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