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Functional Profiling, Identification, and Inhibition of Plasmepsins in Intraerythrocytic Malaria Parasites
Author(s) -
Liu Kai,
Shi Haibin,
Xiao Huogen,
Chong Alvin G. L.,
Bi Xuezhi,
Chang YoungTae,
Tan Kevin S. W.,
Yada Rickey Y.,
Yao Shao Q.
Publication year - 2009
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200903747
Subject(s) - malaria , vacuole , identification (biology) , computational biology , biology , profiling (computer programming) , proteases , biochemistry , immunology , computer science , ecology , cytoplasm , operating system , enzyme
Profile and eliminate! Plasmepsins (PMs), aspartic proteases required for malaria‐parasite growth, are promising antimalarial targets. The in situ screening of PMs with probes formed from β‐hydroxyazides 1 and alkynes with a photo‐cross‐linking unit and a tetraethylrhodamine reporter led to the identification of the small‐molecule inhibitor 2 , which inhibits all four food‐vacuole PMs and showed potent antimalarial activity in red‐blood‐cell cultures.