Journal article

Screening of the 'Stasis Box' identifies two kinase inhibitors under pharmaceutical development with activity against Haemonchus contortus

Yaqing Jiao, Sarah Preston, Anson V Koehler, Andreas J Stroehlein, Bill CH Chang, Kaylene J Simpson, Karla J Cowley, Michael J Palmer, Benoit Laleu, Timothy NC Wells, Abdul Jabbar, Robin B Gasser

PARASITES & 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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