17 October 2012
Better Blockers
Adrenaline junkies seek the chemical high of this hormone rushing through their body. This thrill is made possible by adrenoceptors, proteins that bind adrenaline, and belong to the G-protein coupled receptor (GPCR) family pictured. Drugs called beta blockers are used to obstruct adrenoceptors. Blocking the β1 adrenoceptor (circled in blue), which when activated causes our hearts to race, is helpful in treating heart failure and high blood pressure. Some people carry a mutant β1 adrenoceptor that binds certain beta blockers better than others. By solving the structure of the mutant adrenoceptor while it’s being blocked scientists can now figure out why this is the case. This research is possible due to the pioneering studies into GPCRs led by Robert Lefkowitz and Brian Kobilka; honoured a week ago today with the Nobel Prize in Chemistry. Kobilka solved the first structure of a human GPCR - the β2 adrenoceptor (circled in red).
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