Discovery of potent and selective small-molecule PAR-2 agonists

  • J Med Chem. 2008 Sep 25;51(18):5490-3. doi: 10.1021/jm800754r.
Jimmi Gerner Seitzberg  1 ,  Anne Eeg Knapp ,  Birgitte Winther Lund ,  Sine Mandrup Bertozzi ,  Erika A Currier ,  Jian-Nong Ma ,  Vladimir Sherbukhin ,  Ethan S Burstein ,  Roger Olsson
Affiliations
  • 1. ACADIA Pharmaceuticals AB, Medeon Science Park, Per Albin Hanssons Väg 35, S-205 12 Malmö, Sweden.
PMID: 18720984 DOI: 10.1021/jm800754r
Abstract

Proteinase activated receptor-2 plays a crucial role in a wide variety of conditions with a strong inflammatory component. We present the discovery and characterization of two structurally different, potent, selective, and metabolically stable small-molecule PAR-2 agonists. These ligands may be useful as pharmacological tools for elucidating the complex physiological role of the PAR-2 receptors as well as for the development of PAR-2 antagonists.

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