AI Article Synopsis
- DNA-encoded library (DEL) screens are effective tools for discovering potential drugs targeting various biological molecules.
- The review highlights trends in how molecular properties change from initial hits to optimized leads, providing case studies that illustrate specific optimization strategies.
- DEL has unique characteristics, such as combinatorial synthesis methods and linker effects, that influence the hit-to-lead optimization process differently compared to traditional high throughput screening (HTS) methods.
Article Abstract
DNA-encoded library (DEL) screens have emerged as a powerful hit-finding tool for a number of biological targets. In this Innovations article, we review published hit-to-lead optimization studies following DEL screens. Trends in molecular property changes from hit to lead are identified, and specific optimization tactics are exemplified in case studies. Across the studies, physicochemical property and structural changes post-DEL screening are similar to those which occur during hit-to-lead optimization following high throughputscreens (HTS). However, unique aspects of DEL-the combinatorial synthetic methods which enable DEL synthesis and the linker effects at the DNA attachment point-impact the strategies and outcomes of hit-to-lead optimizations.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7957921 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.0c00615 | DOI Listing |
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