Scientists at The Scripps Research Institute (TSRI) have peered deep into the heart of a key protein used in drug design and discovered dynamic structural features that may lead to new ways to target diseases. The protein, called the A2A adenosine receptor (A2aAR), is a member of the G-protein-coupled receptor (GPCR) family, which are the targets of roughly 40 percent of all approved pharmaceuticals.
The new, more detailed image of A2aAR’s signalling mechanism reveals key parts of its inner workings, including an amino acid that acts like a “toggle switch” to control signals across the cell membrane.
“This basic knowledge is potentially helpful for improving drug design,” said Nobel laureate Kurt Wuthrich, PhD, professor of structural biology at TSRI and senior author of the study.
The findings were published today in the journal Cell.
Imaging technique reveals how protein changes shape
All human cells contain A2aAR and other GPCRs embedded in their plasma membrane. More than 800 GPCRs have been discovered in the human body, and each has a role in regulating a bodily function. For example, A2aAR regulates blood flow and inflammation and mediates the effects of caffeine. A2aAR is also a validated target for treating Parkinson’s disease and a relatively new target for targeting cancers.
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