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Advancing small-molecule drug discovery by encoded dual-display technologies
Alice Lessing1, Dimitar Petrov1, Jörg Scheuermann1
1ETH Zürich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, Zürich, Switzerland.
Trends in Pharmacological Sciences
|September 22, 2023
Summary
DNA-encoded chemical library (DEL) technology, including novel dual-display methods, accelerates small-molecule drug discovery. This approach enhances hit identification for drug targets and protein degradation, offering versatile applications in drug development.
Area of Science:
- Medicinal Chemistry
- Drug Discovery Technology
- Chemical Biology
Background:
- DNA-encoded chemical library (DEL) technology is a cornerstone of modern small-molecule drug discovery.
- DEL enables cost-effective and high-success-rate identification of ligands for various target proteins.
- It has shown promise in identifying ligands for targeted protein degradation (TPD).
Purpose of the Study:
- To review recent advancements in DNA- or peptide nucleic acid (PNA)-encoded chemical libraries.
- To highlight the capabilities of dual-display DEL technologies for sophisticated applications.
- To discuss the potential of dual-display for future drug discovery endeavors.
Main Methods:
- Utilizing DNA- or PNA-encoded chemical libraries with simultaneous display of ligand pairs (dual-display).
- Exploring both stable and dynamic dual-display DEL formats for affinity-based selections.
- Implementing novel methods for seamless conversion between single- and double-stranded library formats.
Main Results:
- Dual-display DEL technologies enable innovative affinity-based selection modalities, including in-cell applications.
- The development of versatile single- and double-stranded library format conversions.
- Identification of initial drug candidates emerging from dual-display technologies.
Conclusions:
- Dual-display DEL represents a significant advancement, expanding the scope of DEL applications.
- This technology offers enhanced versatility and sophisticated selection capabilities for drug discovery.
- Dual-display holds considerable future potential for identifying novel therapeutics and advancing drug development pipelines.
