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2:45 PM, Jul 13, 2017  |  BC Innovations | Targets & Mechanisms

Insider signaling

only in the endosome, the partners want to lead the way in rethinking targeting of GPCRs …
The findings could not only open the door to a new class of inhibitors for GPCRs …
non-opioid analgesics is gaining national attention. The idea of endosomal signaling goes against the canonical GPCR
12:00 AM, Sep 15, 2016  |  BC Innovations | Targets & Mechanisms

KOR-recting MS

Francisco , used an unbiased approach, implementing a screening strategy to identify G protein-coupled receptors (GPCRs …
promoting myelin repair. Kappa clusters In the UCSF study, Chan's team screened 250 compounds targeting GPCRs …
said the computational method used by his collaborators to find PZM21 should work for any GPCR
12:00 AM, Sep 01, 2016  |  BC Innovations | Targets & Mechanisms

Biased against pain

he said, adding the findings "open up the possibility of ultimately doing this with every GPCR
underscore the importance of generating the crystal structures required for the program. "As structures of GPCRs …
very useful." So far, he said, researchers have crystallized only about 7% of all the GPCRs …
12:00 AM, Jan 22, 2015  |  BC Innovations | Targets & Mechanisms

Pseudo-allergy exposed

to drugs. To find the cause of pseudo-allergic reactions, Dong's group focused on MRGPRX2, a GPCR
had normal reactions to IgE and endothelin - a hormone that acts via an unrelated GPCR
suggested deletion of MRGPRX2 eliminated the IgE-independent reaction, but did not affect general antibody and GPCR
12:00 AM, Oct 17, 2013  |  BC Innovations | Targets & Mechanisms

HER2's outside help

studies have shown that HER2 and other EGFRs can be activated by a variety of GPCRs …
Dana-Farber Cancer Institute , has found that HER2 can be activated in vivo by another GPCR-neurokinin …
finding is the most clear-cut example to date for cross-activation of EGFR family members by GPCRs …
12:00 AM, Sep 26, 2013  |  BC Innovations | Targets & Mechanisms

Hedgehog battles Down syndrome

corrected by transient treatment with a small molecule activator of smoothened ( SMO ), a GPCR
12:00 AM, Dec 06, 2012  |  BC Innovations | Targets & Mechanisms

Thinking outside the amyloid box

broad-spectrum inhibitors. In 2009, De Strooper and researchers at Galapagos N.V. reported that an orphan GPCR
12:00 AM, Jul 19, 2012  |  BC Innovations | Targets & Mechanisms

OutFOXing tumors

resurrected to treat anti-EGFR-resistant cancers." Because dopamine receptors are a subclass of G protein-coupled receptors (GPCRs …
Narla said the repurposing search could be far-reaching. "Compounds that target dopamine receptors or GPCRs might …
that are just sitting on the shelf because they had shown a suboptimal profile as GPCR
12:00 AM, Aug 18, 2011  |  BC Innovations | Targets & Mechanisms

EBI2: the race is on

converging on an autoimmune target called EBI2 and are starting to flesh out the orphan GPCR's …
1 Moving toward models Researchers now need to explore the therapeutic potential of targeting the GPCR
12:00 AM, Aug 12, 2010  |  BC Innovations | Targets & Mechanisms

The GPCR-cancer connection

at Genentech, now has sequenced 1,507 cancer-associated or druggable genes, including 156 G protein-coupled receptors (GPCRs …
are emerging as important classes of genomic alterations"-are not detected by the sequencing approach employed. GPCRs …
identification of 35 additional significantly altered genes. This list of candidate cancer genes includes 19 GPCRs …

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