Potent small agonists of protease activated receptor 2

Yau, Mei-Kwan, Suen, Jacky Y., Xu, Weijun, Lim, Junxian, Liu, Ligong, Adams, Mark N., He, Yaowu, Hooper, John D., Reid, Robert C. and Fairlie, David P. (2016) Potent small agonists of protease activated receptor 2. ACS Medicinal Chemistry Letters, 7 1: 105-110. doi:10.1021/acsmedchemlett.5b00429

Author Yau, Mei-Kwan
Suen, Jacky Y.
Xu, Weijun
Lim, Junxian
Liu, Ligong
Adams, Mark N.
He, Yaowu
Hooper, John D.
Reid, Robert C.
Fairlie, David P.
Title Potent small agonists of protease activated receptor 2
Journal name ACS Medicinal Chemistry Letters   Check publisher's open access policy
ISSN 1948-5875
Publication date 2016
Year available 2015
Sub-type Article (original research)
DOI 10.1021/acsmedchemlett.5b00429
Open Access Status Not Open Access
Volume 7
Issue 1
Start page 105
End page 110
Total pages 6
Place of publication Washington, DC, United States
Publisher American Chemical Society
Collection year 2016
Language eng
Formatted abstract
Many proteases cut the PAR2 N-terminus resulting in conformational changes that activate cells. Synthetic peptides corresponding to newly exposed N-terminal sequences of PAR2 also activate the receptor at micromolar concentrations. PAR2-selective small molecules reported here induce PAR2-mediated intracellular calcium signaling at nanomolar concentrations (EC50 = 15–100 nM, iCa2+, CHO-hPAR2 cells). These are the most potent and efficient small molecule ligands to activate PAR2-mediated calcium release and chemotaxis, including for human breast and prostate cancer cells.
Keyword Protease activated receptor 2
Structure−activity relationships
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Mater Research Institute-UQ (MRI-UQ)
Official 2016 Collection
Institute for Molecular Bioscience - Publications
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Citation counts: TR Web of Science Citation Count  Cited 0 times in Thomson Reuters Web of Science Article
Scopus Citation Count Cited 2 times in Scopus Article | Citations
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Created: Wed, 09 Dec 2015, 08:01:16 EST by Susan Allen on behalf of Institute for Molecular Bioscience