Researchers believe they have found a way to change the action of 60 percent of currently available medications, in some cases making them many times more effective, according to an article published in the April 21 edition of the journal Science. The discovery has the potential to improve treatments for diseases including heart disease, cancer, diabetes, depression and arthritis. The study describes a new way to manipulate perhaps the most important signaling mechanism in human cells: G-protein coupled receptors (GPCRs).

Human cells must be able to send signals that switch life processes on and off as they react to the nutrients, toxins, hormones and even the light particles they are exposed to. GPCRs are a key part of such signaling cascades, passing on messages that make vision possible, carry nerve messages, enable white blood cells to attack infection and set the timing of the heartbeat. Faulty GPCR signaling, on the other hand, plays a key role in several major diseases. As a result, GCPRs are targeted by 12 of the top 20 selling drugs, including Coreg for congestive heart failure, Cozaar for high blood pressure, Zoladex for breast cancer, Buspar for anxiety and Clozaril for schizophrenia, as well as by Zantac and Claritin. Together the drug class accounts for $200 billion in annual sales.

Authors of the current study believe they have found a new way to regulate the same GCPR pathways, but at different points. Where most drugs change the behavior of GPCRs on the outside of cells, the new class of drugs seeks to influence related signaling on the inside. Early studies suggest that the newly discovered "drug candidates" can provide better control of pathways involved in pain relief, inflammation and heart disease, while leaving healthy functions in place.

"We believe we have discovered a new class of drugs that could make current drugs more effective, but that also represents a completely new, independent way of treating the same diseas
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Contact: Greg Williams
Greg_Williams@urmc.rochester.edu
585-273-1757
University of Rochester Medical Center
20-Apr-2006

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