Relevance of Nuclear Receptors
Nuclear receptors regulate gene expression levels by gene promotor binding and by recruitment of coregulators. Cofactor recruitment is a crucial regulatory step in nuclear receptor (NR) signal transduction. The pathways towards  gene expression involve ligand-dependent and independent interactions between NR and coregulator (CoR) proteins. In view of drug development, profiling these NR-CoR interactions is of importance to understand  mechanisms of drug action, to steer drug specificity, to understand putative adverse drug effects (on- versus off target), and to tailor the pharmacotherapies.
PamGene's unique position to understand nuclear receptors  

Modulation of nuclear receptor activity is usually quantitatively analyzed by assaying target gene transcription or downstream events. These parameters are however the net result of the nuclear receptor interaction with a wide range of individual coregulators. Studying nuclear receptor interactions with coregulators in a more global manner has been a challenge. Nuclear receptors usually have multiple coregulators to choose from and the biologic outcome of activation of the receptors then depends on the different coregulators expressed and their relative affinity to the nuclear receptor. However, conventional methods (E.g. FRET, Y2H, phage display, and colocalization studies in fluorescence microscopy) generally allow the study of one receptor–coregulator pair. PamGene's assay applies a peptide array that can assess interaction of full-length nuclear receptors with a set of coregulators, in a high-throughput manner. 



 

Application note: 

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