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LONDON, United Kingdom

Grant
Agency: Cordis | Branch: FP7 | Program: CP-FP | Phase: HEALTH.2013.2.3.1-1 | Award Amount: 5.39M | Year: 2013

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.


Grant
Agency: Cordis | Branch: FP7 | Program: MC-ITN | Phase: FP7-PEOPLE-ITN-2008 | Award Amount: 2.08M | Year: 2009

Researchers who aspire to work in drug discovery need to adapt to constantly changing technology and be able to harness new tools both to ask and to answer pertinent scientific questions. Structural biology was going to rationalize drug design. Next, combinatorial chemistry was to be the industrial panacea, only to be superseded by high-throughput screening of chemical libraries. Technologies such as molecular cell biology, in silico modelling, genetic engineering and NMR, are now also part of an ever-evolving set of tools and approach that researchers need to keep pace. This changing technological landscape is also affecting employment. Technological advances are also making some skills less marketable, while creating demands for other skills that have not traditionally been associated with drug development. Scientists that can communicate across disciplines are increasingly in demand and those with multidisciplinary skills are at a premium. This aim of this initial training network is to improve the career perspectives of early stage researchers by providing multidisciplinary training in a network of industrial and academic partners involved in the discovery, development and commercialization of novel antibacterial and anti-infective drugs.

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