An in situ combinatorial methodology to synthesize and screen chemical probes

Antonie J. van der Zouwen, Jonas Lohse, Lianne H. E. Wieske, Katharina F. Hohmann, Ramon van der Vlag, Martin D. Witte*

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

2 Citations (Scopus)
219 Downloads (Pure)

Abstract

Chemical probes that label proteins of interest in the context of complex biological samples are useful research tools. The reactive group that forms the covalent bond with the target protein has a large effect on the selectivity and selecting the appropriate group determines the success of a probe. We here report the development of a combinatorial methodology based on imine chemistry that enables straightforward in situ synthesis and screening of different reactive groups and thereby simplifies identification of probe leads. Using our methodology, we found chemical probes targeting BirA and chloramphenicol acetyl transferase, two proteins associated with antibacterial activity and resistance.

Original languageEnglish
Pages (from-to)2050-2053
Number of pages4
JournalChemical Communications
Volume55
Issue number14
DOIs
Publication statusPublished - 18-Feb-2019

Keywords

  • CHEMISTRY
  • PROTEINS
  • DISCOVERY
  • LIGAND
  • INHIBITORS
  • PROXIMITY
  • REVEALS
  • BIOLOGY
  • TARGET

Cite this