Exploiting the methylerythritol phosphate pathway as a source of drug targets for novel anti-infectives

Informazioni relative al progetto

MepAnti

ID dell’accordo di sovvenzione: 860816

DOI

10.3030/860816

Progetto chiuso

Data della firma CE 12 Maggio 2020

Data di avvio 1 Aprile 2020

Data di completamento 30 Settembre 2024

Finanziato da

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Costo totale

€ 3 174 724,80

Contributo UE

€ 3 174 724,80

Coordinato da

HELMHOLTZ-ZENTRUM FUR INFEKTIONSFORSCHUNG GMBH
Germany

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Risultati finali

Documents, reports (8)

ESR PhD theses

ESR PhD theses (months 4154)

Scientific publications

Scientific publications (months 1754)

Presentation at conferences

Presentation at conferences (months 1754)

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LinkedINFacebook group

Distribution of network course and workshop material (WP4)

Distribution of network course and workshop material months 8 14 22 28 34 40

Articles in the popular press, press release, interviews in TV and radio shows

Articles in the popular press, press release, interviews in TV and radio shows (months 1754)

Distribution of network course and workshop material (WP5)

Distribution of network course and workshop material (months 8, 14, 22, 28, 34, 40)

Dissemination of new teaching material for secondary and high schools

Other (3)

FameLab competition
PhD degree awarded

PhD degree awarded (months 4154)

ESRs recruitment

ESRs recruitment months 59

Websites, patent fillings, videos etc. (3)

MepAntI website
Patents

Patents (months 1748)

Transfer and licensing of patents

Transfer and licensing of patents (months 1154)

Pubblicazioni

Peer reviewed articles (11)

Structure of Mycobacterium tuberculosis 1-Deoxy-D-Xylulose 5-Phosphate Synthase in Complex with Butylacetylphosphonate

Autori: Victor Oliveira Gawriljuk, Rick Oerlemans, Robin M. Gierse, Riya Jotwani, Anna K. H. Hirsch, Matthew R. Groves
Pubblicato in: Crystals, Numero 13, 2023, Pagina/e 737, ISSN 2073-4352
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cryst13050737

Studying Target–Engagement of Anti-Infectives by Solvent-Induced Protein Precipitation and Quantitative Mass Spectrometry

Autori: Lorenzo Bizzarri, Dominik Steinbrunn, Thibaut Quennesson, Antoine Lacour, Gabriella Ines Bianchino, Patricia Bravo, Philippe Chaignon, Jonas Lohse, Pascal Mäser, Myriam Seemann, Serge Van Calenbergh, Anna K. H. Hirsch, Hannes Hahne
Pubblicato in: ACS Infectious Diseases, 2024, ISSN 2373-8227
Editore: American Chemical Society
DOI: 10.1021/acsinfecdis.4c00417

Targeting <i>Plasmodium falciparum</i> IspD in the Methyl-<scp>d</scp>-erythritol Phosphate Pathway: Urea-Based Compounds with Nanomolar Potency on Target and Low-Micromolar Whole-Cell Activity

Autori: Daan Willocx, Lorenzo Bizzarri, Alaa Alhayek, Deepika Kannan, Patricia Bravo, Boris Illarionov, Katharina Rox, Jonas Lohse, Markus Fischer, Andreas M. Kany, Hannes Hahne, Matthias Rottmann, Matthias Witschel, Audrey Odom John, Mostafa M. Hamed, Eleonora Diamanti, Anna K. H. Hirsch
Pubblicato in: Journal of Medicinal Chemistry, Numero 67, 2024, Pagina/e 17070-17086, ISSN 0022-2623
Editore: American Chemical Society
DOI: 10.1021/acs.jmedchem.4c00212

Target-Directed Dynamic Combinatorial Chemistry Affords Binders of <i>Mycobacterium tuberculosis</i> IspE

