2. Academic Validation
  3. Discovery of potent and selective small-molecule PAR-2 agonists

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

Affiliation

  • 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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