Cellular Gatekeepers Do More than Open Doors for Drugs, UCSF Study Finds

Friday, April 05, 2013

Mark von Zastrow, MD, PhDvon ZastrowUCSF News – April 5, 2013

The cellular gatekeepers that escort the most common pharmaceuticals into our cells continue to work within the cells as well, according to a UC San Francisco discovery that could transform drug design and lead to new ways to treat disease.

Almost half of approved pharmaceuticals — for cancer, heart failure, inflammatory diseases, and others — act through gatekeepers on cell surfaces known as G-protein-coupled receptors (GPCRs). More than 1,000 specific GPCR proteins play roles in nerve signaling, immune responses, sensory perception and many other physiological phenomena governed by the trillions of cells within our bodies.

A team led by UCSF cell biologist Mark von Zastrow, MD, PhD, now has demonstrated that these receptor proteins can remain active longer than expected — even after being pulled into the cell after the attachment of a drug or natural activator. The researchers also demonstrated the value of a new way to study the receptors once they’re inside the cell, one which may shed light on why therapeutics have unexpected effects or varying degrees of effectiveness, according to von Zastrow. The study appeared in the March 28 issue of Nature.


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