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Related Experiment Video

Updated: Jul 1, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

A Systematic Direct-to-Biology Approach Identified Potent Cereblon HaloPROTACs.

Rebecca Stevens^1,2, Kwok-Ho Chan¹, Alice Moore¹

¹Research Technologies, Medicines Research Centre, GSK, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

ACS Chemical Biology

|June 30, 2026

Summary

New HaloPROTACs targeting protein degradation were developed using cereblon (CRBN) binders. These tools show high potency and selectivity, advancing targeted protein degradation research without needing specific target ligands.

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High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

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Last Updated: Jul 1, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

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Published on: May 15, 2019

The Development and Application of Biophysical Assays for Evaluating Ternary Complex Formation Induced by Proteolysis Targeting Chimeras (PROTACS)

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Published on: January 12, 2024

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

Area of Science:

Biochemistry
Molecular Biology
Chemical Biology

Background:

HaloTags are versatile tools for protein labeling and studying target biology.
HaloPROTACs are heterobifunctional molecules that induce proximity between E3 ligases and target proteins for degradation.
This induced proximity enables temporal- and dose-dependent protein degradation and efficient cellular knockdown.

Purpose of the Study:

To develop novel cereblon (CRBN)-recruiting HaloPROTACs.
To identify potent and selective HaloPROTACs through high-throughput synthesis and screening.
To compare the efficacy of new CRBN binders with existing IMiD-based binders.

Main Methods:

Utilized plate-based high-throughput synthesis for generating diverse CRBN HaloPROTAC libraries.
Employed direct-to-biology screening for evaluating HaloPROTAC efficacy.
Tested over 100 structurally diverse CRBN HaloPROTACs in a FAK-tagged cell line.

Main Results:

Identified highly potent CRBN-recruiting HaloPROTACs.
HaloPROTACs with dihydrouracil CRBN binders demonstrated superior potency and selectivity.
These novel binders outperformed IMiD-based counterparts in efficacy.

Conclusions:

Successfully developed novel CRBN-based HaloPROTACs.
The new HaloPROTACs offer enhanced capabilities for targeted protein degradation.
These tools represent a valuable addition to the HaloPROTAC toolkit for biological research.