Article
Ligand-induced conformational change of Plasmodium falciparum AMA1 detected using 19F NMR.
Journal of medicinal chemistry - 14 Aug 2014
Ge Xiaopeng, MacRaild Christopher A, Devine Shane M, Debono Cael O, Wang Geqing, Scammells Peter J, Scanlon Martin J, Anders Robin F, Foley Michael, Norton Raymond S
Abstract excerpt
We established an efficient means of probing ligand-induced conformational change in the malaria drug target AMA1 using 19F NMR. AMA1 was labeled with 5-fluorotryptophan (5F-Trp), and the resulting 5F-Trp resonances were assigned by mutagenesis of the native Trp residues. By introducing additional Trp residues at strategic sites within a ligand-responsive loop, we detected distinct conformational consequences...
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