PARmedics is designing small molecules that block one or more of the PAR-2 pathways for more targeted and effective therapies.
Protease-activated-receptor-2 (PAR-2) is a member of a superfamily of proteins known as G-protein-coupled receptors (GPCRs). There are hundreds of GPCRs in the human proteome, that transmit signals in response to a diverse array factors. PAR-2 responds to proteases released during tissue injury and inflammation, that cleave at specific sites in the N-terminus to generate distinct signaling responses within the cell.
Depending on the tissue and the signaling pathway that is activated, PAR-2 can elicit pain and inflammation, or promote protective responses. Using medicinal chemistry principals based on the regions of the receptor that are crucial for its activation, we are designing small molecules that block one or more of these PAR-2 pathways, for more targeted therapies for chronic pain, migraine, asthma and respiratory infections.
We are developing a novel class of small molecules that inhibit Protease-activated Receptor-2 (PAR-2), a receptor found in neurons, airway and immune cells, that generates cellular signals involved in inflammation and pain. Our first-in-class small molecules have the potential to fill an unmet need for treating airway inflammation and chronic pain, with reduced adverse effects, by targeting a receptor that directly promotes both conditions.