G Protein Coupled Receptor News and Research

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Paroxetine shows promise against heart failure

A medication usually used to help treat depression and anxiety disorders has the potential to help prevent heart failure, according to researchers at the University of Michigan.

2 Oct 2012

Heptares uses StaR technology to solve structure of CRF-1 receptor

Heptares Therapeutics today announces that it has used its StaR technology to solve entirely in-house the first structure of a Family B sub-class G protein-coupled receptor (GPCR).

10 Sep 2012

Trevena to present TRV027 Phase 1 clinical data at 16th Annual Heart Failure Society of America Meeting

Trevena, Inc., the leader in the discovery of G-protein coupled receptor (GPCR) biased ligands, today announced that it is presenting a poster featuring Phase 1 clinical data on TRV027 at the 16th Annual Heart Failure Society of America Meeting being held in Seattle, WA, September 9th-12th. Trevena is developing TRV027 for the treatment of acute decompensated heart failure.

7 Sep 2012

Researchers identify brain receptor that appears to play a central role in regulating appetite

Researchers at Columbia University Medical Center (CUMC) have identified a brain receptor that appears to play a central role in regulating appetite. The findings, published today in the online edition of Cell, could lead to new drugs for preventing or treating obesity.

8 Jun 2012

GPR21 inhibitors may hold promise for diabetes

In recent years, a growing body of evidence has linked inflammation to the development of insulin resistance. In insulin resistance, the hormone insulin is less effective in promoting glucose uptake from the bloodstream into other tissues. Obesity is a major factor that contributes to insulin resistance, which can eventually lead to type 2 diabetes. Previous studies have shown that proinflammatory molecules found in fat tissue decreases sensitivity of tissues to insulin.

2 Jun 2012

Expression of specific GPCRs appears to play a role in prognosis of CLL

Researchers at the University of California-San Diego School of Medicine have shown that G protein-coupled receptor expression may predict the prognosis of patients with chronic lymphocytic leukemia. Their findings may identify new ways to treat such patients.

25 Apr 2012

Heptares exercises exclusive option to license new A2A antagonist for CNS disorders

Heptares Therapeutics, the leading GPCR drug discovery company, announces that an operating company of Shire PLC, the global specialty biopharmaceutical company, has exercised its exclusive option to license a novel adenosine A2A antagonist discovered by Heptares that is currently in preclinical development.

20 Mar 2012

TAK-875 - an emerging therapy for Type 2 diabetes

In a trial of 426 patients with Type 2 diabetes, TAK-875 reduced blood sugar below a pre-determined level in as much as 48 percent of those receiving it after 12 weeks, compared with 40 percent of those who took glimepiride, the older drug, according to findings published online by The Lancet medical journal. The research was presented in June at the American Diabetes Association’s annual meeting in San Diego.

28 Feb 2012

TAK-875 as effective as glimepiride in treating type 2 diabetes

TAK-875, a new treatment for type 2 diabetes, improves blood sugar control and is equally effective as glimepiride, but has a significantly lower risk of creating a dangerous drop in blood sugar, called hypoglycemia, according to a new study.

27 Feb 2012

New drug improves glycaemic control with minimum risk of hypoglycemia in type 2 diabetics

27 Feb 2012

Study underscores power of real-time cell monitoring to dissect pluridimensionality of GPCR signaling

A research team led by Dr. Michel Bouvier at the Institute for Research in Immunology and Cancer (IRIC) of the University of Montreal in Quebec, used the Roche xCELLigence SP Instrument to measure changes in cell response following ligand stimulation.

From Roche Sequencing and Life Science 16 Feb 2012

Trevena commences TRV130 Phase I clinical trial for severe post-operative pain

Trevena, Inc., the leader in discovery and development of G-protein coupled receptor (GPCR) biased ligands, announced today the initiation of a Phase I clinical trial of TRV130, a novel candidate designed for the intravenous treatment of moderate-to-severe post-operative pain.

13 Feb 2012

Researchers discover function and expression of CD97 in malignant gliomas

Researchers at Virginia Commonwealth University Medical Center's VCU Massey Cancer Center and Harold F. Young Neurosurgical Center and Old Dominion University have discovered that suppression of Wilms tumor 1 protein (WT1) results in downregulation of CD97 gene expression in three glioblastoma cell lines and reduces the characteristic invasiveness exhibited by glial tumor cells.

8 Feb 2012

Penn research group receives NCI grant to establish BETRNet

A research group at the Perelman School of Medicine of the University of Pennsylvania, led by John Lynch, MD, PhD, assistant professor of Medicine in the Division of Gastroenterology, has received a National Cancer Institute (NCI) grant to establish a Barrett's esophagus translational research network (BETRNet) with Columbia University and the Mayo Clinic.

4 Nov 2011

Simmons Center to evaluate CGEN-25009 for treatment of idiopathic pulmonary fibrosis

Compugen Ltd. and the Pulmonary Fibrosis Foundation announced today that the Pulmonary Fibrosis Foundation will provide a grant to scientists at the University of Pittsburgh Dorothy P. and Richard P.

13 Oct 2011

Study: Protein's structural arrangement can change its signaling function

In a joint study, scientists from the California and Florida campuses of The Scripps Research Institute have shown that changes in a protein's structure can change its signaling function and they have pinpointed the precise regions where those changes take place.

8 Sep 2011

Researchers influence activity of nerve cells with laser light

Unlike conventional methods, with the so-called optogenetics, the researchers are able to target one cell type. "We are now going to use this method to find out exactly what goes wrong in the nerve cells in movement disorders such as ataxias", said Prof. Dr. Stefan Herlitze.

21 Jul 2011

Roche RTCA HT Instrument allows fully-automated impedance screens for GPCRs

Label-free technologies have entered the stage of cellular drug discovery and high-throughput screening (HTS). For the measurement of G protein-coupled receptor (GPCR) activation electrical impedance represents an excellent universal readout technology, since different signaling pathways can be measured in one assay format using recombinant as well as primary cells.

17 Jun 2011

New targeted therapy may halt tumor growth in men with advanced prostate cancer

A new targeted therapy for prostate cancer halts tumor growth in animals with advanced prostate cancer that is resistant to hormone therapy, a new study finds. The results will be presented Saturday at The Endocrine Society's 93rd Annual Meeting in Boston.

6 Jun 2011

Heptares, Shire sign deal to develop novel A2A antagonist for CNS disease treatment

Heptares Therapeutics today announced it has signed an exclusive option agreement with Shire Pharmaceuticals for a novel adenosine A2A antagonist discovered by Heptares and currently in preclinical development.

9 May 2011