Toward drugs for protease-activated receptor 2 (PAR2)

Yau, Mei-Kwan, Liu, L.igong and Fairlie, David P. (2013) Toward drugs for protease-activated receptor 2 (PAR2). Journal of Medicinal Chemistry, 56 19: 7477-7497. doi:10.1021/jm400638v

Author Yau, Mei-Kwan
Liu, L.igong
Fairlie, David P.
Title Toward drugs for protease-activated receptor 2 (PAR2)
Journal name Journal of Medicinal Chemistry   Check publisher's open access policy
ISSN 0022-2623
Publication date 2013-10-10
Year available 2013
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1021/jm400638v
Open Access Status
Volume 56
Issue 19
Start page 7477
End page 7497
Total pages 21
Place of publication Washington, DC United States
Publisher American Chemical Society
Language eng
Subject 1313 Molecular Medicine
3002 Drug Discovery
Abstract PAR2 has a distinctive functional phenotype among an unusual group of GPCRs called protease activated receptors, which self-activate after cleavage of their N-termini by mainly serine proteases. PAR2 is the most highly expressed PAR on certain immune cells, and it is activated by multiple proteases (but not thrombin) in inflammation. PAR2 is expressed on many types of primary human cells and cancer cells. PAR2 knockout mice and PAR2 agonists and antagonists have implicated PAR2 as a promising target in inflammatory conditions; respiratory, gastrointestinal, metabolic, cardiovascular, and neurological dysfunction; and cancers. This article summarizes salient features of PAR2 structure, activation, and function; opportunities for disease intervention via PAR2; pharmacological properties of published or patented PAR2 modulators (small molecule agonists and antagonists, pepducins, antibodies); and some personal perspectives on limitations of assessing their properties and on promising new directions for PAR2 modulation.
Keyword Breast cancer cells
Thymic stromal lymphopoietin
Intestinal Epithelial Cells
Human endothelial cells
Tissue Factor
Q-Index Code C1
Q-Index Status Confirmed Code
Grant ID 569595
Institutional Status UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Official 2014 Collection
Institute for Molecular Bioscience - Publications
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 25 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 29 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Fri, 29 Nov 2013, 06:29:49 EST by System User on behalf of Institute for Molecular Bioscience