Bromodomains have had screening groups in their pocket ever since emerging as an attractive drug target. It’s been much easier for researchers to get excited about this class than it has for them to find potent and selective inhibitors of these closely related domains…until now.
Cayman Chemical has developed a robust in vitro system for measuring interactions between bromodomains and their acetylated peptide-binding partners using a Time-Resolved FRET methodology. These assays are designed to take the worry out of FRET in bromodomain inhibitor discovery by combining impressive sensitivity with a flexible format.
Bromodomain TR-FRET Assays Take the Worry Out of FRET
Cayman bromodomain inhibitor screening assays boast a big performance boost from their own specially made Europium chelate, which is directly labeled onto the bromodomain. This approach uses one less binding event, avoids the need for antibodies, and keeps Europium and APC closer together for stronger FRET signals. It sounds complicated, but the bottom line for the end-user is an assay with dramatically increased sensitivity that requires lower bromo concentrations as compared to standard TR-FRET assays which rely on Europium conjugated antibodies.
Sometimes it’s better to be a bit inhibited. These arrows point the way.
Cayman’s R&D team routinely matches the Ki values found in the literature for known bromodomain inhibitors. Plus, Cayman produces those bromodomain-Europium conjugates in-house, so they’re able to maintain consistently high quality, while keeping costs in check.
Lighting Up Bromodomain Drug Discovery
Cayman Chemical’s line of bromodomain assays allows scientists equipped with high-throughput techniques to quickly and accurately profile putative bromodomain inhibitors against either a panel of bromodomains, or to screen a selected bromodomain for novel inhibitor chemotypes, while using the same assay platform.
This validated assay system includes many features to help accelerate high-throughput screening efforts:
- Simple, mix-and-read assay format that’s stable for several hours
- Assay formats in 384-wells, or scalable to higher density plate formats
- Compatible with standard laboratory automation
Unlike some other assays out there, this one doesn’t use expensive antibodies or fussy PCR amplification for detection. The time and costs you save minimally compromise sensitivity when comparing it to other cumbersome methods.
There are several bromodomain assay kits available to choose from:
- BRDT bromodomain 1 TR-FRET Assay Kit
- BRD2 bromodomain 1 TR-FRET Assay Kit
- BRD2 bromodomain 2 TR-FRET Assay Kit
- BRD3 bromodomain 1 TR-FRET Assay Kit
- BRD4 bromodomain 1 TR-FRET Assay Kit
- BRD4 bromodomain 2 TR-FRET Assay Kit
You can also find a complete listing of epigenetic research products at the Cayman Chemical website.