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12:00 AM, Aug 17, 2015  |  BioCentury | Product Development

Structure knows best

to Heptares co-founder, Chairman and CEO Malcolm Weir, the unit built its StaR platform for GPCR
more amenable for development in the clinic," he said. StaR uses point mutations to stabilize GPCRs …
used in either high throughput screening or X-ray crystallography to determine their structure. Without stabilization, GPCRs …
12:00 AM, May 13, 2013  |  BioCentury | Product Development

An association for dissociation

acute setting, as well as the development of additional programs based on biased interaction with GPCRs …
based on the theory that ligands that selectively activate or antagonize signaling pathways downstream of GPCRs …
could have a better therapeutic index than traditional GPCR-targeting molecules. That's because biased ligands are screened …
12:00 AM, Aug 22, 2011  |  BioCentury | Product Development

Beta testing GPR40

dead, while 30% are either functional or non-responsive cells. GPR40 is a G protein-coupled receptor (GPCR
12:00 AM, Jun 20, 2011  |  BioCentury | Product Development

Broadening immunology's reach

of the histamine H4 receptor ( HRH4 ; H4) in early development. H4 is a GPCR
12:00 AM, Aug 23, 2010  |  BioCentury | Product Development

Gamma no-go

APP" than directly hitting gamma secretase's active site. Fischer noted that GPR3 is an orphan GPCR
12:00 AM, Jan 14, 2008  |  BioCentury | Product Development

Have signal; want potency

to as 19AJ but J&J preferred to call GDIR, is an orphan G protein-coupled receptor (GPCR
12:00 AM, Mar 26, 2007  |  BioCentury | Product Development

Metabolic Milestones

moving through the clinic that antagonize the cannabinoid CB1 receptor , a G protein-coupled receptor (GPCR
12:00 AM, May 15, 2006  |  BioCentury | Product Development

PPAR plus

Mouney, co-founder, chairman and CEO. "We've shown in animals that it also acts on a GPCR
12:00 AM, Feb 06, 2006  |  BioCentury | Product Development

Breathless opportunities

been linked to the recruitment of inflammatory cells through activation of chemokine G protein-coupled receptors (GPCRs …
D2 receptor . PGD2, more commonly known as chemoattractant receptor homolog CRTH2 , is a GPCR
unit of Johnson & Johnson (JNJ, New Brunswick, N.J.), to develop oral antagonists against a GPCR
12:00 AM, May 09, 2005  |  BioCentury | Product Development

Plucking from pharma

stomach. Its mechanism of action is poorly understood, according to Geesaman. "Its receptor is a GPCR