# Selective PET imaging probes targeting BD1 of N-terminal bromodomains

> **NIH NIH R03** · MASSACHUSETTS GENERAL HOSPITAL · 2020 · $249,280

## Abstract

Project Summary
Bromodomain proteins function as epigenetic “readers” and play a key role in epigenetic regulation of gene
transcription by binding to acetylated lysine residues (Ac-K) on histone tails. BET proteins have two conserved
N-terminal bromodomains (BD1 and BD2). The bromodomain and extra-terminal domain (BET) inhibitors have
been extensive studied for tumors treatment in the past few years. Recently, BET inhibitors have been reported
to play a key role in brain functions, such as learning and memory, also show a therapeutic potential for substance
abuse. BET proteins have diverse roles in regulating tissue-specific transcriptional programs, therefore, targeting
of specific BET domains will be important for investigating the safety of potential therapeutics.
Unfortunately, there are no suitable non-invasive imaging tools for investigating BET expression and activity in
animals or in man. The development of techniques for visualizing specific BET domains in vivo represents a key
step in understanding both the normal function and pathophysiology of BET in brain. Moreover, these techniques
will accelerate the discovery of small molecule therapeutics that selectively interacts with the specific BET
domains. The project is designed to develop novel PET imaging probes for BD2 domain of BET. We will modify
the structure of our lead compounds and label BET inhibitors with fluorine-18 and evaluate the potential of these
molecules to serve as F-18 radiotracers for BET in humans by imaging their distribution and pharmacokinetics
in rodents and non-human primates.

## Key facts

- **NIH application ID:** 10054837
- **Project number:** 1R03DA050860-01A1
- **Recipient organization:** MASSACHUSETTS GENERAL HOSPITAL
- **Principal Investigator:** Changning Wang
- **Activity code:** R03 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $249,280
- **Award type:** 1
- **Project period:** 2020-07-15 → 2022-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10054837

## Citation

> US National Institutes of Health, RePORTER application 10054837, Selective PET imaging probes targeting BD1 of N-terminal bromodomains (1R03DA050860-01A1). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10054837. Licensed CC0.

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