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Designing Better Blood Pressure Drugs

An experiment at the Department of Energy's SLAC National Accelerator Laboratory led by Vadim Cherezov, a chemistry professor at the University of Southern California, has revealed in atomic detail how a hypertension drug binds to a cellular receptor that plays a key role in regulating blood pressure. The results could help scientists design new drugs that better control blood pressure while limiting side effects. The research was done at SLAC's Linac Coherent Light Source (LCLS) X-ray laser, a DOE Office of Science User Facility. The results were published in the May 7th 2015 issue of Cell.

A release from the university explains that the research focused on a type of drug known as an ARB, or angiotensin receptor blocker. Used by millions of people each year, ARBs are designed to block a receptor in cell membranes so it cannot bind with angiotensin II, a hormone that induces the constriction of blood vessels, causing an increase in blood pressure.

The release quotes Cherezov as saying, "Many ARBs have been developed, but the interaction between the drug and the receptor has been unknown at the atomic level. Now we have determined the structure of the joined ARB and receptor in atomic detail, and we have shown that all of the previous molecular models – the best guesses for how they fit together – were wrong in many important details. These results can be used to design other types of compounds and predict how they will bind to the receptors."

Fighting a 'Silent Killer'

About three in 10 U.S. adults suffer from hypertension, or high blood pressure, and about 75 percent of them take prescribed medication to treat it. Hypertension is a major risk factor for heart disease and stroke, the leading causes of death in the U.S., and it is known as a "silent killer" because there may be no outward symptoms.

"Everybody would like to find the agent or mechanism to more actively and efficiently control blood pressure," said Dr. Stanley G. Rockson, professor of cardiovascular medicine at the Stanford School of Medicine. "If we can understand the molecular mechanisms better, and come up with a targeted drug that's more effective, we can streamline therapy."

ARBs are a multibillion-dollar industry, with fewer side effects than some other hypertension medications. But because their effectiveness at higher doses may be limited, they are often used in combination with other drugs, complicating treatment when patients fail to follow the complete regimen, Rockson said. The development of a single, more effective drug would help.

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