Washington, October 2 (ANI): Paroxetine, 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 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.