3.2.3.2 Natural-Product-Enriched DELs

Abstract

Natural products are privileged compounds of natural evolution that are often rich in sp³ carbon atoms, bear multiple stereocenters, and have diverse skeletons. These features endow natural products with a broad spectrum of pharmacological activities. As a consequence, natural products play a key role in the history of medical treatment and drug discovery. The natural-product-enriched DNA-encoded library (nDEL) approach allows natural products or bioactive chemical molecules with known biological functions to be readily annotated with unique amplifiable DNA barcodes by so-called “late-stage” DNA labeling reactions. The final DNA-annotated natural products are included in a DEL, which can be packaged in a single test-tube and screened against a broad spectrum of cellular targets.

Key words

DNA-encoded libraries - natural products - drug discovery - labeling - screening

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