Flipping the 'biochemical switch' to turn off illness

Posted by pt91 at Mar 15, 2012 03:45 PM |
Leicester researchers 'switch off' chemical linked to heart disease and stroke.
Flipping the 'biochemical switch' to turn off illness

Model of the human P2X1 receptor for ATP, the three subunits that make up the functional receptor are shown in red, white and blue.

Researchers in our Department of Cell Physiology and Pharmacology have announced a major step forwards in the fight against heart disease and strokes. The research has detected a so-called 'biochemical switch' which can contribute to these conditions, and has lead to a better understanding of how this switch is 'turned on.'

Funded by the Wellcome Trust and the British Heart Foundation, and lead by Professor Richard Evans, the research centres on the P2X1 receptor on blood platelets which can potentially reduce dangerous blood clotting.

The procedure involved the researchers undertaking biochemical studies and purifying the receptor, and then studying it through an electron microscope, allowing them to detect a change in its shape when it’s activated. The three sections of the receptor appear to ‘twist’ against each other and the researchers have summarised that if they can stop this twisting, then the receptor cannot be completely activated.

Only with the understanding of how the receptor is activated can a drug be developed to prohibit this activation. This important Leicester-led breakthrough, published in Proceedings of the National Academy of Sciences (PNAS) is a positive first step in a longer journey towards preventing heart attacks and strokes that are caused by this particular type of blood clotting.

Working alongside Professor Evans are Jonathan A Roberts, Rebecca C Allsopp, Sam El Ajouz and Catherine Vial from Cell Physiology and Pharmacology, Ralf Schmid from our Department of Biochemistry and Mark T Young from Cardiff University.