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http://jbx.sagepub.com/content/20/1/131.long
Together with VU collaborators, IOTA scientists David Bailey, Paul England and Anitha Shanmugham have published a paper entitled “Fragment based screening in tandem with phenotypic screening provides novel anti-parasitic hits” in the Journal of Biomolecular Screening. The paper explores the role of fragment library screening in the development of new anti-parasitic drug hits.
Fragment based screening is a target based approach to drug discovery that involves screening a relatively small library of fragments that could potentially be inhibitors of a specific target. A more effective approach to finding new drug leads may be phenotypic screening, in which large libraries of compounds are screened against sets of target cells in order to determine biological activity. By utilizing the specificity of target based screening as a starting point for finding novel drug scaffolds, phenotypic screening can be focused to produce novel drug libraries by modulating the scaffolds of previously determined effective fragment hits. This two fold approach was successful in discovering novel drug hits with high anti-protozoal activity and low toxicity.
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