Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)

Yau, Mei-Kwan, Lim, Junxian, Liu, Ligong and Fairlie, David P. (2016) Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015). Expert Opinion on Therapeutic Patents, 26 4: 471-483. doi:10.1517/13543776.2016.1154540

Author Yau, Mei-Kwan
Lim, Junxian
Liu, Ligong
Fairlie, David P.
Title Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)
Journal name Expert Opinion on Therapeutic Patents   Check publisher's open access policy
ISSN 1744-7674
Publication date 2016-03-04
Year available 2016
Sub-type Article (original research)
DOI 10.1517/13543776.2016.1154540
Open Access Status Not Open Access
Volume 26
Issue 4
Start page 471
End page 483
Total pages 13
Place of publication Abingdon, Oxfordshire, United Kingdom
Publisher Taylor & Francis
Collection year 2017
Language eng
Formatted abstract
Introduction: Protease activated receptor 2 (PAR2) is a self-activated G protein-coupled receptor that has been implicated in several diseases, including inflammatory, gastrointestinal, respiratory, metabolic diseases, cancers and others, making it an important prospective drug target. No known endogenous ligands are available for PAR2, so having potent exogenous agonists and antagonists can be helpful for studying physiological functions of PAR2.

Areas covered: This review covers agonist-, antagonist-, antibody- and pepducin-based modulators of PAR2 reported in patent applications between 2010–2015, along with their available structure-activity relationships, biological activities and potential uses for studying PAR2.

Expert opinion: In the last six years, substantial efforts were made towards developing PAR2 modulators, but most lack potency or selectivity or have poor pharmacokinetic profiles. Many PAR2 modulators were assessed by measuring Gαq protein-mediated calcium release in cells. This may be insufficient to fully characterize ligand function, since different ligands signal through PAR2 via multiple signaling pathways. It may be feasible to develop biased ligands as drugs that can selectively modulate one or more specific signaling pathways linking PAR2 to a specific diseased state. Accordingly, potent, orally bioavailable, pathway- and receptor-selective PAR2 modulators may be an achievable goal to realizing effective drugs that can treat PAR2-mediated diseases.
Keyword Protease activated receptor 2 (PAR2)
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: HERDC Pre-Audit
Institute for Molecular Bioscience - Publications
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