Autori: Maria Braun-Cornejo, Camilla Ornago, Vidhisha Sonawane, Jörg Haupenthal, Andreas M. Kany, Eleonora Diamanti, Gwenaëlle Jézéquel, Norbert Reiling, Wulf Blankenfeldt, Peter Maas, Anna K. H. Hirsch
Pubblicato in: ACS Omega, Numero 9, 2024, Pagina/e 38160-38168, ISSN 2470-1343
Editore: American Chemical Society
DOI: 10.1021/acsomega.4c05537

First crystal structures of 1‑deoxy‑d‑xylulose 5‑phosphate synthase (DXPS) from Mycobacterium tuberculosis indicate a distinct mechanism of intermediate stabilization

Autori: Robin M. Gierse, Rick Oerlemans, Eswar R. Reddem, Victor O. Gawriljuk, Alaa Alhayek, Dominik Baitinger, Harald Jakobi, Bernd Laber, Gudrun Lange, Anna K. H. Hirsch, Matthew R. Groves
Pubblicato in: Scientific Reports, 2022, ISSN 2045-2322
Editore: Nature Publishing Group
DOI: 10.1038/s41598-022-11205-9

The Reductive Dehydroxylation Catalyzed by IspH, a Source of Inspiration for the Development of Novel Anti-Infectives

Autori: Hannah Jobelius, Gabriella Ines Bianchino, Franck Borel, Philippe Chaignon, Myriam Seemann
Pubblicato in: Molecules, 2022, ISSN 1420-3049
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules27030708

Targeting the IspD Enzyme in the MEP Pathway: Identification of a Novel Fragment Class

Autori: Eleonora Diamanti, Mostafa M. Hamed, Antoine Lacour, Patricia Bravo,Boris Illarionov, Markus Fischer, Matthias Rottmann, Matthias Witschel,Anna K. H. Hirsch
Pubblicato in: ChemMedChem, 2021, ISSN 1860-7187
Editore: Wiley-VCH
DOI: 10.1002/cmdc.202100679

Synthesis and kinetic evaluation of analogs of (E)-4-amino-3-methylbut-2-en-1-yl diphosphate, a potent inhibitor of the IspH metalloenzyme

Autori: Benoît Eric Petit, Hannah Jobelius, Gabriella Ines Bianchino, Mélina Guérin, Franck Borel, Philippe Chaignon, Myriam Seemann
Pubblicato in: Comptes Rendus. Chimie, Numero 26, 2024, Pagina/e 1-14, ISSN 1878-1543
Editore: Academie des Sciences- Institut de France
DOI: 10.5802/crchim.254

Cryo-EM structure of 1-deoxy-D-xylulose 5-phosphate synthase DXPS from Plasmodium falciparum reveals a distinct N-terminal domain

Autori: Victor O. Gawriljuk, Andre S. Godoy, Rick Oerlemans, Luise A. T. Welker, Anna K. H. Hirsch, Matthew R. Groves
Pubblicato in: Nature Communications, Numero 15, 2024, ISSN 2041-1723
Editore: Nature Publishing Group
DOI: 10.1038/s41467-024-50671-9

Acyloxymethyl and alkoxycarbonyloxymethyl prodrugs of a fosmidomycin surrogate as antimalarial and antibacterial agents

Autori: Charlotte Courtens, Frits van Charante, Thibaut Quennesson, Martijn Risseeuw, Paul Cos, Guy Caljon, Tom Coenye, Serge Van Calenbergh
Pubblicato in: European Journal of Medicinal Chemistry, Numero 245, 2023, Pagina/e 114924, ISSN 0223-5234
Editore: Elsevier BV
DOI: 10.1016/j.ejmech.2022.114924

On the hunt for metalloenzyme inhibitors: Investigating the presence of metal‐coordinating compounds in screening libraries and chemical spaces

Autori: Bruna Schuck, Ruth Brenk
Pubblicato in: Archiv der Pharmazie, Numero 357, 2024, ISSN 0365-6233
Editore: John Wiley & Sons Ltd.
DOI: 10.1002/ardp.202300648