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A Membrane Protein Drug-Screening Methodology: 15N Solid-State NMR Study

This study presents a novel drug-screening methodology for membrane proteins using 15N solid-state NMR. The study includes the development of a flow system, PISEMA spectra analysis, and a structure-activity relationship (SAR) series. The results of viral inhibition assays and miniplaques screenings are also discussed.

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A Membrane Protein Drug-Screening Methodology: 15N Solid-State NMR Study

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  1. 15N Solid-State NMR Study for the Development of a Membrane Protein Drug-Screening Methodology Anna K. Wright, Ivan Hung, D.D. Busath, A. Kolocouris, Timothy A. Cross Experimental Nuclear Conference, April 2013

  2. PISEMA WT M2 TMD in AAO • 15N-Ile33,42 M2-TMD in aligned DMPC bilayers deposited onto AAO filters • Two spots, two residues • Potential for flow system

  3. PISEMA S31N M2 TMD on Glass • Superimposed PISEMA spectra of 15N- Val28,Ala30,Ile42 S31N M2-TMD in aligned DMPC bilayers on glass slides, with (red) and without (black) drug present • Strong impacts near and far

  4. Set 2, Viral Inhibition Assays • Structure-Activity Relationship (SAR) Series • Brent Johnson • H1N1 virus in MDCK culture • Anti-influenza antibodies to count miniplaques • Here are the results of the screens.  All drugs run at 50 uM. • Drug      Miniplaques • AK10        14, 20 • AK37        8, 11 • AK38        5,6 • AK39        19, 18 • AK40        15, 13 • Controls    78, 109, 88, 84 • Looks like all of them are active

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