New research conducted by GlaxoSmithKline (GSK) was published in Nature identifying promising potential leads to develop new medicines to treat malaria. The research comes from a year-long screening of more than two million compounds in GSK’s chemical library to seek out those that could inhibit the malaria parasite, P. falciparum, and reports on an analysis of the more than 13,500 compounds, or hits, that showed greatest activity.
The largest group of compounds, where their mode of action is understood, were kinase inhibitors and the authors suggest that further exploration of these compounds might lead to novel antimalarial therapeutic strategies.
In an accompanying editorial piece in Nature, David A Fidock from the Departments of Microbiology & Immunology and of Medicine (Infectious Diseases), Columbia University Medical Center, New York commented: “This would constitute an important new direction for antimalarial drug development — one that might cross paths with the vast chemical repositories developed to target kinases in other disorders.”
The study also identified compounds that may be inhibiting processes in human red blood cells which could be necessary for the parasite's survival. This opens up a novel possibility of fighting infection by looking to halt these processes in human red blood cells, rather than stopping the malaria parasite itself.
GSK is committed to stimulating new research into neglected tropical diseases, such as malaria, which blight developing countries. In January 2010, as part of the company’s commitment to open innovation in this area, GSK announced its intention to share data and chemical structures identified in its screening of the two million compounds from its library against the parasites that cause malaria using on-line resources.
As of today, the 13,533 ‘hits’ are accessible on public websites, marking the first time that a pharmaceutical company has made universally available the structures of so many compounds. More than 80 per cent of these molecules are proprietary to GSK, and therefore the information will be new to the research community.
All these data are available online through the European Bioinformatics Institute (EMBL-EBI) and Collaborative Drug Discovery. Together with the added intelligence in the Nature publication, scientists globally have been given thousands of chemical starting points to stimulate their research into this deadly disease which kills one child in Africa every 30 seconds.
“The world desperately needs new medicines to fight malaria,” said Dr Patrick Vallance, head of Drug Discovery at GSK. “These data provide us and other researchers around the world with several new leads to follow. We hope this information will drive further studies into the disease, and we call for all researchers to add their findings back to the EBI to create an open worldwide collaboration to expand our collective knowledge and make new medicines.”