SLAS DISCOVERY · 2016 · 23 citations · 14 references
PharmacyBiochemistryMedicinal ChemistryDrug DesignDrug DiscoveryMass Spectrometric AnalysisChemical Library DesignEnzyme InhibitionFragment-based Lead DiscoveryMass SpectrometryNatural Product Drug DiscoveryNatural Product-based Drug DesignBinder DiscoveryFragment Library ScreeningFragment Screening LibrariesMass Spectrometric ScreeningMass Spectrometry-based ScreeningNatural Product ExtractionNatural Product Library ScreeningPlasmodium Falciparum
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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The Determination of Enzyme Dissociation Constants
Hans Lineweaver, Dean Burk · Journal of the American Chemical Society · 1934 · 12.1K citations
Artemisinin: Discovery from the Chinese Herbal Garden
Louis H. Miller, Xin‐zhuan Su · Cell · 2011 · 433 citations · Full text