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 usef...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2008-09, Vol.51 (18), p.5490-5493
Main Authors: Seitzberg, Jimmi Gerner, Knapp, Anne Eeg, Lund, Birgitte Winther, Mandrup Bertozzi, Sine, Currier, Erika A, Ma, Jian-Nong, Sherbukhin, Vladimir, Burstein, Ethan S, Olsson, Roger
Format: Article
Language:English
Subjects:
Biological and medical sciences
Drug Design
Humans
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
Receptor, PAR-2 - agonists
Structure-Activity Relationship
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm800754r