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Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing?

AuthorsAmata, Emanuele; Xi, Hualin; Colmenarejo, Gonzalo; Díaz-González, Rosario; Cordon-Obras, Carlos; Berlanga, M.; Manzano, Pilar; Erath, Jessey; Roncal, Norma E.; Lee, Patricia J.; Leed, Susan E.; Rodríguez, Ana ; Sciotti, Richard J.; Navarro, M.; Pollastri, M.P.
KeywordsPreferred lead repurposing
Trypanosoma brucei
Trypanosoma cruzi
Leishmania major
Plasmodium falciparum
Published Kinase Inhibitor Set
Issue DateMar-2016
PublisherAmerican Chemical Society
CitationACS Infectious Diseases
AbstractA kinase-targeting cell-based high-throughput screen (HTS) against Trypanosoma brucei was recently reported, and this screening set included the Published Kinase Inhibitor Set (PKIS). From the PKIS was identified 53 compounds with pEC(50) >= 6. Utilizing the published data available for the PKIS, a statistical analysis of these active antiparasitic compounds was performed, allowing identification of a set of human kinases having inhibitors that show a high likelihood for blocking T. brucei cellular proliferation in vitro. This observation was confirmed by testing other established inhibitors of these human kinases and by mining past screening campaigns at GlaxoSmithKline. Overall, although the parasite targets of action are not known, inhibitors of this set of human kinases displayed an enhanced hit rate relative to a random kinase-targeting HTS campaign, suggesting that repurposing efforts should focus primarily on inhibitors of these specific human kinases. We therefore term this statistical analysis-driven approach "preferred lead repurposing".
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