Nobel Prize in Chemistry Awarded for Research into GPCRs

The 2012 Nobel Prize in Chemistry has been awarded to Robert Lefkowitz and Brian Kobilka for their research into how G-protein-coupled receptors (GPCRs) function. These receptors enable a cell to sense its environment, interacting with surrounding cells and adapting to new situations.

Scientists knew that hormones had powerful effects and suspected that cell surfaces contained some kind of recipient for these. However what these receptors were and how they worked was unclear. Lefkowitz started to use radioactivity in 1968 in order to trace cells' receptors. He attached an iodine isotope to various hormones, and thanks to the radiation, he managed to unveil several receptors, among those a receptor for adrenalin: β-adrenergic receptor. His team of researchers extracted the receptor from its hiding place in the cell wall to gain an initial understanding of how it works.

During the 1980s, Kobilka joined the team and proceeded to work on isolating the gene that codes for the β-adrenergic receptor from the human genome. His creative approach allowed him to attain his goal. When the researchers analyzed the gene, they discovered that the receptor was similar to one in the eye that captures light. They realized that there is a whole family of receptors that look alike and function in the same manner.

This family of receptors is now known as G-protein–coupled receptors. The work of Lefkowitz and Kobilka is crucial for understanding how G-protein–coupled receptors function. This has had an important impact with about half of all medications achieving their effect through G-protein–coupled receptors. Furthermore, in 2011, Kobilka achieved another break-through; he and his research team captured an image of the β-adrenergic receptor at the exact moment that it is activated by a hormone and sends a signal into the cell.