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Adrenaline receptor 'frozen in action' by VIB researchers
Date:1/12/2011

Brussels - Adrenaline, the hormone that prepares our body to fight or flight, acts on a hyperdynamic receptor. This molecule switches so fast between several positions, that it was impossible to image it. Until now. Scientists, including Jan Steyaert of VIB and the Vrije Universiteit Brussel in Belgium, and colleagues from Stanford University in the US, have "frozen the molecule in action" using Xaperones, tiny, stable antibodies developed by the Brussels scientists. The Xaperones bind like a key to a lock, holding the adrenaline receptor in one position -- the on position. After binding the adrenaline receptor to the Xaperone, the researchers could use X-ray crystallography techniques to determine its structure. The results are published in Nature.

Prospects for medicine

The breakthrough is not only a scientific first, the newly developed technique also offers promising prospects for medicine. The adrenaline switch is the target of widely used drugs such as asthma inhibitors and beta blockers. The latter are used worldwide as a medicine for heart disease.

But the applications are not limited to asthma or heart disease. Over 30% of all drugs on sale in pharmacies today switch similar receptors on or off. Through the newly developed technique, these receptors can now be accurately described, which is a necessary first step to determine their action and develop new or better drugs.

Receptors as switches in the body

Adrenaline is a hormone that is released under stress. It is a messenger molecule which causes the heart to beat faster, causes us to sweat suddenly and releases sugar as an immediately usable source of energy. These reactions are the result of the fact that adrenaline binds with a specific switch (known as beta2-adrenergic receptor). This switch is embedded in the membrane surrounding our cells. When adrenaline binds to the receptor, the individual cell knows that the rest of the body is prep
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Contact: Joris Gansemans
joris.gansemans@vib.be
329-244-6611
VIB (the Flanders Institute for Biotechnology)
Source:Eurekalert

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