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J Med Chem. 2009 May 14;52(9):2875-9. doi: 10.1021/jm9000665.

An innovative method to study target protein-drug interactions by mass spectrometry.

Author information

  • 1Department of Pharmaceutical Chemistry and Bioanalytics, Institute of Pharmacy, Martin-Luther-Universität Halle-Wittenberg, Wolfgang-Langenbeck-Strasse 4, D-06120 Halle/Saale, Germany.

Abstract

We report the combination of chemical cross-linking and high-resolution mass spectrometry for analyzing conformational changes in target proteins that are induced by drug binding. With this approach conformational changes in the peroxisome proliferator-activated receptor alpha (PPARalpha) upon binding of low-molecular weight compounds were readily detected, proving that the strategy provides a basis to efficiently characterize target protein-drug interactions.

PMID:
19379014
[PubMed - indexed for MEDLINE]
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