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High-Throughput Screening: today's biochemical and cell-based approaches.
Vincent Blay1, Bhairavi Tolani2, Sunita P Ho1
1Division of Biomaterials and Bioengineering, School of Dentistry, University of California San Francisco, San Francisco, CA 94143, USA; Department of Urology, School of Medicine, University of California San Francisco, San Francisco, CA 94143, USA.
Drug Discovery Today
|August 18, 2020
Summary
High-throughput screening (HTS) identifies potential drug compounds using biochemical and cell-based assays. This review covers various HTS methods and target deconvolution strategies for drug discovery.
Area of Science:
- Drug discovery and development
- Chemical biology
- Assay development
Background:
- High-throughput screening (HTS) is crucial for identifying initial chemical matter in drug development.
- A wide array of biochemical and cell-based assays are currently employed for hit identification.
Purpose of the Study:
- To provide a comprehensive review of current HTS methods for hit identification.
- To discuss target deconvolution strategies and tools following hit discovery.
- To highlight considerations for selecting HTS methods and future research directions.
Main Methods:
- Biochemical assays: fluorescence polarization, FRET, TR-FRET, fluorescence lifetime analysis.
- Binding-based methods: NMR, SPR, mass spectrometry, DSF.
- Cell-based assays: viability, reporter gene, second messenger, high-throughput microscopy.
- High-content screening (HCS) and target deconvolution tools (chemical proteomics, in silico, chemical genetics, CRISPR/dCas-based screens).
Main Results:
- Detailed survey of diverse HTS methodologies for hit identification.
- Overview of target deconvolution techniques, including advanced CRISPR/dCas screens.
- Discussion on factors influencing HTS method selection.
Conclusions:
- The choice of HTS method depends on specific project needs and goals.
- Emerging technologies like HCS and CRISPR-based screens offer powerful approaches.
- Continued innovation in HTS and target deconvolution is vital for advancing drug discovery.
