BC Innovations | May 23, 2017
Distillery Techniques

Drug platforms

TECHNOLOGY: Structural analyses Crystallographic analyses of a PAR2 variant bound to PAR2 inhibitors could guide the design of therapies for cancer, inflammation and other PAR2-dependent diseases. The PAR2 variant contained point mutations in nine thermostabilizing...
BC Extra | May 1, 2017
Clinical News

Paper identifies MOA of PAR2 antagonists

In a paper published in Nature , researchers at the Heptares Therapeutics Ltd. subsidiary of Sosei Group Corp. (Tokyo:4565) and AstraZeneca plc (LSE:AZN; NYSE:AZN) identified the binding mechanism of two protease-activated receptor 2 (PAR2) antagonists, suggesting...
BC Innovations | Feb 12, 2015
Translation in Brief

Heptares up to PAR2

Heptares Therapeutics Ltd. has solved the long sought-after X-ray structure of Protease-activated receptor ( PAR2 ), a difficult-to-express GPCR that is activated by proteolytic cleavage. Now its partner AstraZeneca plc has used the structure to identify...
BC Innovations | Oct 18, 2012
Distillery Therapeutics

Indication: Neurology

Indication Target/marker/pathway Summary Licensing status Publication and contact information Neurology Pain Protease-activated receptor 2 (PAR2) Rodent studies suggest inhibiting PAR2 signaling could help treat cancer-associated pain. In mice, injection of supernatant from human squamous cell...
BC Innovations | May 12, 2011
Distillery Therapeutics

Indication: Inflammation

This week in therapeutics Indication Target/marker/pathway Summary Licensing status Publication and contact information Inflammation Inflammatory disease Protease-activated receptor 2 (PAR2) In vitro and mouse studies identified a pepducin antagonist of PAR2 that could help treat...
BC Innovations | Jul 16, 2009
Distillery Therapeutics

Indication: Cancer

Indication Target/marker/pathway Summary Licensing status Publication and contact information Cancer Prostate cancer Kallikrein-related peptidase 4 (KLK4); protease-activated receptor 1 (PAR1); PAR2 Studies in cell culture identified a KLK4-selective inhibitor that could be useful for treating...
BC Innovations | Jul 9, 2009
Distillery Therapeutics

Indication: Inflammation

Indication Target/marker/pathway Summary Licensing status Publication and contact information Inflammation Allergy Sphingosine-1-phosphate receptor 1 (S1PR1; S1P1; EDG1); protease-activated receptor 2 (PAR2) Studies in mice suggest that agonizing S1PR1 or PAR2 could help prevent vascular leak...
BioCentury | Sep 30, 2002
Tools & Techniques

The inside scoop in GPCRs

Because G protein-coupled receptors are a validated family of targets and play a role in a wide variety of processes such as cellular metabolism and growth, inflammation, neuronal signaling and blood coagulation, there has been...
BC Week In Review | Jul 2, 2001
Company News

J&J other research news

Researchers at JNJ's R.W. Johnson Pharmaceutical Research and colleagues published in Nature Medicine that local injection of rats' paws with sub-inflammatory doses of PAR2 agonists decreased the pain threshold to thermal insult. The PAR2 agonist-induced...
BC Week In Review | Feb 14, 2000
Company News

University of California other research news

UCSF researchers and colleagues published in Nature Medicine that cleavage of PAR2 on spinal neurons by the proteases trypsin and mast cell tryptase induces the release of proinflammatory neuropeptides . They suggest that the same mechanism...
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