First-in-class small molecule for rare inflammatory diseases
Proteinase-activating Receptors (PARs) constitute a family of four GPCRs with a peculiar mechanism of activation through the cleavage of their extracellular domain. Amongst them, PAR2 has been shown to be involved in multiple inflammatory processes. In parallel, biased signaling has previously been described for PAR2 with ligands of different nature. However, the influence of the different PAR2 signaling pathways on the therapeutic activity and toxicity of these compounds is still poorly understood.
We launched a program in order to better understand the roles of the different signaling pathways downstream of PAR2 activation in the inflammatory responses, and to discover novel biased negative allosteric modulators (NAMs) for the treatment of rare inflammatory diseases.
This program is currently at the hit-to-lead stage.