Journal article

Novel broad-spectrum activity-based probes to profile malarial cysteine proteases

Michele SY Tan, Dara Davison, Mateo I Sanchez, Bethany M Anderson, Stephen Howell, Ambrosius Snijders, Laura E Edgington-Mitchell, Edgar Deu

PLoS One | PUBLIC LIBRARY SCIENCE | Published : 2020

Abstract

Clan CA cysteine proteases, also known as papain-like proteases, play important roles throughout the malaria parasite life cycle and are therefore potential drug targets to treat this disease and prevent its transmission. In order to study the biological function of these proteases and to chemically validate some of them as viable drug targets, highly specific inhibitors need to be developed. This is especially challenging given the large number of clan CA proteases present in Plasmodium species (ten in Plasmodium falciparum), and the difficulty of designing selective inhibitors that do not cross-react with other members of the same family. Additionally, any efforts to develop antimalarial d..

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Grants

Awarded by Welcome Trust


Awarded by Royal Society Sir Henry Dale Fellowship


Awarded by Marie Curie Career Integration Grant


Awarded by National Health and Medical Research Council of Australia (NHMRC)


Funding Acknowledgements

This work was funded by the Welcome Trust and Royal Society Sir Henry Dale Fellowship 099950 and the Marie Curie Career Integration Grant PCIG14-GA-2013-631809, both awarded to E.D. LEM was supported by an Early Career Fellowship from the National Health and Medical Research Council of Australia (NHMRC, GNT1091636) and a Grimwade Fellowship sponsored by the Russell and Mab Grimwade Miegunyah Fund at the University of Melbourne. Finally, we would also like to thank the Medical Research Council for funding SYT through the National Institute for Medical Research student placement program. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.