Indentification and optimisation of novel anti-infective agents using multiple hit-identification strategies

Informazioni relative al progetto

NovAnI

ID dell’accordo di sovvenzione: 757913

DOI

10.3030/757913

Progetto chiuso

Data della firma CE 12 Gennaio 2018

Data di avvio 1 Febbraio 2018

Data di completamento 31 Gennaio 2023

Finanziato da

• EXCELLENT SCIENCE - European Research Council (ERC)

Costo totale

€ 1 499 367,00

Contributo UE

€ 1 499 367,00

Coordinato da

HELMHOLTZ-ZENTRUM FUR INFEKTIONSFORSCHUNG GMBH
Germany

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 .

Pubblicazioni

Peer reviewed articles (21)

Evaluation of Bacterial RNA Polymerase Inhibitors in a Staphylococcus aureus -Based Wound Infection Model in SKH1 Mice

Autori: Jörg Haupenthal, Yannik Kautz, Walid A. M. Elgaher, Linda Pätzold, Teresa Röhrig, Matthias W. Laschke, Thomas Tschernig, Anna K. H. Hirsch, Vadim Molodtsov, Katsuhiko S. Murakami, Rolf W. Hartmann, Markus Bischoff
Pubblicato in: ACS Infectious Diseases, Numero 6/10, 2020, Pagina/e 2573-2581, ISSN 2373-8227
Editore: American Chemical Society
DOI: 10.1021/acsinfecdis.0c00034

Protein‐Templated Hit Identification through an Ugi Four‐Component Reaction

Autori: Federica Mancini, M. Yagiz Unver, Walid A. M. Elgaher, Varsha R. Jumde, Alaa Alhayek, Peer Lukat, Jennifer Herrmann, Martin D. Witte, Matthias Köck, Wulf Blankenfeldt, Rolf Müller, Anna K. H. Hirsch
Pubblicato in: Chemistry – A European Journal, 2020, ISSN 0947-6539
Editore: John Wiley & Sons Ltd.
DOI: 10.1002/chem.202002250

From Wood to Tetrahydro-2-benzazepines in Three Waste-Free Steps: Modular Synthesis of Biologically Active Lignin-Derived Scaffolds

Autori: Saravanakumar Elangovan, Anastasiia Afanasenko, Jörg Haupenthal, Zhuohua Sun, Yongzhuang Liu, Anna K. H. Hirsch, Katalin Barta
Pubblicato in: ACS Central Science, Numero 5/10, 2019, Pagina/e 1707-1716, ISSN 2374-7943
Editore: American Chemical Society
DOI: 10.1021/acscentsci.9b00781

Identification of RAD51–BRCA2 Inhibitors Using <i>N</i>-Acylhydrazone-Based Dynamic Combinatorial Chemistry

Autori: Greta Bagnolini; Beatrice Balboni; Fabrizio Schipani; Dario Gioia; Marina Veronesi; Francesca De Franco; Cansu Kaya; Ravindra P. Jumde; Jose Antonio Ortega; Stefania Girotto; Anna K. H. Hirsch; Marinella Roberti; Andrea Cavalli
Pubblicato in: ACS Med Chem Letters, Numero 1, 2022, ISSN 1948-5875
Editore: American Chemical Society
DOI: 10.1021/acsmedchemlett.2c00063

Discovery of Small-Molecule Stabilizers of 14-3-3 Protein–Protein Interactions via Dynamic Combinatorial Chemistry

Autori: Alwin M. Hartman, Walid A. M. Elgaher, Nathalie Hertrich, Sebastian A. Andrei, Christian Ottmann, Anna K. H. Hirsch
Pubblicato in: ACS Medicinal Chemistry Letters, Numero 11/5, 2020, Pagina/e 1041-1046, ISSN 1948-5875
Editore: American Chemical Society
DOI: 10.1021/acsmedchemlett.9b00541

Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach

Autori: Markella Konstantinidou, Francesca Magari, Fandi Sutanto, Jörg Haupenthal, Varsha R. Jumde, M. Yagiz Ünver, Andreas Heine, Carlos Jamie Camacho, Anna K. H. Hirsch, Gerhard Klebe, Alexander Dömling
Pubblicato in: ChemMedChem, Numero 15/8, 2020, Pagina/e 680-684, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202000024

Design and Synthesis of Bioisosteres of Acylhydrazones as Stable Inhibitors of the Aspartic Protease Endothiapepsin

Autori: Varsha R. Jumde, Milon Mondal, Robin M. Gierse, M. Yagiz Unver, Francesca Magari, Roos C. W. van Lier, Andreas Heine, Gerhard Klebe, Anna K. H. Hirsch
Pubblicato in: ChemMedChem, Numero 13/21, 2018, Pagina/e 2266-2270, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.201800446

Potential Dental Biofilm Inhibitors: Dynamic Combinatorial Chemistry Affords Sugar‐Based Molecules that Target Bacterial Glucosyltransferase

Autori: Alwin M. Hartman, Varsha R. Jumde, Walid A. M. Elgaher, Evelien M. Te Poele, Lubbert Dijkhuizen, Anna K. H. Hirsch
Pubblicato in: ChemMedChem, 2020, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202000222

N -Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting Pseudomonas aeruginosa Elastase and Clostridium Collagenases

Autori: Jelena Konstantinović, Samir Yahiaoui, Alaa Alhayek, Jörg Haupenthal, Esther Schönauer, Anastasia Andreas, Andreas M. Kany, Rolf Müller, Jesko Koehnke, Fabian K. Berger, Markus Bischoff, Rolf W. Hartmann, Hans Brandstetter, Anna K. H. Hirsch
Pubblicato in: Journal of Medicinal Chemistry, Numero 63/15, 2020, Pagina/e 8359-8368, ISSN 0022-2623
Editore: American Chemical Society
DOI: 10.1021/acs.jmedchem.0c00584

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, Numero 6, 2022, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202100679

"Phosphonate as a Stable Zinc-Binding Group for ""Pathoblocker"" Inhibitors of Clostridial Collagenase H (ColH)."

Autori: Katrin Voos; Esther Schönauer; Alaa Alhayek; Jörg Haupenthal; Anastasia Andreas; Rolf Müller; Rolf W. Hartmann; Hans Brandstetter; Anna K. H. Hirsch; Christian Ducho
Pubblicato in: Chemmedchem, Numero 1, 2021, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202000994

Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases

Autori: Alaa Alhayek; Ahmed S. Abdelsamie; Esther Schönauer; Virgyl Camberlein; Evelyn Hutterer; Gernot Posselt; Jamil Serwanja; Constantin Blöchl; Christian G. Huber; Jörg Haupenthal; Hans Brandstetter; Silja Wessler; Anna K. H. Hirsch
Pubblicato in: J Med Chem, Numero 1, 2022, ISSN 0022-2623
Editore: American Chemical Society
DOI: 10.1021/acs.jmedchem.2c00785

Structure-Guided Optimization of Small-Molecule Folate Uptake Inhibitors Targeting the Energy-Coupling Factor Transporters

Autori: Alexander F. Kiefer, Spyridon Bousis, Mostafa M. Hamed, Eleonora Diamanti, Jörg Haupenthal, Anna K.H. Hirsch
Pubblicato in: Journal of Medicinal Chemistry, 2022, ISSN 0022-2623
Editore: American Chemical Society
DOI: 10.1021/acs.jmedchem.1c02114

Discovery of novel drug-like antitubercular hits targeting the MEP pathway enzyme DXPS by strategic application of ligand-based virtual screening.

