G Protein Coupled Receptor News and Research

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Caliper Discovery Alliances and Services receives a $1.8M funding commitment for the EPA's ToxCast program

Caliper Life Sciences, Inc., a leading provider of tools and services for drug discovery and life sciences research, today announced that its Caliper Discovery Alliances and Services (CDAS) unit has been awarded a new funding commitment for $1.8 million under its contract with the Environmental Protection Agency (EPA) for the EPA's ToxCast screening program.

9 Nov 2009

NIH awards Trevena $7.65M Grand Opportunity grant

Trevena Inc., a leader in the discovery of G-protein coupled receptor (GPCR) biased ligands announced today that it was awarded a $7.65 million Grand Opportunity (GO) Grant by the office of the director of the National Institutes of Health (NIH). This grant will further fund Trevena’s work to identify and characterize functionally selective biased ligands for a wide range of GPCRs.

3 Nov 2009

Positive results from Metabolex' Phase 1 MBX-2982 clinical trial for treating type 2 diabetes

Metabolex, Inc., a biopharmaceutical company focused on the discovery and development of proprietary new medicines for the treatment of metabolic diseases, announced positive results from two multiple ascending dose Phase 1 clinical trials of MBX-2982.

14 Oct 2009

Heptares Therapeutics to apply its StaR technology to generate novel drug leads against GPCR target

Heptares Therapeutics Ltd, the drug discovery company focused on G-protein-coupled receptor (GPCR) targets, announced today that it has entered into an option agreement with the Novartis Option Fund under which Heptares will apply its proprietary StaR(TM) technology to generate novel drug leads against a nominated, unspecified GPCR target of interest to Novartis.

12 Oct 2009

New mechanism of bone formation may help fight osteoporosis

The natural cycle of building bone to maintain skeletal strength and then breaking it down for the body's calcium needs is delicately balanced, but diseases like osteoporosis break down too much bone without adequate bone replacement, leading to bone fractures.

8 Oct 2009

Paper discussing the mechanism of the selective TGR5 agonist INT-777 published in Cell Metabolism

Bile acids are known to be key regulators of lipid, glucose and overall energy metabolism. Bile acid activation of the G protein-coupled receptor TGR5 has been shown to induce energy expenditure in muscle and brown fat, thereby conferring resistance to weight gain.

2 Sep 2009

Niacin findings could open up new avenues for drug discovery

Deft molecular detective work at Duke University Medical Center suggests that scientists may soon be able to resurrect niacin as one of the best and cheapest ways to manage cholesterol.

6 Apr 2009

Long-term gene therapy used to reverse heart damage in heart failure

Long-term gene therapy resulted in improved cardiac function and reversed deterioration of the heart in rats with heart failure, according to a recent study conducted by researchers at Thomas Jefferson University's Center for Translational Medicine.

30 Dec 2008

Many receptor models used in drug design may not be useful after all

It may very well be that models used for the design of new drugs have to be regarded as impractical. This is the sobering though important conclusion of the work of two Leiden University scientists published in Science this week.

5 Oct 2008

New gene discovered that determines hair texture and density in humans

A Columbia University Medical Center research team has discovered a new gene involved in determining hair texture in humans.

26 Feb 2008

Discovery of 'overdrive' protein could broaden drug design options

New research by scientists at the University of North Carolina at Chapel Hill shows for the first time that an important family of proteins known to function at the cell surface also functions at a site within the cell.

13 Feb 2008

Kisspeptin and GPR54 may be the future of ovarian cancer treatment

Kisspeptin and its receptor GPR54 predict a favourable clinical outcome in women with ovarian carcinoma, and are specific for the clear cell carcinoma subtype, research published this week in the online open access journal, BMC Medicine, reveals.

16 Nov 2007

Stanford researchers get precise picture of cell target for drugs

More than half of all drugs given to patients work by targeting a particular type of "docking station," or receptor, found on body cells, to steer the cell's machinery toward healing an illness.

25 Oct 2007

How does the opioid system work?

The opioid system controls pain, reward and addictive behaviors. Opioids exert their pharmacological actions through three opioid receptors, mu, delta and kappa whose genes have been cloned (Oprm, Oprd1 and Oprk1, respectively).

15 Oct 2007

Testes offer a promising new source of stem cells

After a decade of research, Howard Hughes Medical Institute scientists have succeeded in reprogramming adult stem cells from the testes of male mice into functional blood vessels and contractile cardiac tissue.

20 Sep 2007

Nitric oxide may be the key to why specific drugs for heart failure or asthma lose their effectiveness over time

A naturally occurring molecule in the body appears to control whether certain medications, such as beta adrenergic receptor agonists used in acute heart failure or in inhalers for asthma, lose their effectiveness over time.

4 May 2007

Researchers finds meth receptor that could lead to therapy

A recently discovered signaling system in the brain has just been shown to be turned on by methamphetamine, an Oregon Health & Science University study found.

19 Apr 2007

Estrogen improves host response after traumatic injury

Researchers have identified the receptor pathway used by estrogen to decrease liver injury after trauma and hemorrhage.

2 Apr 2007

Enzyme discovery could reduce Kaposi sarcoma tumour growth and lead to drugs suitable for treating other viral cancers

A report in the Journal of Biological Chemistry shows that inhibition of heme oxygenase-1, an enzyme involved in iron metabolism, reduces Kaposi sarcoma tumor growth. This discovery could result in the production of new drugs to treat this and other viral cancers.

28 Apr 2006

Novel compound may help fight obesity

A new study reveals an attractive new target for therapies aimed at the treatment of obesity and related metabolic disorders, researchers report in the March Cell Metabolism.

9 Mar 2006