Community Research and Development Information Service - CORDIS

FP7

OPENMEDCHEM — Result In Brief

Project ID: 316773
Funded under: FP7-PEOPLE
Country: Belgium
Domain: Health, Fundamental Research

Pharma and academia work together on tuberculosis

Merging public-private research resources has given three young researchers the benefits from first-class training in the design and production of new drugs for tuberculosis (TB).
Pharma and academia work together on tuberculosis
The OPENMEDCHEM (Medicinal chemistry open innovation doctorates) project brought together the industry giant GlaxoSmithKline and the University of Antwerp under an Innovative Training Networks - European Industrial Doctorates (ITN-EID) initiative.

Early-stage researchers (ESRs) selected five highly promising compound families on the basis of antimycobacterial potential and ‘druglikeness’ scores. A structure-activity relationship analysis revealed two families with most potential for further investigation and for production of hybrid compounds that would ultimately yield groundbreaking therapeutic molecules.

At project close, all compou had been extensively characterised, leading to large sets of useful chemical and biological data. These data sets include the in vitro antimycobacterial potency and a range of physicochemical, biopharmaceutical and toxicological properties. The most promising compounds were tested for resistance, and one molecule was investigated in a mouse model of respiratory TB.

Highlighting the benefit of the industry-academic partnership, all ESRs ran an intramacrophage assay (TB bacilli are rapidly taken up by these white blood cells in humans and other animals) on a selection of their compounds using an advanced confocal microscopy readout. No hybrid molecules showed better potency when compared with the best parent compounds and with cytotoxicity data; the project thus discontinued research on one of the promising families.

Biochemical targets in the TB disease causing Mycobacterium tuberculosis were identified in all families. For one of these targets, methionine aminopeptidase, results of the validation experiments are still pending.

In total, the OPENMEDCHEM project has investigated four new classes of antimycobacterials. With potential as a basis for drug discovery programmes, this vast information platform can be used by industry and academic institutions. In particular, one compound has the potential for a lead optimisation evaluation. Around a third of the data has been reported in scientific journals and the remaining part is due for publication. With TB a major threat to healthcare with new incurable multiresistant strains, society at large stands to benefit from this research.

Related information

Subjects

Life Sciences

Keywords

Academia, tuberculosis, drug, TB, OPENMEDCHEM, industry
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