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Events

Towards the Development and Discovery of TcTS Inhibitors for Treatment of Chagas Disease

Date: 
Thursday, November 22, 2018 - 18:30 to 19:30
Speaker: 
Kyle Robinson - Withers Group
Affiliation: 
Department of Chemistry, University of British Columbia
Event Category: 
CBDG - Chemical Biology Discussion Group
Location: 
Chemistry D300

Abstract: Trypanosoma cruzi trans sialidase (TcTS) has been identified as a potential therapeutic target for treatment of Chagas disease. Thus, rational inhibitor design and screening approaches have been carried out to identify improved trans-sialidase inhibitors. A library of C9-modified difluorosialic acid analogues has been synthesized to evaluate efficacy of these mechanism based inhibitors towards TcTS activity. In search of new inhibitor motifs, screening of nearly 1000 marine sponge extracts was employed, leading to the identification of low µM inhibitors of the  target enzyme.