(Press-News.org) ANN ARBOR—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.
John Tesmer, research professor at the U-M Life Sciences Institute and professor in the Department of Pharmacology at the U-M Medical School, and his research team at the Tesmer lab found that paroxetine, a selective serotonin reuptake inhibitor (SSRI) sold under the name Paxil, inhibits G protein-coupled receptor kinase 2 (GRK2), a protein kinase that becomes over-expressed when people have heart failure.
Although so-called "off target" effects are known for many commonly used drugs, this is the first report that identifies a direct link between a specific SSRI and a protein target in the signal system they study, said Kristoff Homan, a postdoctoral fellow in Tesmer's lab.
The paper, "Paroxetine is a Direct Inhibitor of G Protein-Coupled Receptor Kinase 2 and Increases Myocardial Contractility," was published electronically ahead of print on Aug. 21 in ACS Chemical Biology.
The discovery almost did not happen. "It was completely serendipitous," Homan said.
Before beginning a larger search for compounds that would inhibit GRK2, the researchers screened a small library of approximately 2,000 compounds that contains many FDA-approved drugs as a test of their screening procedure—and found that paroxetine binds to and inhibits the activity of GRK2.
GRK2 becomes increasingly expressed as the system that regulates normal heartbeat and the strength of the heart's contractions weakens. Paroxetine, the team found, improved the strength of the heart's contractions in an animal model without interfering with the heart rate.
Paroxetine is FDA-approved and has been clinically used as an SSRI for nearly 30 years, but at prescribed doses the compound probably does not inhibit GRK2 enough to be used for heart failure.
But if the researchers can identify modifications to the chemical structure of paroxetine that improve potency while decreasing SSRI activity, which Homan thinks they can do, the team hopes to start the process of optimization and to develop these compounds into therapeutic leads within the next several years, he said.
###Study: http://pubs.acs.org/doi/abs/10.1021/cb3003013.
Tesmer's lab: www.lsi.umich.edu/facultyresearch/labs/tesmer
Popular antidepressant might prevent heart failure
2012-10-02
ELSE PRESS RELEASES FROM THIS DATE:
Stem cells improve visual function in blind mice
2012-10-02
An experimental treatment for blindness, developed from a patient's skin cells, improved the vision of blind mice in a study conducted by Columbia ophthalmologists and stem cell researchers.
The findings suggest that induced pluripotent stem (iPS) cells – which are derived from adult human skin cells but have embryonic properties – could soon be used to restore vision in people with macular degeneration and other diseases that affect the eye's retina.
"With eye diseases, I think we're getting close to a scenario where a patient's own skin cells are used to replace retina ...
Fluoxetine increases aggressive behavior, affects brain development among adolescent hamsters
2012-10-02
BOSTON, Mass.-- Fluoxetine was the first drug approved by the FDA for major depressive disorder (MDD) in children and adolescents, and to this date, it remains one of only two selective serotonin reuptake inhibitors (SSRIs) registered for treatment of MDD in children and adolescents, despite reports that indicate this class of drugs is associated with side effects, such as agitation, hostility and aggression.
SSRIs have been amongst the most widely prescribed medications in psychiatry for over a decade. While there is a wealth of information regarding their effectiveness ...
Smartphone technology acceptable for telemedicine
2012-10-02
PHOENIX -- A new Mayo Clinic study confirms the use of smartphones medical images to evaluate stroke patients in remote locations through telemedicine. The study, the first to test the effectiveness of smartphone teleradiology applications in a real-world telestroke network, was recently published in Stroke, a journal of the American Heart Association.
"Essentially what this means is that telemedicine can fit in our pockets," says Bart Demaerschalk, M.D., professor of Neurology, and medical director of Mayo Clinic Telestroke. "For patients this means access to expertise ...
Omega-3 supplements may slow a biological effect of aging
2012-10-02
COLUMBUS, Ohio – Taking enough omega-3 fatty acid supplements to change the balance of oils in the diet could slow a key biological process linked to aging, new research suggests.
The study showed that most overweight but healthy middle-aged and older adults who took omega-3 supplements for four months altered a ratio of their fatty acid consumption in a way that helped preserve tiny segments of DNA in their white blood cells.
These segments, called telomeres, are known to shorten over time in many types of cells as a consequence of aging. In the study, lengthening ...
US firms bringing work home from overseas
2012-10-02
EAST LANSING, Mich. — Increasingly, U.S. firms are moving or considering moving their manufacturing operations back to domestic soil from overseas, finds a new study co-authored by a Michigan State University supply chain expert.
Fueling the trend are rising labor costs in emerging countries, high oil prices and increasing transportation costs, global risks such as political instability and other factors, said Tobias Schoenherr.
"Going overseas is not the panacea that it was thought of just a decade or so ago," said Schoenherr, assistant professor in MSU's top-ranked ...
Iowa State researchers study clam shells for clues to the Atlantic's climate history
2012-10-02
AMES, Iowa – Two Iowa State University graduate students are just back from the Gulf of Maine with another big catch of clam shells.
Shelly Griffin and Madelyn Mette recently boarded a lobster boat, dropped a scallop dredge into 30 meters of ocean water and pulled up load after load of Arctica islandica.
"These are the clams that end up in clam chowder," said Alan Wanamaker, an assistant professor of geological and atmospheric sciences in the College of Liberal Arts and Sciences. Wanamaker studies paleoclimatology, the variations and trends of past climates and environments, ...
Researchers harness the immune system to improve stem cell transplant outcomes
2012-10-02
VIDEO:
Dr. Amir Toor from Virginia Commonwealth University Massey Cancer Center's Bone Marrow Transplant program explains a recent clinical trial evaluating a new therapy for multiple myeloma that harnesses the power...
Click here for more information.
Richmond, Va. – (October 1, 2012) – A novel therapy in the early stages of development at Virginia Commonwealth University Massey Cancer Center shows promise in providing lasting protection against the progression of multiple ...
GI societies issue new colonoscopy surveillance guidelines
2012-10-02
Bethesda, MD (Oct. 1, 2012) — Patients at average risk of colorectal cancer who have a clean colonoscopy do not need to repeat the test for 10 years. This and many other practical recommendations for cancer prevention were issued in "Guidelines for Colonoscopy Surveillance After Screening and Polypectomy,"1 a consensus update issued by the U.S. Multisociety Task Force on Colorectal Cancer.
Colorectal cancer is preventable when precancerous polyps (growths) are found and removed before they turn into cancer. Screening for average risk patients is recommended to begin ...
New technologies advance livestock genomics for agricultural and biomedical uses
2012-10-02
MINNEAPOLIS / ST. PAUL (10/01/2012) —New genome editing technologies developed at the University of Minnesota for use on livestock will allow scientists to learn more about human diseases.
The genomic technique, known as TALENS, is described in a report published today in the scientific journal Proceedings of the National Academy of Sciences. The technique is cheaper and faster than previous technologies that allow scientists to genetically modify livestock animals; the animals are used to learn more about human diseases, which in turn can help researchers develop cures. ...
The obese brain may thwart weight loss
2012-10-02
"Betcha can't eat just one!" For obese people trying to lose weight, the Lays potato chip advertising slogan hits a bit too close to home as it describes the daily battle to resist high calorie foods.
But new research by Terry Davidson, director of American University's Center for Behavioral Neuroscience, indicates that diets that lead to obesity—diets high in saturated fat and refined sugar—may cause changes to the brains of obese people that in turn may fuel overconsumption of those same foods and make weight loss more challenging.
"It is a vicious cycle that may ...