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Modulating the masters: chemical tools to dissect CBP and p300 function
1Life Sciences Institute, University of Michigan, 210 Washtenaw Avenue, Ann Arbor, MI 48109-2216, USA.
Abstract:
Dysregulation of transcription is found in nearly every human disease, and as a result there has been intense interest in developing new therapeutics that target regulators of transcription. CREB binding protein (CBP) and its paralogue p300 are attractive targets due to their function as `master coactivators'. Although inhibitors of several CBP/p300 domains have been identified, the selectivity of many of these compounds has remained underexplored. Here, we review recent successes in the development of chemical tools targeting several CBP/p300 domains with selectivity acceptable for use as chemical probes. Additionally, we highlight recent studies which have used these probes to expand our understanding of interdomain interactions and differential coactivator usage.
Insights
Researchers are developing targeted therapies for diseases by focusing on transcription regulators like CREB binding protein (CBP) and p300. New chemical probes show promise for understanding these master coactivators and their roles in disease.
Area of Science:
- Biochemistry
- Molecular Biology
- Drug Discovery
Background:
- Transcription dysregulation is implicated in numerous human diseases.
- CREB binding protein (CBP) and its paralogue p300 are key transcriptional coactivators.
- Targeting CBP/p300 offers a therapeutic strategy for various diseases.
Purpose of the Study:
- To review the development of selective chemical tools targeting CBP/p300 domains.
- To highlight the utility of these chemical probes in understanding CBP/p300 function.
- To explore interdomain interactions and differential coactivator usage.
Main Methods:
- Review of recent literature on chemical probe development for CBP/p300.
- Analysis of studies utilizing selective CBP/p300 inhibitors.
- Examination of research on CBP/p300 interdomain communication.
Main Results:
- Several chemical tools targeting CBP/p300 domains with acceptable selectivity have been developed.
- These probes serve as valuable chemical probes for biological research.
- Recent studies have leveraged these probes to elucidate CBP/p300 biology.
Conclusions:
- Selective chemical probes for CBP/p300 are advancing research into transcription regulation.
- These tools facilitate a deeper understanding of disease mechanisms driven by transcription dysregulation.
- Further development and application of these probes hold therapeutic potential.
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