Open-Source Project Spurs New Drug Discoveries

     (CN) — The first ever open-source drug discovery has successfully identified compounds that can be used to treat and prevent parasite-borne illnesses like malaria and even cancer, according to new research.
     Medicines for Malaria Venture, a nonprofit group based in Geneva, Switzerland, distributed 400 diverse compounds with antimalarial activity — called the Malaria Box — to 200 labs in 30 nations in late 2011. The findings from subsequent studies and analyses were published Thursday in the journal PLOS Pathogens.
     Distributing the Malaria Box to various labs enabled scientists to analyze the compounds and develop findings that have led to more than 30 new drug-development projects for a variety of diseases.
     As a stipulation to receiving the samples, the various research groups had to deposit the information from their studies in the public domain.
     “The trial was successful not only in identifying compounds to pursue for antimalarials, but it also identified compounds to treat other parasites and cancer,” lead author Wesley Van Voorhis, the director of the Center for Emerging and Re-emerging Infectious Diseases, said.
     The new study includes 236 screens of the Malaria Box, along with a comparison of results from 55 assays — an analytic procedure that assesses an organic sample — that were previously published. The data was then formatted to allow meta-analyses of the combined dataset.
     The combined biochemical and cellular assays have highlighted potential mechanisms of action for 135 of the compounds active in killing multiple life-cycle stages of the malaria parasite. Additionally, 32 compounds demonstrated activity against other pathogens, including the dengue fever vector the Aedes aegypti mosquito — which is also the primary vector of the Zika virus.
     “Excitingly some of these compounds also showed outstanding activity against other disease agents including fungi, bacteria, other single-cellular parasites, worms and even human cancer cells,” the study says.
     Owing to the thorough analysis of the compounds in the Malaria Box, the National Cancer Institute is now working on a colon cancer drug, Van Voorhis said. Several U.S. labs are investigating drugs to fight other parasites, and multiple European labs are working on anti-worm compounds.
     The success of distributing the compounds with antimalarial activity has prompted Medicines for Malaria Venture to send labs the Pathogen Box, a set of compounds that have broader potential applicability. The box is also available now to labs around the world.
     Researchers also cited the lack of connection between academia and industry as a major hindrance to innovation in drug discovery.
     “Much of the global resource in biology is present in universities, whereas the focus of medicinal chemistry is still largely within industry. Open-source drug discovery, with sharing of information, is clearly a first step towards overcoming that gap,” the study says.

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