In:
Pharmacology Research & Perspectives, Wiley, Vol. 5, No. 3 ( 2017-06)
Abstract:
Prostaglandin ( PG ) E 2 is the key driver of inflammation associated with arthritic conditions. Inhibitors of PGE 2 production ( NSAID s 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 2 are transduced through various receptor sub‐types. Prostaglandin E 2 type 4 receptor ( EP 4) is associated with the development of inflammation and autoimmunity. We therefore are interested in identifying novel EP 4 antagonists to treat the signs and symptoms of arthritis without the potential side effects of PGE 2 modulators such as NSAID s and Coxibs. Novel EP 4 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.
Type of Medium:
Online Resource
ISSN:
2052-1707
,
2052-1707
DOI:
10.1002/prp2.2017.5.issue-3
Language:
English
Publisher:
Wiley
Publication Date:
2017
detail.hit.zdb_id:
2740389-0
SSG:
15,3
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