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Discovery of Potent and Selective Small-Molecule PAR-2 Agonists

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journal contribution
posted on 25.09.2008, 00:00 by Jimmi Gerner Seitzberg, Anne Eeg Knapp, Birgitte Winther Lund, Sine Mandrup Bertozzi, Erika A. Currier, Jian-Nong Ma, Vladimir Sherbukhin, Ethan S. Burstein, Roger Olsson
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.