Potential small molecule therapeutic for treatment of peripheral inflammation, neurological disorders and carcinogenesis.
- EP2 is a key receptor for cancer progression, peripheral and brain inflammation.
- Lead compound candidates display high EP2 potency and selectivity.
- Compound effectively inhibits inflammation
The inflammatory response is a significant component of the immune system. Both acute and chronic inflammation contribute to well over 10 million cases in the United States. These cases include post-operative cognitive dysfunction (POCD), post-operative delirium, Alzheimer’s disease, traumatic brain injury (TBI), carcinogenesis and many more. Such instances of inflammation have been linked to the activation of EP2 receptor, which promotes inflammation, tumor growth and progression. No other EP2 specific antagonists are on the market and there remains a large unmet need for anti-inflammatory drugs with minimal side effects.
To address the issues involved with targeted cancer therapy and global inhibition of COX enzymes, researchers at Emory University developed potent and selective antagonists - for prostaglandin-E2receptor EP2. Prostaglandin E2 (PGE2) is the dominant enzymatic product of COX-2, and EP2 activation by PGE2 has been shown to promote inflammatory reactions in several tissues including brain. The lead compound candidates display a 5,000-fold selectivity over the highly related EP4 receptor. Due to the ability of the lead compound candidates to prevent inflammation, as well as cancer progression, the potential market extends to patients of various physiological consequences associated with EP2 activation.
- Lead candidates have been identified.
- In vitro and in vivo proof-of-concept (POC) data available
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