NABARSI

New AntiBacterials with Inhibitory activity on Aminoacyl-tRNA Synthetases

Coordinatore	ERASMUS UNIVERSITAIR MEDISCH CENTRUM ROTTERDAM    more  Organization address address: 's Gravendijkwal 230 city: ROTTERDAM postcode: 3015CE contact info Titolo: Dr. Nome: John Cognome: Hays Email: send email Telefono: +3101070 32177 Fax: +3101070 36875
Nazionalità Coordinatore	Netherlands [NL]
Totale costo	5˙389˙151 €
EC contributo	4˙102˙157 €
Programma	FP7-HEALTH Specific Programme "Cooperation": Health
Code Call	FP7-HEALTH-2013-INNOVATION-2
Funding Scheme	CP-FP
Anno di inizio	2013
Periodo (anno-mese-giorno)	2013-06-01   -   2016-05-31

 Partecipanti

#	participant	country	role	EC contrib. [€]
1	ERASMUS UNIVERSITAIR MEDISCH CENTRUM ROTTERDAM  Organization address address: 's Gravendijkwal 230 city: ROTTERDAM postcode: 3015CE contact info Titolo: Dr. Nome: John Cognome: Hays Email: send email Telefono: +3101070 32177 Fax: +3101070 36875	NL (ROTTERDAM)	coordinator	577˙819.20
2	OMNIA MOLECULAR S.L.  Organization address address: Calle JOSEP SAMITIER - PARC CIENTIFIC DE BARCELONA 1-5 city: BARCELONA postcode: 8028 contact info Titolo: Dr. Nome: Lluis Cognome: Ribas De Pouplana Email: send email Telefono: +34 934034868 Fax: +34 934034970	ES (BARCELONA)	participant	1˙042˙132.30
3	InhibOx Limited  Organization address address: CORNHILL 24 city: LONDON postcode: EC3V 3ND contact info Titolo: Dr. Nome: Paul Cognome: Finn Email: send email Telefono: +44 1865 261468	UK (LONDON)	participant	1˙013˙501.00
4	LATVIJAS ORGANISKAS SINTEZES INSTITUTS  Organization address address: AIZKRAUKLES 21 city: RIGA postcode: 1006 contact info Titolo: Ms. Nome: Dace Cognome: Karkle Email: send email Telefono: +371 67014803	LV (RIGA)	participant	848˙025.00
5	UNIVERSITY OF LEEDS  Organization address address: WOODHOUSE LANE city: LEEDS postcode: LS2 9JT contact info Titolo: Mr. Nome: Martin Cognome: Hamilton Email: send email Telefono: +44 113 3434090	UK (LEEDS)	participant	620˙680.00

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 Obiettivo del progetto (Objective)

'The NABARSI consortium will develop a cutting-edge drug discovery project to increase the antibacterial pipeline. The main goal of NABARSI is to find new chemical entities (NCEs) with antibacterial efficacy in animal models of multi-drug resistant (MDR) bacterial infection and to exploit the results through obtaining a co-development with industry. The NABARSI consortium consists of 5 partners: Omnia Molecular (Omnia, SME; Spain). InhibOx (SME, UK). Latvian Institute of Organic Synthesis (LIOS, Latvia), Leeds University (Leeds, UK) and Erasmus Medical Centre (ErasmusMC, The Netherlands - Coordinator). Antibacterial activity will be achieved through inhibition of essential aminoacyl-tRNA synthetases (aaRS). Individual aaRS are highly conserved across bacteria, enabling the discovery of broad-spectrum antibacterials. To reduce the likelihood of resistance, NABARSI will look for NCEs with inhibitory activity against multiple aaRS enzymes. InhibOx and LIOS will design NCEs by rational and fragment based drug discovery methods followed by synthetic structure optimization. To increase chemical diversity, virtual screening of large (>100 M) compound libraries available at InhibOx will be performed. Limitations of previous aaRS inhibitors will be overcome by novel approaches such as the In Omnia assay: activity of the compounds on pathogenic aaRS enzyme is measured inside a human cell, allowing rejection of compounds acting through human aaRS and identifying compounds that cross biological membranes. The expertise of Leeds in mode of action studies will be used at an early stage. Activity of the NCEs on clinical isolates of MDR strains available at ErasmusMC will be assessed. Resistance appearance frequency and mechanisms will also be assessed early by selection and characterization of resistant mutants by ErasmusMC and Leeds. A co-development agreement with pharmaceutical companies will be intensively sought with the aim of exploiting the NCEs upon finalisation of NABARSI.'