Expanding the "minimalist" small molecule tagging approach to different bioactive compounds

Wenjie Lang, Chaonan Yuan, Biwei Zhu, Sijun Pan, Jian Liu, Jie Luo, Shikun Nie, Qing Zhu, Jun Seok Lee, Jingyan Ge

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


"Minimalist" small molecule tagging (MSMT) is a promising approach that easily converts bioactive compounds into affinity-based probes (AfBPs) for proteomic studies. In this work, seven bioactive compounds targeting diversified protein classes were installed with "minimalist" linkers through common reactions to generate the corresponding AfBPs. These probes were evaluated for cell-based protein profiling and target validation. Among them, the entinostat-derived probe EN and the camptothecin-derived probe CA were further utilized in cellular imaging and SILAC-based large-scale target identification. Our extensive studies suggest that the "minimalist" small molecule tagging approach could be expanded to different classes of bioactive compounds for modification into AfBPs as a dual functional tool for both proteomics and cellular imaging.

Original languageEnglish
Pages (from-to)3010-3017
Number of pages8
JournalOrganic and Biomolecular Chemistry
Issue number11
Publication statusPublished - 2019
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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