Journal
JOURNAL OF BIOMOLECULAR SCREENING
Volume 21, Issue 2, Pages 194-200Publisher
SAGE PUBLICATIONS INC
DOI: 10.1177/1087057115622605
Keywords
malaria; FTMS; PfRab11a
Funding
- Australian Research Council [ARC LIEF LE0237908]
- Australian Research Council (ARC [DP0343419, LP120100485]
- Bill & Melinda Gates Foundation Grand Challenges Explorations Grant Phase II [OPP1035218 GCE]
- Australian Research Council [LP120100485, DP0343419] Funding Source: Australian Research Council
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Electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry (ESI-FTICR-MS or ESI-FTMS) was used to screen 192 natural product extracts and a 659-member natural product-based fragment library for bindings to a potential malaria drug target, Plasmodium falciparum Rab11a (PfRab11a, PF13_0119). One natural product extract and 11 fragments showed binding activity. A new natural product, arborside E, was identified from the active extract of Psydrax montigena as a weak binder. Its binding activity and inhibitory activity against PfRab11a were confirmed by ESI-FTMS titration experiments and an orthogonal enzyme assay.
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