Interdisciplinary Training Network for Validation of Gram-Negative Antibacterial Targets

Risultati finali

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

Pubblicazioni

Inhibition of O -acetylserine sulfhydrylase by fluoroalanine derivatives

Autori: Nina Franko, Konstantinos Grammatoglou, Barbara Campanini, Gabriele Costantino, Aigars Jirgensons, Andrea Mozzarelli
Pubblicato in: Journal of Enzyme Inhibition and Medicinal Chemistry, Numero 33/1, 2018, Pagina/e 1343-1351, ISSN 1475-6366
Editore: 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

Autori: 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
Pubblicato in: Journal of Enzyme Inhibition and Medicinal Chemistry, Numero 33/1, 2018, Pagina/e 1444-1452, ISSN 1475-6366
Editore: 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

Autori: Joana Magalhães, Nina Franko, Giannamaria Annunziato, Marco Pieroni, Roberto Benoni, Anna Nikitjuka, Andrea Mozzarelli, Stefano Bettati, Anna Karawajczyk, Aigars Jirgensons, Barbara Campanini, Gabriele Costantino
Pubblicato in: Journal of Enzyme Inhibition and Medicinal Chemistry, Numero 34/1, 2018, Pagina/e 31-43, ISSN 1475-6366
Editore: Taylor & Francis
DOI: 10.1080/14756366.2018.1518959

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

Autori: Silvia Stotani, Christoph Lorenz, Matthias Winkler, Federico Medda, Edwige Picazo, Raquel Ortega Martinez, Anna Karawajczyk, Jorge Sanchez-Quesada, Fabrizio Giordanetto
Pubblicato in: ACS Combinatorial Science, Numero 18/6, 2016, Pagina/e 330-336, ISSN 2156-8952
Editore: 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

Autori: Silvia Stotani, Viviana Gatta, Federico Medda, Mohan Padmanaban, Anna Karawajczyk, Päivi Tammela, Fabrizio Giordanetto, Dimitrios Tzalis, Simona Collina
Pubblicato in: Molecules, Numero 23/10, 2018, Pagina/e 2545, ISSN 1420-3049
Editore: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules23102545

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

Autori: Prasanthi Medarametla, Viviana Gatta, Tommi Kajander, Tuomo Laitinen, Päivi Tammela, Antti Poso
Pubblicato in: ChemMedChem, Numero 13/22, 2018, Pagina/e 2400-2407, ISSN 1860-7179
Editore: 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

Autori: Alyssa C. McVey, Prasanthi Medarametla, Xavier Chee, Sean Bartlett, Antti Poso, David R. Spring, Taufiq Rahman, Martin Welch
Pubblicato in: Biochemistry, Numero 56/41, 2017, Pagina/e 5539-5549, ISSN 0006-2960
Editore: 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

Autori: Tihomir Tomašič, Michaela Barančoková, Nace Zidar, Janez Ilaš, Päivi Tammela, Danijel Kikelj
Pubblicato in: Archiv der Pharmazie, Numero 351/1, 2018, Pagina/e 1700333, ISSN 0365-6233
Editore: John Wiley & Sons Ltd.
DOI: 10.1002/ardp.201700333

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

Autori: Martina Durcik, Päivi Tammela, Michaela Barančoková, Tihomir Tomašič, Janez Ilaš, Danijel Kikelj, Nace Zidar
Pubblicato in: ChemMedChem, Numero 13/2, 2018, Pagina/e 186-198, ISSN 1860-7179
Editore: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.201700549

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

Autori: Žiga Jakopin, Janez Ilaš, Michaela Barančoková, Matjaž Brvar, Päivi Tammela, Marija Sollner Dolenc, Tihomir Tomašič, Danijel Kikelj
Pubblicato in: European Journal of Medicinal Chemistry, Numero 130, 2017, Pagina/e 171-184, ISSN 0223-5234
Editore: Elsevier BV
DOI: 10.1016/j.ejmech.2017.02.046

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

Autori: Michaela Barančoková, Danijel Kikelj, Janez Ilaš
Pubblicato in: Future Medicinal Chemistry, Numero 10/10, 2018, Pagina/e 1207-1227, ISSN 1756-8919
Editore: 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

Autori: 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
Pubblicato in: Journal of Enzyme Inhibition and Medicinal Chemistry, Numero 31/sup4, 2016, Pagina/e 78-87, ISSN 1475-6366
Editore: 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.

Autori: Tomašič T1, Mirt M2, Barančoková M2, Ilaš J2, Zidar N2, Tammela P3, Kikelj D2
Pubblicato in: Bioorganic & Medicinal Chemistry, Numero Vol. 25, Iss. 1 (2017), 2017, Pagina/e 338-349, ISSN 0968-0896
Editore: Pergamon Press Ltd.
DOI: 10.1016/j.bmc.2016.10.038

Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors

Autori: Gjorgjieva M1, Tomašič T1, Barančokova M1, Katsamakas S1,2, Ilaš J1, Tammela P3, Peterlin Mašič L1, Kikelj D1.
Pubblicato in: Journal of Medicinal Chemistry, Numero Vol. 59, iss. 19 (2016), 2016, Pagina/e 8941-8954, ISSN 0022-2623
Editore: American Chemical Society
DOI: 10.1021/acs.jmedchem.6b00864

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

Autori: 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
Pubblicato in: Journal of Medicinal Chemistry, Numero 62/2, 2019, Pagina/e 774-797, ISSN 0022-2623
Editore: American Chemical Society
DOI: 10.1021/acs.jmedchem.8b01466

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

Autori: Joana Magalhães, Giannamaria Annunziato, Nina Franko, Marco Pieroni, Barbara Campanini, Agostino Bruno, Gabriele Costantino
Pubblicato in: Journal of Chemical Information and Modeling, Numero 58/3, 2018, Pagina/e 710-723, ISSN 1549-9596
Editore: American Chemical Society
DOI: 10.1021/acs.jcim.7b00733

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

Autori: Alyssa McVey, Sean Bartlett, Martin Welch
Pubblicato in: 2017
Editore: Microbiology Society Meeting

Targeting the glyoxylate shunt for antibacterial intervention in Pseudomonas aeruginosa

Autori: Alyssa McVey, Sean Bartlett and Martin Welch
Pubblicato in: 2017
Editore: Pseudomonas conference 2017

Enzyme inhibition as a new strategy to overcome Multidrug Resistant Bacteria

Autori: Joana Magalhães, Giannamaria Annunziato, Marco Pieroni, Nina Franko, Barbara Campanini, Andrea Mozzarelli, Vanesa Estevez, Antonio Felici, and Gabriele Costantino
Pubblicato in: 2016
Editore: 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

Autori: Michaela Barančoková, Janez Ilaš, Marina Gjorgjieva, Tihomir Tomašič, Päivi Tammela, Vanesa Garrido, Antonio Felici, and Danijel Kikelj
Pubblicato in: 2016
Editore: 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

Autori: A Felici, M Antolini, M. Negri, V. Garrido Estevez, R Zahler, L Rahme, M Pucci, Aldo Feriani, and Daniele Andreotti
Pubblicato in: 2017
Editore: European Clinical Microbiology Society

Risultati finali

Pubblicazioni

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