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

Authors :: Seitzberg JG
Knapp AE
Lund BW
Mandrup Bertozzi S
Currier EA
Ma JN
Sherbukhin V
Burstein ES
Olsson R
Source :: Journal of medicinal chemistry [J Med Chem] 2008 Sep 25; Vol. 51 (18), pp. 5490-3. Date of Electronic Publication: 2008 Aug 23.
Publication Year :: 2008
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.