MALARIA: Research on chemicals

Geneva, 20 May 2010. In an unprecedented move, data from three new projects supported by Medicines for Malaria Venture (MMV) have been made available in the public domain. The first, conducted by GlaxoSmithKline (GSK) has identified promising leads to develop new antimalarials. The second, the screening of compounds of the Genomics Institute of the Novartis Research Foundation (GNF) has been released to the European Bioinformatics Institute (EMBL-EBI). The third, conducted by Prof. Kip Guy at St Jude Children’s Research Hospital, Memphis, will also be released to the EMBL-EBI this week.
The GSK research comes from a year-long screening of more than 2 million compounds in GSK’s chemical library to identify those that could inhibit the malaria parasite, P. falciparum, and reports on an analysis of over 13,500 compounds that showed greatest activity. The largest group of compounds whose mode of action is understood was kinase inhibitors. The study also identified compounds that might be inhibiting processes in human red blood cells necessary for the parasite's survival. This opens up a novel possibility of fighting infection by halting these processes rather than stopping the malaria parasite itself.
All these data are available online through the European Bioinformatics Institute (EMBL-EBI) http://www.ebi.ac.uk/chemblntd/download, Collaborative Drug Discovery http://www.collaborativedrug.com/ and PubChem from the National Library of Medicine (NIH) http://pubchem.ncbi.nlm.nih.gov/ . Together with added intelligence from a publication in Nature[1], scientists globally have been given thousands of chemical starting points to stimulate their research into this deadly disease.
Data from part of an earlier screen from the Genomics Institute of the Novartis Research Foundation are also being reported. Over 800,000 compounds from external sources were screened, and over 5,600 compounds have confirmed activity on the parasite. The chemical structures of these compounds, the 50% inhibitory concentrations against P. falciparum growth, and general cytotoxicity have also recently been released to the EMBL-EBI.