Ladies and Gentleman, the winners have been announced!

Robert J. Lefkowitz (left) and Brian K. Kobilka (right)
At 2:30AM this morning in California, the recipients of the Nobel Prize in Chemistry were called and informed of their accomplishments. Robert J. Lefkowitz, 69, and Brian K. Kobilka, 57, have discovered the molecular workings and structures of G protein-coupled receptors (GPCRs). GPCRs are a family of proteins that have been discovered to be the transmitters of critical biological messages for functions such as vision, smell, taste, and neurotransmission.

The two men set out on their scientific journey in an attempt to understand the biological processes that occur during a body’s production of stress hormones, such as adrenaline. Science already uncovered what happens to a person when the hormones are produced; a receptor is bound by the hormone and then a person experiences focused vision, quickened breathing, diverting blood from the less important body systems etc. The groundbreaking aspect of Lefkowitz and Kobilka’s findings is that the nature of the receptors for these hormones are now known.

Lefkowitz first traced the signaling of these receptors in the 1970s with radioactive blocking agents attached to hormones. By marking the hormones, Lefkowitz was able to follow where they attached in the body and observe the activities of the receptors they attached to. With much effort, Dr. Lefkowitz was able to identify the receptor proteins and prove they were specific molecules.

In the 1980s, Lefkowitz’s group at Duke University, which Kobilka was a part of, found the gene that actually produced one of the protein receptors. The group saw that the shape of the protein had many long spirals that wove through the cell membrane exactly seven times.

3D image of rhodopsin.
Realizing that the receptor he discovered had the same characteristic seven helicies as another receptor that had been found in the retina, in this case the light receptor rhodopsin, Lefkowitz and his team set out to find several other similar receptors that were found to be in a family of receptors, called the G protein-coupled receptors. Today, about a thousand of these GPCRs are known. They reside on the surface of cells and react to a host of hormones and neurotransmitters. Dr. Kobilka moved to Stanford and progressed to determine the three-dimensional structure of the GPCRs, which involved the utilization of x-ray crystallography.
“We hope by knowing the three-dimensional structure we might be able to develop more selective drugs and more effective drugs,” Dr. Kobilka said. The ultimate goal with all this new information is to refine drug design. Many drug molecules attach to cells, not only at the intended target, but also to other receptors.  This may help eliminate those unwanted side effects that one experiences when taking certain drugs.