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Prostanoid receptor EP2 as a therapeutic target

Thota Ganesh1

  • 1Department of Pharmacology, Emory University School of Medicine , 1510 Clifton Road, Atlanta, Georgia, 30322, United States.

Journal of Medicinal Chemistry
|November 28, 2013
PubMed

Insights

Cyclooxygenase-2 (COX-2) inhibitors are ineffective for neurodegenerative diseases and carry cardiovascular risks. Targeting the downstream prostaglandin E2 receptor EP2 offers a new therapeutic avenue for inflammation.

Area of Science:

  • Neuroinflammation
  • Molecular Biology
  • Drug Discovery

Background:

  • Cyclooxygenase-2 (COX-2) is upregulated in various injury models, correlating with disease progression.
  • COX-2 inhibitors show efficacy in pain and inflammation (arthritis, menstrual cramps) but fail in chronic neurodegenerative diseases.
  • Cardiovascular side effects led to the withdrawal of rofecoxib and valdecoxib, necessitating alternative anti-inflammatory strategies.

Purpose of the Study:

  • To explore the prostaglandin E2 receptor EP2 as a novel therapeutic target for inflammatory diseases.
  • To review the role of EP2 in central nervous system (CNS) and peripheral diseases.
  • To discuss EP2 activation mechanisms and small molecule discovery for modulating its function.

Main Methods:

  • Literature review focusing on the role of EP2 in disease pathogenesis.
  • Analysis of EP2 activation pathways and signaling.
  • Overview of small molecule development targeting EP2 for therapeutic intervention.

Main Results:

  • The EP2 receptor is implicated as a pro-inflammatory mediator in diverse CNS and peripheral conditions.
  • Understanding EP2's mechanism of action is crucial for developing targeted therapies.
  • Small molecules are being developed to either enhance or block EP2 function.

Conclusions:

  • Targeting EP2 downstream of COX-2 represents a promising strategy for future anti-inflammatory therapies.
  • Modulating EP2 offers potential benefits for chronic inflammatory and neurodegenerative diseases.
  • Further research into EP2-targeted therapeutics is warranted.

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