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Interdisciplinary Training Network for Validation of Gram-Negative Antibacterial Targets

Deliverables

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

Publications

Inhibition of O -acetylserine sulfhydrylase by fluoroalanine derivatives

Author(s): Nina Franko, Konstantinos Grammatoglou, Barbara Campanini, Gabriele Costantino, Aigars Jirgensons, Andrea Mozzarelli
Published in: Journal of Enzyme Inhibition and Medicinal Chemistry, Issue 33/1, 2018, Page(s) 1343-1351, ISSN 1475-6366
DOI: 10.1080/14756366.2018.1504040

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

Author(s): 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
Published in: Journal of Enzyme Inhibition and Medicinal Chemistry, Issue 33/1, 2018, Page(s) 1444-1452, ISSN 1475-6366
DOI: 10.1080/14756366.2018.1512596

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

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

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

Author(s): Silvia Stotani, Christoph Lorenz, Matthias Winkler, Federico Medda, Edwige Picazo, Raquel Ortega Martinez, Anna Karawajczyk, Jorge Sanchez-Quesada, Fabrizio Giordanetto
Published in: ACS Combinatorial Science, Issue 18/6, 2016, Page(s) 330-336, ISSN 2156-8952
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

Author(s): Silvia Stotani, Viviana Gatta, Federico Medda, Mohan Padmanaban, Anna Karawajczyk, Päivi Tammela, Fabrizio Giordanetto, Dimitrios Tzalis, Simona Collina
Published in: Molecules, Issue 23/10, 2018, Page(s) 2545, ISSN 1420-3049
DOI: 10.3390/molecules23102545

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

Author(s): Prasanthi Medarametla, Viviana Gatta, Tommi Kajander, Tuomo Laitinen, Päivi Tammela, Antti Poso
Published in: ChemMedChem, Issue 13/22, 2018, Page(s) 2400-2407, ISSN 1860-7179
DOI: 10.1002/cmdc.201800548

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

Author(s): Alyssa C. McVey, Prasanthi Medarametla, Xavier Chee, Sean Bartlett, Antti Poso, David R. Spring, Taufiq Rahman, Martin Welch
Published in: Biochemistry, Issue 56/41, 2017, Page(s) 5539-5549, ISSN 0006-2960
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

Author(s): Tihomir Tomašič, Michaela Barančoková, Nace Zidar, Janez Ilaš, Päivi Tammela, Danijel Kikelj
Published in: Archiv der Pharmazie, Issue 351/1, 2018, Page(s) 1700333, ISSN 0365-6233
DOI: 10.1002/ardp.201700333

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

Author(s): Martina Durcik, Päivi Tammela, Michaela Barančoková, Tihomir Tomašič, Janez Ilaš, Danijel Kikelj, Nace Zidar
Published in: ChemMedChem, Issue 13/2, 2018, Page(s) 186-198, ISSN 1860-7179
DOI: 10.1002/cmdc.201700549

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

Author(s): Žiga Jakopin, Janez Ilaš, Michaela Barančoková, Matjaž Brvar, Päivi Tammela, Marija Sollner Dolenc, Tihomir Tomašič, Danijel Kikelj
Published in: European Journal of Medicinal Chemistry, Issue 130, 2017, Page(s) 171-184, ISSN 0223-5234
DOI: 10.1016/j.ejmech.2017.02.046

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

Author(s): Michaela Barančoková, Danijel Kikelj, Janez Ilaš
Published in: Future Medicinal Chemistry, Issue 10/10, 2018, Page(s) 1207-1227, ISSN 1756-8919
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

Author(s): 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
Published in: Journal of Enzyme Inhibition and Medicinal Chemistry, Issue 31/sup4, 2016, Page(s) 78-87, ISSN 1475-6366
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.

Author(s): Tomašič T1, Mirt M2, Barančoková M2, Ilaš J2, Zidar N2, Tammela P3, Kikelj D2
Published in: Bioorganic & Medicinal Chemistry, Issue Vol. 25, Iss. 1 (2017), 2017, Page(s) 338-349, ISSN 0968-0896
DOI: 10.1016/j.bmc.2016.10.038

Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors

Author(s): Gjorgjieva M1, Tomašič T1, Barančokova M1, Katsamakas S1,2, Ilaš J1, Tammela P3, Peterlin Mašič L1, Kikelj D1.
Published in: Journal of Medicinal Chemistry, Issue Vol. 59, iss. 19 (2016), 2016, Page(s) 8941-8954, ISSN 0022-2623
DOI: 10.1021/acs.jmedchem.6b00864

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

Author(s): 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
Published in: Journal of Medicinal Chemistry, Issue 62/2, 2019, Page(s) 774-797, ISSN 0022-2623
DOI: 10.1021/acs.jmedchem.8b01466

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

Author(s): Joana Magalhães, Giannamaria Annunziato, Nina Franko, Marco Pieroni, Barbara Campanini, Agostino Bruno, Gabriele Costantino
Published in: Journal of Chemical Information and Modeling, Issue 58/3, 2018, Page(s) 710-723, ISSN 1549-9596
DOI: 10.1021/acs.jcim.7b00733

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

Author(s): Alyssa McVey, Sean Bartlett, Martin Welch
Published in: 2017

Targeting the glyoxylate shunt for antibacterial intervention in Pseudomonas aeruginosa

Author(s): Alyssa McVey, Sean Bartlett and Martin Welch
Published in: 2017

Enzyme inhibition as a new strategy to overcome Multidrug Resistant Bacteria

Author(s): Joana Magalhães, Giannamaria Annunziato, Marco Pieroni, Nina Franko, Barbara Campanini, Andrea Mozzarelli, Vanesa Estevez, Antonio Felici, and Gabriele Costantino
Published in: 2016

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

Author(s): Michaela Barančoková, Janez Ilaš, Marina Gjorgjieva, Tihomir Tomašič, Päivi Tammela, Vanesa Garrido, Antonio Felici, and Danijel Kikelj
Published in: 2016

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

Author(s): A Felici, M Antolini, M. Negri, V. Garrido Estevez, R Zahler, L Rahme, M Pucci, Aldo Feriani, and Daniele Andreotti
Published in: 2017

Datasets