Autori: Di Zhu; Sandra Johannsen; Tiziana Masini; Céline Simonin; Jörg Haupenthal; Boris Illarionov; Anastasia Andreas; Mahendra Awale; Robin M. Gierse; Tridia van der Laan; Ramon van der Vlag; Rita Nasti; Mael Poizat; Eric Buhler; Norbert Reiling; Rolf Müller; Markus Fischer; Jean-Louis Reymond; Anna K. H. Hirsch
Pubblicato in: Chemical Science, Numero 1, 2022, ISSN 2041-6539
Editore: Cambridge: Royal Society of Chemistry
DOI: 10.48350/174448

Flotillin-mediated membrane fluidity controls peptidoglycan synthesis and MreB movement.

Autori: Aleksandra Zielinska, Abigail Savietto, Anabela de Sousa Borges, Denis Martinez, Melanie Berbon, Joel R Roelofsen, Alwin M Hartman, Rinse de Boer, Ida J Van der Klei, Anna KH Hirsch, Birgit Habenstein, Marc Bramkamp, Dirk-Jan Scheffers
Pubblicato in: eLife, 2020, ISSN 2050-084X
Editore: eLife Sciences Publications
DOI: 10.7554/elife.57179

Hit-optimization using target-directed dynamic combinatorial chemistry: development of inhibitors of the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase

Autori: Ravindra P. Jumde, Melissa Guardigni, Robin M. Gierse, Alaa Alhayek, Di Zhu, Zhoor Hamid, Sandra Johannsen, Walid A. M. Elgaher, Philipp J. Neusens, Christian Nehls, Jörg Haupenthal, Norbert Reiling Anna K. H. Hirsch
Pubblicato in: Chemical Science, 2021, ISSN 2041-6520
Editore: Royal Society of Chemistry
DOI: 10.1039/d1sc00330e

Bacteriomimetic Liposomes Improve Antibiotic Activity of a Novel Energy-Coupling Factor Transporter Inhibitor

Autori: Menka Drost, Eleonora Diamanti, Kathrin Fuhrmann, Adriely Goes,Atanaz Shams, Jörg Haupenthal, Marcus Koch, Anna K. H. Hirsch, Gregor Fuhrmann
Pubblicato in: Pharmaceutics, 2022, ISSN 1999-4923
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/pharmaceutics14010004

Spray-drying of inhalable, multifunctional formulations for the treatment of biofilms formed in cystic fibrosis

Autori: Nashrawan Lababidi, Eric Ofosu Kissi, Walid A.M. Elgaher, Valentin Sigal, Jörg Haupenthal, Bianca C. Schwarz, Anna K.H. Hirsch, Thomas Rades, Marc Schneider
Pubblicato in: Journal of Controlled Release, Numero 314, 2019, Pagina/e 62-71, ISSN 0168-3659
Editore: Elsevier BV
DOI: 10.1016/j.jconrel.2019.10.038

Energy-Coupling Factor Transporters as Novel Antimicrobial Targets

Autori: Spyridon Bousis, Inda Setyawati, Eleonora Diamanti, Dirk J. Slotboom, Anna K. H. Hirsch
Pubblicato in: Advanced Therapeutics, Numero 2/2, 2019, Pagina/e 1800066, ISSN 2366-3987
Editore: WILEY-VCH
DOI: 10.1002/adtp.201800066

An Efficient Way to Screen Inhibitors of Energy-Coupling Factor (ECF) Transporters in a Bacterial Uptake Assay.

Autori: Spyridon Bousis; Steffen Winkler; Jörg Haupenthal; Francesco Fulco; Eleonora Diamanti; Anna K. H. Hirsch
Pubblicato in: International Journal of Molecular Sciences, Numero 3, 2022, ISSN 1422-0067
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms23052637

A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d -galactose pentaacetate

Autori: Eva Zahorska, Sakonwan Kuhaudomlarp, Saverio Minervini, Sultaan Yousaf, Martin Lepsik, Thorsten Kinsinger, Anna K. H. Hirsch, Anne Imberty, Alexander Titz
Pubblicato in: Chemical Communications, Numero 56/62, 2020, Pagina/e 8822-8825, ISSN 1359-7345
Editore: Royal Society of Chemistry
DOI: 10.1039/d0cc03490h