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Potent Small Agonists of Protease Activated Receptor 2.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2015 Nov 30; Vol. 7 (1), pp. 105-10. Date of Electronic Publication: 2015 Nov 30 (Print Publication: 2016). - Publication Year :
- 2015
-
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, iCa(2+), 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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 7
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26819675
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.5b00429