# A Cell-Based Screen For The Discovery of Novel Proteolysis Targeting Chimeras (PROTACs)

> **NIH NIH R21** · SCRIPPS FLORIDA · 2020 · $237,500

## Abstract

Project Summary
Proteolysis targeting chimeras (PROTACs) represent an exciting new modality to inhibit proteins. These reagents
are chemical dimerizers that recruit an E3 ubiquitin ligase to a target protein of interest, resulting in poly-
ubiquitylation of the target protein and its subsequent degradation by the proteasome. Recently, it has become
clear that the E3 ligase must make productive contacts with the substrate. In other words, not all target proteins
can be turned over by a single E3 Ub ligase. This project will develop a cell-based screen for degradation of a
GFP-target protein fusion that employs a known ligand for the target protein fused to a complex library of
potential E3 ligase ligands, thus allowing the cell to “tell us” which of the ≈ 500 E3 Ub ligases in the cell are best
suited for targeting that protein for destruction.

## Key facts

- **NIH application ID:** 9842656
- **Project number:** 5R21GM131420-02
- **Recipient organization:** SCRIPPS FLORIDA
- **Principal Investigator:** Thomas J. Kodadek
- **Activity code:** R21 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $237,500
- **Award type:** 5
- **Project period:** 2019-01-01 → 2021-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9842656

## Citation

> US National Institutes of Health, RePORTER application 9842656, A Cell-Based Screen For The Discovery of Novel Proteolysis Targeting Chimeras (PROTACs) (5R21GM131420-02). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9842656. Licensed CC0.

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