Targeting Orphan Nuclear Receptors
Nuclear receptors (NRs) are key players in the regulation of gene expression, coordinating protein assemblies upon their surfaces. NRs are regulated by ligand binding, which remodels the interaction surfaces and subsequently influences macromolecular complex formation, many NRs however are still orphan receptors whose bona fide ligands have yet to be identified. Indeed, several important nuclear receptor drug targets, Farnesoid X Receptor (FXR), Liver X Receptor (LXR), and Peroxisome Proliferator-activated Receptors (PPARs) are all successful examples of adopted orphan receptors.
TES Pharma is therefore focused on the deorphanisation of nuclear receptors and the development of an understanding of their pharmacology to transform them into novel therapeutic targets. To support our approach we have developed a panel of human, rodent, and nematode nuclear receptor assays based on AlphaScreen and other technologies which provide the ability to screen compounds across multiple nuclear receptor subtypes. This panel provides a comprehensive system to progressing novel ligands and understanding the science of nuclear receptor modulation.
Leveraging its extensive Nuclear Receptor expertise and fully-integrated drug discovery platform, TES Pharma is generating a broad pipeline of first-in-class and best-in-class compounds as modulators of Orphan Nuclear Receptors.