Key result
EP4 receptor mediates diverse prostaglandin E2 actions, balancing vasoprotective effects with pro-angiogenic and tumor-promoting roles.
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Review highlights the dual protective and tumor-promoting roles of prostanoid receptor EP4, suggesting diverse therapeutic opportunities for selective agonists and antagonists.
The large variety of biological functions governed by prostaglandin (PG) E2 is mediated by signaling through four distinct E-type prostanoid (EP) receptors. The availability of mouse strains with genetic ablation of each EP receptor subtype and the development of selective EP agonists and antagonists have tremendously advanced our understanding of PGE2 as a physiologically and clinically relevant mediator. Moreover, studies using disease models revealed numerous conditions in which distinct EP receptors might be exploited therapeutically. In this context, the EP4 receptor is currently emerging as most versatile and promising among PGE2 receptors. Anti-inflammatory, anti-thrombotic and vasoprotective effects have been proposed for the EP4 receptor, along with its recently described unfavorable tumor-promoting and pro-angiogenic roles. A possible explanation for the diverse biological functions of EP4 might be the multiple signaling pathways switched on upon EP4 activation. The present review attempts to summarize the EP4 receptor-triggered signaling modules and the possible therapeutic applications of EP4-selective agonists and antagonists.
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Kónya et al. (2013) conducted a review in Conditions related to prostaglandin E2 signaling. EP4-selective agonists and antagonists was evaluated. The EP4 receptor is a versatile mediator of prostaglandin E2 with anti-inflammatory, anti-thrombotic, and vasoprotective effects, as well as tumor-promoting and pro-angiogenic roles.
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