AsianScientist (Sep. 26, 2016) – Looking for alternatives to artemisinin for malarial treatment? Why not try crowdsourced drug discovery, as a study published in ACS Central Science has done.
Current gold standard antimalarial treatments are based on artemisinin, a compound developed in the 1970s in China, combined with a partner drug. Resistance to artemisinin and its partners has already emerged in some parts of the world and no viable replacements are currently available. Given the lack of commercial incentive for industry to develop drugs for neglected diseases—and because academic researchers often lack resources to move compounds forward—there is a need for new approaches to drug discovery.
Believing that the solution for drug discovery could lie in open, crowdsourced science, Associate Professor Matthew Todd from the University of Sydney, together with the not-for-profit research and development organization Medicines for Malaria Venture, tested an open-source research mechanism wherein anyone could participate and no patents were sought.
During the project’s run, more than 50 researchers from 21 organizations around the world shared their data and ideas in real time, which started with a large set of potential drug molecules made public by pharmaceutical company GlaxoSmithKline.
Two chemical subseries were derived from the crowdsourcing experiment: one chemical subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity. A second subseries displayed high potency, including activity within gametocyte and liver stage assays, but at the cost of low solubility.
The article can be found at: Williamson et al. (2016) Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles.
Source: University of Sydney; Photo: Pixabay.
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