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Prostaglandin E2 receptors in bone formation

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Abstract

Prostaglandins, PGE2 in particular, have diverse actions on various organs, including inflammation, bone healing, bone formation, embryo implantation, induction of labour and vasodilatation, among others. However, systemic side effects have limited their clinical utility. The pharmacological activities of PGE2 are mediated through four G protein-coupled receptor subtypes, EP1–EP4. Recent studies have shown that EP2 and EP4 receptors play important roles in regulating bone formation and resorption. EP2 and EP4 receptor-selective agonists have been shown to stimulate local or systemic bone formation, augment bone mass and accelerate the healing of fractures or bone defects in animal models upon local or systemic administration, thus, potentially offering new therapeutic options for enhancing bone formation and bone repair in humans. This review will focus on the studies related to bone formation and bone healing in the EP receptor knockout (KO) mice and the EP2 or EP4 receptor-selective agonist treated animal models.

Résumé

Les prostaglandines en particulier la PGE2 ont des actions relativement diverses sur différents organes, notamment en termes d’inflammation, de réparation osseuse, de régénération osseuse, d’implantation embryonnaire, d’induction du travail et de vasodilatation. Ces études ont montré que les récepteurs EP2 et EP4 avaient donc un rôle important dans la régulation de formation osseuse et dans sa résorption. On a pu démontrer que les récepteurs EP2 et EP4 stimulaient de façon locale ou systémique la formation osseuse, augmentaient la masse osseuse et accéléraient la guérison des fractures ou la réparation des défects osseux chez les animaux. Ceci nous offre un nouveau potentiel thérapeutique concernant l’amélioration de la régénération osseuse et la réparation des lésions osseuses chez l’homme. Cette revue permet de mettre en valeur les études relatives à la formation et à la cicatrisation osseuse avec le récepteur EP chez la souris et les récepteurs ajustés EP2, EP4 chez les animaux modèles.

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Authors and Affiliations

  1. Pfizer Global Research and Development, Groton Laboratories, Mail Stop 8118W-208, Groton, CT, 06340, USA

    M. Li & V. M. Paralkar

  2. Pfizer Global Research and Development, Groton Laboratories, Mail Stop 6025-A4235, New London, CT, 06320, USA

    D. D. Thompson

Authors
  1. M. Li
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  2. D. D. Thompson
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  3. V. M. Paralkar
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Correspondence to M. Li or V. M. Paralkar.

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Li, M., Thompson, D.D. & Paralkar, V.M. Prostaglandin E2 receptors in bone formation. International Orthopaedics (SICO 31, 767–772 (2007). https://doi.org/10.1007/s00264-007-0406-x

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  • DOI: https://doi.org/10.1007/s00264-007-0406-x

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