GPCRs (G protein-coupled receptors) are the largest and most diverse family of membrane proteins that transduce extracellular stimuli into intracellular signals. They regulate a wide variety of physiological processes and are also well-validated ‘druggable’ targets.
Our track record
Charnwood Molecular has delivered on multiple GPCR projects. We have particular expertise in assay development and screening, using Promega’s NanoBRET TM GPCR reagents.
This format has significant advantages over traditional methods of compound profiling in 2D well plates:
- Cells adhere to scaffolds and thus, can be effectively moved between plates, replacing buffers without washing and providing the ability to use ‘assay ready compound plates’
- Cells can be cryo-preserved on scaffolds, then defrosted and used repeatedly from the same stock or batch, therefore improving data consistency
Applying the technology to other GPCRs
This technology can be applied to other GPCR’s with the benefits of:
- Highly specific detection of binding interactions due to the inherent distance constrains of BRET
- Small and minimally interfering bioluminescent peptide tag
- Selective cell surface detection
- Non-radioactive and homogeneous live cell assay
- High throughput –can be used for compound profiling in HTS formats