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Expanding the "minimalist" small molecule tagging approach to different bioactive compounds
Wenjie Lang1, Chaonan Yuan, Biwei Zhu
1Key Laboratory of Bioorganic Synthesis of Zhejiang Province, College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou, 310014, P. R. China. gejy@zjut.edu.cn zhuq@zjut.edu.cn.
Organic & Biomolecular Chemistry
|March 1, 2019
Summary
Minimalist small molecule tagging (MSMT) easily creates affinity-based probes (AfBPs) from bioactive compounds. This versatile method enables proteomic studies, target validation, and cellular imaging for diverse applications.
Area of Science:
- Chemical Biology
- Proteomics
- Drug Discovery
Background:
- Minimalist small molecule tagging (MSMT) offers a straightforward method to convert bioactive compounds into affinity-based probes (AfBPs).
- AfBPs are crucial tools for proteomic studies, enabling target identification and validation.
Purpose of the Study:
- To evaluate the MSMT approach for generating AfBPs from diverse bioactive compounds.
- To assess the utility of these AfBPs in cell-based protein profiling, target validation, cellular imaging, and SILAC-based proteomics.
Main Methods:
- Seven bioactive compounds were modified with minimalist linkers using common chemical reactions to create AfBPs.
- The generated AfBPs were employed for cell-based protein profiling, target validation, cellular imaging, and quantitative proteomics (SILAC).
Main Results:
- The MSMT approach was successfully applied to seven distinct bioactive compounds, yielding functional AfBPs.
- Entinostat-derived (EN) and camptothecin-derived (CA) probes demonstrated efficacy in cellular imaging and SILAC-based target identification.
- The study confirmed the probes' utility in both proteomic profiling and target validation.
Conclusions:
- The minimalist small molecule tagging strategy is a versatile and expandable approach for creating dual-functional affinity-based probes.
- This method facilitates the development of novel chemical biology tools for proteomics and cellular imaging applications.
- MSMT provides a valuable platform for drug discovery and understanding biological pathways.