Abstract
Chemical probes are highly valuable reagents for the study of protein targets. The potency and selectivity of a chemical probe for its primary target protein are important contributors to its utility as an experimental reagent. When applying a chemical probe in a new cellular system, it is important to consider several factors. This chapter focuses on cellular target engagement approaches of particular relevance for epigenetic targets. It exemplifies the application of epigenetic chemical probes to epigenetic targets by describing the generation and application of chemical probes targeting two different bromodomain families. The success and impact of chemical probes targeting the Bromodomain and extra-terminal (BET) family and CBP/p300 bromodomains augurs well for current efforts to generate probes for other previously untargeted histone readers, writers, and erasers. These probes are expected to enhance our understanding of these proteins and may reveal opportunities for therapeutic intervention.
| Original language | English |
|---|---|
| Title of host publication | Epigenetic Drug Discovery |
| Publisher | wiley |
| Pages | 133-152 |
| Number of pages | 20 |
| ISBN (Electronic) | 9783527809257 |
| ISBN (Print) | 9783527343140 |
| DOIs | |
| State | Published - 1 Jan 2019 |
| Externally published | Yes |
Keywords
- Bromodomain and extra-terminal family
- cellular target engagement
- epigenetic chemical probes
- ntargeted histone reader
- primary target protein
- therapeutic intervention