Journal article
Screening of the 'Stasis Box' identifies two kinase inhibitors under pharmaceutical development with activity against Haemonchus contortus
Y Jiao, S Preston, AV Koehler, AJ Stroehlein, BCH Chang, KJ Simpson, KJ Cowley, MJ Palmer, B Laleu, TNC Wells, A Jabbar, RB Gasser
Parasites and Vectors | BMC | Published : 2017
Abstract
Background: In partnership with the Medicines for Malaria Venture (MMV), we screened a collection ('Stasis Box') of 400 compounds (which have been in clinical development but have not been approved for illnesses other than neglected infectious diseases) for inhibitory activity against Haemonchus contortus, in order to attempt to repurpose some of the compounds to parasitic nematodes. Methods: We assessed the inhibition of compounds on the motility and/or development of exsheathed third-stage (xL3s) and fourth-stage (L4) larvae of H. contortus using a whole-organism screening assay. Results: In the primary screen, we identified compound MMV690767 (also known as SNS-032) that inhibited xL3 mot..
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Funding Acknowledgements
This study supported by the Australian Research Council (ARC) and Medicines for Malaria Venture (MMV). The Victorian Centre for Functional Genomics (KJS) is supported by funding from the Australian Government's Education Investment Fund, through the Super Science Initiative and the Peter MacCallum Cancer Centre Foundation.