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Development and Application of Activity-based Fluorescent Probes for High-Throughput Screening.
Juan Cheng1, Xin Li1
1College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, Zhejiang, China.
Current Medicinal Chemistry
|May 26, 2021
Summary
Activity-based fluorescent probes enhance high-throughput screening (HTS) for drug discovery. This review details probe mechanisms and future development to improve hit identification and drug development.
Area of Science:
- Biochemistry
- Analytical Chemistry
- Drug Discovery
Background:
- High-throughput screening (HTS) is crucial for identifying drug candidates.
- Assay sensitivity remains a key challenge in HTS.
- Fluorescence-based assays are preferred for their sensitivity and ease of use.
Purpose of the Study:
- To review activity-based fluorescent probes used in HTS assays.
- To emphasize the structure-related working mechanisms of these probes.
- To explore the development of improved probes for drug discovery.
Main Methods:
- Literature review of activity-based fluorescent probes.
- Analysis of probe structure-activity relationships.
- Exploration of future probe development strategies.
Main Results:
- Fluorescence-based assays are dominant in HTS due to high sensitivity.
- Activity-based probes are valuable tools for monitoring HTS outputs.
- Understanding probe mechanisms is key to optimizing their design.
Conclusions:
- Activity-based fluorescent probes significantly advance HTS capabilities.
- Further development of novel probes can accelerate drug discovery.
- Optimized probes will enhance hit identification and therapeutic development.
