Proteinase activated receptor (PAR-2) is a cell surface receptor known to play a critical role in mediating acute and chronic inflammation. EntreMed is developing a peptide that blocks PAR-2 activity, the first such compound identified as a PAR-2 antagonist.
Results of the company’s preclinical studies indicate that its PAR-2 antagonist inhibits both tumor growth and the formation of new blood vessels in cancer models. Additionally, the compound has been shown to be an inhibitor of inflammation in preclinical rheumatoid arthritis and acute inflammation models.
Antagonists of PAR-2 signaling demonstrate a potential relationship between the onset of inflammation and the regulation of tumor growth and angiogenesis.
The PAR-2 program is part of an integrated EntreMed development effort, which is focused on a new generation of multi-mechanism drugs for the treatment of cancer and inflammatory diseases that attack disease cells directly and the blood vessels that nourish them.
“The PAR-2 program is a key component of our pipeline,” said Dr Carolyn Sidor, EntreMed’s vice president and chief medical officer. “We are conducting further studies to understand PAR-2’s mechanisms-of-action, identify additional small molecule PAR-2 antagonists, and determine the potential applications for PAR-2 in oncology and inflammatory diseases.”