title: Discovery of potent and selective small-molecule PAR-2 agonists.
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.
authors: ACADIA Pharmaceuticals AB, Medeon Science Park, Per Albin Hanssons Väg 35, S-205 12 Malmö, Sweden.
authors: Jimmi Gerner
authors: JG
authors: Seitzberg
authors: Anne Eeg
authors: AE
authors: Knapp
authors: Birgitte Winther
authors: BW
authors: Lund
authors: Sine
authors: S
authors: Mandrup Bertozzi
authors: Erika A
authors: EA
authors: Currier
authors: Jian-Nong
authors: JN
authors: Ma
authors: Vladimir
authors: V
authors: Sherbukhin
authors: Ethan S
authors: ES
authors: Burstein
authors: Roger
authors: R
authors: Olsson
mesh_terms: D015195:Drug Design; D006801:Humans; D044464:Receptor, PAR-2 / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D044464:Receptor, PAR-2