Awards and Prizes

2012 Chemistry Nobel to Lefkowitz and Kobilka

[Robert Lefkowitz] Robert Lefkowitz
[Brian Kobilka] Brian Kobilka

Robert Lefkowitz and Brian Kobilka shared the 2012 Nobel Prize in Chemistry for groundbreaking discoveries that revealed the inner workings of G-protein–coupled receptors (GPCRs), a large family of membrane-bound recepters that influence most aspects of our health and are prime targets for drug action. In 1968 Robert Lefkowitz labeled various hormones with radioactive iodine in order to identify receptors that bound the hormones, including the receptor for adrenalin. He extracted the receptor from the cell wall and gained an initial understanding of how it works.

[Activated complex] Crystal structure of activated β-2 adrenergic receptor β2AR (red) in complex with G-proteins (green, cyan and yellow). Credit: S. G. F. Rasmussen et al., Nature, 477, 549–555 (2011).

In the 1980s, Brian Kobilka isolated the gene that codes for the β-adrenergic receptor from the human genome. The team realized that this receptor looked very similar to the rhodopsin receptor from the eye. They realized that there is a whole family of GPCRs that look alike and function in the same manner. The studies by Lefkowitz and Kobilka are crucial for understanding how GPCRs function because about half of all medications achieve their effect through GPCRs. In 2011, Kobilka 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. This image is a molecular masterpiece – the result of decades of research.

From ACA RefleXions, Winter 2012