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Cell Chem Biol. 2016 Apr 21;23(4):435-41. doi: 10.1016/j.chembiol.2016.03.008. Epub 2016 Mar 31.

Small-Molecule Target Engagement in Cells.

Author information

1
Department of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.
2
Department of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany; Technical University Dortmund, Department of Chemistry and Chemical Biology, Otto-Hahn-Strasse 6, 44227 Dortmund, Germany. Electronic address: herbert.waldmann@mpi-dortmund.mpg.de.

Abstract

Monitoring how, when, and where small molecules engage their targets inside living cells is a critical step in chemical biology and pharmacological research, because it enables compound efficacy and confirmation of mode of action to be assessed. In this mini-review we summarize the currently available methodologies to detect and prove direct target engagement in cells and offer a critical view of their key advantages and disadvantages. As the interest of the field shifts toward discovery and validation of high-quality agents, we expect that efforts to develop and refine these types of methodologies will also intensify in the near future.

PMID:
27049669
DOI:
10.1016/j.chembiol.2016.03.008
[Indexed for MEDLINE]
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