Nuclear receptor profiling


 

Nuclear receptors (NRs) are major targets for drug discovery. Upon ligand binding, NRs undergo a conformational change, which alters their binding preference for coregulators. Short α-helical sequences in the coregulator proteins, LXXLL (in coactivators) or LXXXIXXXL (in corepressors), are essential for the NR-coregulator interactions. However, little is known on how specificity is dictated.

 

To obtain a comprehensive overview of NR-coregulator interactions, we developed MARCoNI: Microarray Assay for Real-time Coregulator-Nuclear Receptor Interaction. This is a PamChip® microarray containing 53 or 155 coregulator peptides and provides an assay which allows for characterization of nuclear receptor function, i.e. coregulator binding.
 
A set of peptides, each representing a coregulator derived motif (NR-box), is immobilised in an array format to the solid phase of the PamChip (lower left). A fluorescently labelled antibody visualises the peptide binding of the NR in the assay mix, which is detected by the PamStation ® instrument.
 
We have a 22 nuclear receptor assay available. For more information contact Rinie van Beuningen, VP Business Development rvbeuningen@pamgene.com +31 73 615 80 80.