Interdisciplinary Training Network for Validation of Gram-Negative Antibacterial Targets

Livrables

PCDPs

ESR supervisors selected and all PCDPs written

Short course

2-day short course organized on antibacterial targets and validation

SAB

SAB board members appointed

ESR recruitments

Call for ESR applicants published and recruiting course organised

INTEGRATE Outreach Conference

Final conference and outreach event to promote findings of INTEGRATE

Kick-off Meeting

Kick off meeting organized and press announcement released. Supervisory Board will be organised at the same moment.

Gender Equality in Science Course

All ESRs and beneficiaries attend a Gender Equality in Science Course

Website

INTEGRATE website operational

Publications

Inhibition of O -acetylserine sulfhydrylase by fluoroalanine derivatives

Auteurs: Nina Franko, Konstantinos Grammatoglou, Barbara Campanini, Gabriele Costantino, Aigars Jirgensons, Andrea Mozzarelli
Publié dans: Journal of Enzyme Inhibition and Medicinal Chemistry, Numéro 33/1, 2018, Page(s) 1343-1351, ISSN 1475-6366
Éditeur: Taylor & Francis
DOI: 10.1080/14756366.2018.1504040

Discovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand–based drug design

Auteurs: Joana Magalhães, Nina Franko, Giannamaria Annunziato, Martin Welch, Stephen K. Dolan, Agostino Bruno, Andrea Mozzarelli, Stefano Armao, Aigars Jirgensons, Marco Pieroni, Gabriele Costantino, Barbara Campanini
Publié dans: Journal of Enzyme Inhibition and Medicinal Chemistry, Numéro 33/1, 2018, Page(s) 1444-1452, ISSN 1475-6366
Éditeur: Taylor & Francis
DOI: 10.1080/14756366.2018.1512596

Refining the structure−activity relationships of 2-phenylcyclopropane carboxylic acids as inhibitors of O-acetylserine sulfhydrylase isoforms

Auteurs: Joana Magalhães, Nina Franko, Giannamaria Annunziato, Marco Pieroni, Roberto Benoni, Anna Nikitjuka, Andrea Mozzarelli, Stefano Bettati, Anna Karawajczyk, Aigars Jirgensons, Barbara Campanini, Gabriele Costantino
Publié dans: Journal of Enzyme Inhibition and Medicinal Chemistry, Numéro 34/1, 2018, Page(s) 31-43, ISSN 1475-6366
Éditeur: Taylor & Francis
DOI: 10.1080/14756366.2018.1518959

Design and Synthesis of Fsp 3 -Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening

Auteurs: Silvia Stotani, Christoph Lorenz, Matthias Winkler, Federico Medda, Edwige Picazo, Raquel Ortega Martinez, Anna Karawajczyk, Jorge Sanchez-Quesada, Fabrizio Giordanetto
Publié dans: ACS Combinatorial Science, Numéro 18/6, 2016, Page(s) 330-336, ISSN 2156-8952
Éditeur: American Chemical Society
DOI: 10.1021/acscombsci.6b00005

A Versatile Strategy for the Synthesis of 4,5-Dihydroxy-2,3-Pentanedione (DPD) and Related Compounds as Potential Modulators of Bacterial Quorum Sensing

Auteurs: Silvia Stotani, Viviana Gatta, Federico Medda, Mohan Padmanaban, Anna Karawajczyk, Päivi Tammela, Fabrizio Giordanetto, Dimitrios Tzalis, Simona Collina
Publié dans: Molecules, Numéro 23/10, 2018, Page(s) 2545, ISSN 1420-3049
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules23102545

Structure-Based Virtual Screening of LsrK Kinase Inhibitors to Target Quorum Sensing

Auteurs: Prasanthi Medarametla, Viviana Gatta, Tommi Kajander, Tuomo Laitinen, Päivi Tammela, Antti Poso
Publié dans: ChemMedChem, Numéro 13/22, 2018, Page(s) 2400-2407, ISSN 1860-7179
Éditeur: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.201800548

Structural and Functional Characterization of Malate Synthase G from Opportunistic Pathogen Pseudomonas aeruginosa

Auteurs: Alyssa C. McVey, Prasanthi Medarametla, Xavier Chee, Sean Bartlett, Antti Poso, David R. Spring, Taufiq Rahman, Martin Welch
Publié dans: Biochemistry, Numéro 56/41, 2017, Page(s) 5539-5549, ISSN 0006-2960
Éditeur: American Chemical Society
DOI: 10.1021/acs.biochem.7b00852

Design, synthesis, and biological evaluation of 1-ethyl-3-(thiazol-2-yl)urea derivatives as Escherichia coli DNA gyrase inhibitors

Auteurs: Tihomir Tomašič, Michaela Barančoková, Nace Zidar, Janez Ilaš, Päivi Tammela, Danijel Kikelj
Publié dans: Archiv der Pharmazie, Numéro 351/1, 2018, Page(s) 1700333, ISSN 0365-6233
Éditeur: John Wiley & Sons Ltd.
DOI: 10.1002/ardp.201700333

Synthesis and Evaluation of N -Phenylpyrrolamides as DNA Gyrase B Inhibitors

Auteurs: Martina Durcik, Päivi Tammela, Michaela Barančoková, Tihomir Tomašič, Janez Ilaš, Danijel Kikelj, Nace Zidar
Publié dans: ChemMedChem, Numéro 13/2, 2018, Page(s) 186-198, ISSN 1860-7179
Éditeur: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.201700549

Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase inhibitors

Auteurs: Žiga Jakopin, Janez Ilaš, Michaela Barančoková, Matjaž Brvar, Päivi Tammela, Marija Sollner Dolenc, Tihomir Tomašič, Danijel Kikelj
Publié dans: European Journal of Medicinal Chemistry, Numéro 130, 2017, Page(s) 171-184, ISSN 0223-5234
Éditeur: Elsevier BV
DOI: 10.1016/j.ejmech.2017.02.046

Recent progress in the discovery and development of DNA gyrase B inhibitors

Auteurs: Michaela Barančoková, Danijel Kikelj, Janez Ilaš
Publié dans: Future Medicinal Chemistry, Numéro 10/10, 2018, Page(s) 1207-1227, ISSN 1756-8919
Éditeur: Future Science Ltd.
DOI: 10.4155/fmc-2017-0257

Cyclopropane-1,2-dicarboxylic acids as new tools for the biophysical investigation of O -acetylserine sulfhydrylases by fluorimetric methods and saturation transfer difference (STD) NMR

Auteurs: Giannamaria Annunziato, Marco Pieroni, Roberto Benoni, Barbara Campanini, Thelma A. Pertinhez, Chiara Pecchini, Agostino Bruno, Joana Magalhães, Stefano Bettati, Nina Franko, Andrea Mozzarelli, Gabriele Costantino
Publié dans: Journal of Enzyme Inhibition and Medicinal Chemistry, Numéro 31/sup4, 2016, Page(s) 78-87, ISSN 1475-6366
Éditeur: Taylor & Francis
DOI: 10.1080/14756366.2016.1218486

Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors.

Auteurs: Tomašič T1, Mirt M2, Barančoková M2, Ilaš J2, Zidar N2, Tammela P3, Kikelj D2
Publié dans: Bioorganic & Medicinal Chemistry, Numéro Vol. 25, Iss. 1 (2017), 2017, Page(s) 338-349, ISSN 0968-0896
Éditeur: Pergamon Press Ltd.
DOI: 10.1016/j.bmc.2016.10.038

Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors

Auteurs: Gjorgjieva M1, Tomašič T1, Barančokova M1, Katsamakas S1,2, Ilaš J1, Tammela P3, Peterlin Mašič L1, Kikelj D1.
Publié dans: Journal of Medicinal Chemistry, Numéro Vol. 59, iss. 19 (2016), 2016, Page(s) 8941-8954, ISSN 0022-2623
Éditeur: American Chemical Society
DOI: 10.1021/acs.jmedchem.6b00864

α-Amino Diphenyl Phosphonates as Novel Inhibitors of Escherichia coli ClpP Protease

Auteurs: Carlos Moreno-Cinos, Elisa Sassetti, Irene G. Salado, Gesa Witt, Siham Benramdane, Laura Reinhardt, Cristina D. Cruz, Jurgen Joossens, Pieter Van der Veken, Heike Brötz-Oesterhelt, Päivi Tammela, Mathias Winterhalter, Philip Gribbon, Björn Windshügel, Koen Augustyns
Publié dans: Journal of Medicinal Chemistry, Numéro 62/2, 2019, Page(s) 774-797, ISSN 0022-2623
Éditeur: American Chemical Society
DOI: 10.1021/acs.jmedchem.8b01466

Integration of Enhanced Sampling Methods with Saturation Transfer Difference Experiments to Identify Protein Druggable Pockets

Auteurs: Joana Magalhães, Giannamaria Annunziato, Nina Franko, Marco Pieroni, Barbara Campanini, Agostino Bruno, Gabriele Costantino
Publié dans: Journal of Chemical Information and Modeling, Numéro 58/3, 2018, Page(s) 710-723, ISSN 1549-9596
Éditeur: American Chemical Society
DOI: 10.1021/acs.jcim.7b00733

Structural and functional characterisation of the glyoxylate shunt enzymes from Pseudomonas aeruginosa - ORAL CONFERENCE TALK

Auteurs: Alyssa McVey, Sean Bartlett, Martin Welch
Publié dans: 2017
Éditeur: Microbiology Society Meeting

Targeting the glyoxylate shunt for antibacterial intervention in Pseudomonas aeruginosa

Auteurs: Alyssa McVey, Sean Bartlett and Martin Welch
Publié dans: 2017
Éditeur: Pseudomonas conference 2017

Enzyme inhibition as a new strategy to overcome Multidrug Resistant Bacteria

Auteurs: Joana Magalhães, Giannamaria Annunziato, Marco Pieroni, Nina Franko, Barbara Campanini, Andrea Mozzarelli, Vanesa Estevez, Antonio Felici, and Gabriele Costantino
Publié dans: 2016
Éditeur: XXIV EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2016)

Discovery of novel Gyrase B and GyraseB/Topoisomerase IV (ParE) dual Inhibitors with in vitro antibacterial activity

Auteurs: Michaela Barančoková, Janez Ilaš, Marina Gjorgjieva, Tihomir Tomašič, Päivi Tammela, Vanesa Garrido, Antonio Felici, and Danijel Kikelj
Publié dans: 2016
Éditeur: 6th Meeting of the Paul Ehrlich MedChem Euro-PhD Network, Budapest, Hungary - 18-20 November 2016

Design, synthesis and in vitro profiling of novel inhibitors of Pseudomonas aeruginosa MvfR

Auteurs: A Felici, M Antolini, M. Negri, V. Garrido Estevez, R Zahler, L Rahme, M Pucci, Aldo Feriani, and Daniele Andreotti
Publié dans: 2017
Éditeur: European Clinical Microbiology Society

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