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Membrane Protein Structure in Live Cells: Methodology for Studying Drug Interaction by Mass Spectrometry-Based Footprinting

Mass spectrometry-based footprinting is an emerging approach for studying protein structure. Because integral membrane proteins are difficult targets for conventional structural biology, we recently developed a mass spectrometry (MS) footprinting method to probe membrane protein–drug interactions in live cells. This method can detect structural differences between apo and drug-bound states of membrane proteins, with the changes inferred from MS quantification of the cysteine modification pattern, generated by residue-specific chemical labeling. Here, we describe the experimental design, interpretation, advantages, and limitations of using cysteine footprinting by taking as an example the interaction of warfarin with vitamin K epoxide reductase, a human membrane protein. Compared with other structural methods, footprinting of proteins in live cells produces structural information for the near native state. Knowledge of cellular conformational states is a necessary complement to the high-resolution structur...

Authors:   Guomin Shen; Shuang Li; Weidong Cui; Shixuan Liu; Yihu Yang; Michael Gross; Weikai Li
Journal:   Biochemistry
Year:   2017
DOI:   10.1021/acs.biochem.7b00874
Publication date:   20-Dec-2017
Facts, background information, dossiers
  • vitamin K
  • structural biology
  • proteins
  • labelling
  • interactions
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