# Asymmetric synthesis of DNA-encoded libraries of natural product-like compounds.

> **NIH NIH R43** · DELUGE BIOTECHNOLOGIES, INC. · 2022 · $223,389

## Abstract

Project Summary
DNA-encoded library (DEL) technology is a powerful method for the discovery of protein ligands. It is capable
of screening millions of small molecules for a fraction of the price required to conduct traditional, function-based
high-throughput screens. A current limitation of the technology is that it is difficult to incorporate large numbers
of sp3 chiral centers into libraries, since few, if any, asymmetric synthesis methods have been validated for DEL
synthesis. This is unfortunate, since there is general agreement that DELs with more natural product-like
characteristics would be a highly valuable source of drug leads. Here we will adapt asymmetric organocatalytic
aldol reactions for solid-phase synthesis of DELs. This effort will involve the development of a novel proximity
catalysis method to drive otherwise recalcitrant reactions. If successful, this work will enable the synthesis of
DELs of unprecedented stereochemical complexity.

## Key facts

- **NIH application ID:** 10479368
- **Project number:** 1R43GM142342-01A1
- **Recipient organization:** DELUGE BIOTECHNOLOGIES, INC.
- **Principal Investigator:** Nicholas Paciaroni
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $223,389
- **Award type:** 1
- **Project period:** 2022-04-01 → 2023-09-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10479368

## Citation

> US National Institutes of Health, RePORTER application 10479368, Asymmetric synthesis of DNA-encoded libraries of natural product-like compounds. (1R43GM142342-01A1). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/10479368. Licensed CC0.

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