Structure-based design and analysis of SuFEx chemical probes
Lyn H Jones1, Jeffery W Kelly2
1Center for Protein Degradation , Dana-Farber Cancer Institute , 360 Longwood Avenue , Boston , MA 02215 , USA .
RSC Medicinal Chemistry
|January 22, 2021
Summary
Sulfur(VI)-fluoride exchange (SuFEx) chemistry allows precise protein labeling. New insights into protein environments guide the design of advanced SuFEx probes for chemical biology and drug discovery.
Area of Science:
- Chemical Biology
- Medicinal Chemistry
- Organic Chemistry
Background:
- Sulfur(VI)-fluoride exchange (SuFEx) chemistry offers precise reactivity for chemical probe development.
- Understanding protein microenvironments is crucial for targeted labeling and probe design.
Purpose of the Study:
- To review recent findings on SuFEx chemistry in protein labeling.
- To explore how protein-probe structures and proteomic data inform SuFEx probe design.
- To guide future development of SuFEx probes for chemical biology and drug discovery.
Main Methods:
- Analysis of emerging protein-probe structural data.
- Review of proteomic mapping experiments.
- Synthesis of new information to guide rational probe design.
Main Results:
- SuFEx chemistry enables context-specific labeling of protein binding sites.
- Protein microenvironment characteristics influence the reactivity of targetable amino acid residues.
- New findings provide a basis for improved rational design of SuFEx probes.
Conclusions:
- The rational design of SuFEx probes is advancing due to a deeper understanding of protein environments.
- These advancements will impact various applications in chemical biology and drug discovery.
- SuFEx chemistry remains a powerful tool for exploring biological systems.
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