# Harnessing E3 Ligases for Cancer Therapy

> **NIH NIH R01** · UNIVERSITY OF CALIFORNIA BERKELEY · 2024 · $388,151

## Abstract

Targeted protein degradation (TPD) has arisen as a powerful therapeutic modality for degrading
and eliminating cancer-causing proteins and has enabled potential access into classically
undruggable protein targets. Two main TPD approaches currently employed include
heterobifunctional Proteolysis Targeting Chimeras (PROTACs) and monovalent molecular glue
degraders that both use small-molecules to induce the proximity of E3 ubiquitin ligases with
target proteins to ubiquitinate and degrade specific disease targets of interest. However, there
are still major bottlenecks in realizing the full potential of TPD platforms. In this proposal, we will
overcome bottlenecks in cancer drug discovery by developing innovative next-generation
approaches for TPD using covalent chemoproteomic strategies, including expanding upon
rational chemical design strategies to discover molecular glue degraders and uncover
permissive E3 ligases for TPD applications and covalently targeting and destabilizing
undruggable oncogenic transcription factors.

## Key facts

- **NIH application ID:** 10913762
- **Project number:** 2R01CA240981-06
- **Recipient organization:** UNIVERSITY OF CALIFORNIA BERKELEY
- **Principal Investigator:** Daniel Nomura
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2024
- **Award amount:** $388,151
- **Award type:** 2
- **Project period:** 2019-07-01 → 2029-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10913762

## Citation

> US National Institutes of Health, RePORTER application 10913762, Harnessing E3 Ligases for Cancer Therapy (2R01CA240981-06). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10913762. Licensed CC0.

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