duca
Publié dans: GlycoPedia, Numéro e-chapter, 2020
Éditeur: GlycoPedia (https://www.glycopedia.eu/)

The Fascinating World of SigLec Proteins: A Primer

Auteurs: Benedetta Girardi, Serge Perez
Publié dans: GlycoPedia, Numéro e-chapter, 2022
Éditeur: GlvcoPedia (https://www.glvcopedia.eu/)

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