AI Article Synopsis
- Prostaglandin E (PGE) plays a crucial role in driving inflammation in arthritic conditions, necessitating the use of inhibitors like NSAIDs and Coxibs for treatment, which can cause significant side effects.
- Researchers aim to find new EP4 antagonists that target inflammation and autoimmunity associated with PGE, potentially offering a safer alternative to traditional treatments.
- Several novel EP4 antagonists have been discovered through various in vitro assays, demonstrating selectivity and potency, and have shown effectiveness in animal models for treating pain, inflammation, and arthritis.
Article Abstract
Prostaglandin (PG) E is the key driver of inflammation associated with arthritic conditions. Inhibitors of PGE production (NSAIDs and Coxibs) are used to treat these conditions, but carry significant side effect risks due to the inhibition of all prostanoids that play important physiological function. The activities of PGE are transduced through various receptor sub-types. Prostaglandin E type 4 receptor (EP4) is associated with the development of inflammation and autoimmunity. We therefore are interested in identifying novel EP4 antagonists to treat the signs and symptoms of arthritis without the potential side effects of PGE modulators such as NSAIDs and Coxibs. Novel EP4 antagonists representing distinct chemical scaffolds were identified using a variety of in vitro functional assays and were shown to be selective and potent. The compounds were shown to be efficacious in animal models of analgesia, inflammation, and arthritis.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5464344 | PMC |
| http://dx.doi.org/10.1002/prp2.316 | DOI Listing |
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