Licensing status

Publication and contact information

Drug platforms

Small molecule modulators of
G protein-coupled receptor 183 (GPR183; EBI2)

Small molecule modulators of EBI2 could be useful for probing the function of the receptor and its relevance to human diseases. EBI2 activation stimulates immune cell migration and has been genetically linked to autoimmune diseases including type 1 diabetes, but only one small molecule antagonist has been previously reported and no small molecule agonists have been reported. A chemical screen identified a small molecule agonist of mouse and human EBI2 with single-digit micromolar EC50 values. The agonist was then used to discover two small molecules that antagonized mouse and human EBI2 with nanomolar IC50 values. Next steps include collaborating with academic groups to elucidate the role of the oxysterol and EBI2 pathway in human diseases.

SciBX 7(17); doi:10.1038/scibx.2014.505
Published online May 1, 2014

Patent and licensing status undisclosed

Gessier, F. et al. J. Med. Chem.; published online March 28, 2014;
Contact: Andreas W. Sailer, Novartis Institutes for BioMedical Research,
Basel, Switzerland