# Orally active CBP/p300 degraders

> **NIH NIH R01** · UNIVERSITY OF MICHIGAN AT ANN ARBOR · 2024 · $688,392

## Abstract

Abstract: The histone acetyltransferase CREB-binding protein (CBP) and its paralogue p300 protein are key
transcriptional co-activators and attractive therapeutic targets for human prostate cancer and other types of
human cancers. Development of highly potent and orally active small-molecule degraders of CBP and p300
proteins represents a promising new therapeutic strategy. Our preliminary data demonstrate that our designed
degraders are highly effective in inducing rapid and complete degradation of both CBP and p300 proteins in
tumor cells at sub-xnanomolar concentrations and >100-times more potent in in inhibition of cell growth than
CBP/p300 inhibitors. Our optimized CBP/p300 degraders achieve excellent pharmacokinetics and oral
bioavailability in mice. Oral administration of our optimized CBP/p300 degrader strongly inhibits tumor growth
in animal models of human cancer at well-tolerated dose-schedules. Collectively, our preliminary data provide
compelling data to support the further evaluation, optimization and development of orally active CBP/p300
degraders as a new anticancer therapy.

## Key facts

- **NIH application ID:** 10855441
- **Project number:** 1R01CA289013-01
- **Recipient organization:** UNIVERSITY OF MICHIGAN AT ANN ARBOR
- **Principal Investigator:** SHAOMENG WANG
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2024
- **Award amount:** $688,392
- **Award type:** 1
- **Project period:** 2024-03-01 → 2029-02-28

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10855441

## Citation

> US National Institutes of Health, RePORTER application 10855441, Orally active CBP/p300 degraders (1R01CA289013-01). Retrieved via AI Analytics 2026-05-21 from https://api.ai-analytics.org/grant/nih/10855441. Licensed CC0.

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