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October 10, 2012

2012 Nobel Prize in Chemistry for Work on Cell Receptors

2012 Nobel Prize in Chemistry for Work on Cell ReceptorsThe 2012 Nobel prize in chemistry has been awarded to Robert Lefkowitz of the Howard Hughes Medical Institute and Duke University in Durham, US, and Brian Kobilka of Stanford University, US, for "studies of G-protein coupled receptors" (GPCRs). Such receptors let body cells sense and respond to outside signals such as light, danger, odor or the flavor of food. "GPCRs mediate most of the physiologic responses to hormones and neurotransmitters", Kobilka told ChemPhysChem. "They are also fascinating membrane proteins from a basic science perspective. We hope that our research will translate into safer and more effective therapeutics."

Each cell in the body has tiny receptors that enable it to sense its environment, so that it can adapt to new situations. However, for many years, it remained unclear how the cells could "communicate" with the outside world. Scientists knew that hormones, such as adrenalin, had powerful effects on the body –and they suspected that cell surfaces should contain some kind of recipient for these hormones– but they didn't know exactly what they looked like or how they acted. Thanks to the work of Lefkowitz and Kobilka, we now know what these receptors are, how they are built and how they act. "They work as a gateway to the cell," Lefkowitz told a news conference in Stockholm by phone. "As a result they are crucial... to regulate almost every known physiological process with humans."

There are many known GPCRs in the human body. Some of them allow us to distinguish between different smells and flavors, others regulate important biological processes, and others control our body's reaction to hormones and neurotransmitters such as adrenalin, histamine, dopamine or serotonin.

Using radioactivity, Lefkowitz managed to unveil several receptors in 1968, including the receptor for adrenaline. With these first results, he and his team started to understand how such receptors work. In the 1980s, shortly after Kobilka had joined Lefkowitz' group, the US researchers made a second important discovery: They found that there is a whole family of receptors that look alike and function in the same manner –a family that is now called G-protein-coupled receptors.

In 2011, Kobilka achieved another breakthrough when his team captured an image of the receptor for adrenaline at the moment when it was being activated by a hormone and was sending a signal into the cell. "This image is a molecular masterpiece –the result of decades of research", said the Royal Swedish Academy of Sciences in a press release.

The studies carried out by Lefkowitz and Kobilka are key for developing better drugs, and the 2012 Nobel Prize in Chemistry is a well-deserved recognition for the two scientists. "I'm very happy and honored to be sharing the prize with Professor Lefkowitz", Kobilka said. About 50% of all medications (including beta blockers and antihistamines) act on these receptors so learning about them will be of great help in pharmaceutics and medicinal chemistry.

Image: Nobel Medal (© ® The Nobel Foundation). Source and further information at www.nobelprize.org. Read a related article in ChemistryViews.

Kira Welter

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