Scientists unlock potential heart attack drug without side effects

Melbourne scientists are getting closer and closer to making a drug that will stop a heart attack, without any side effects. Professors Arthur Cristopoulos and Peter Scammells from the Monash Institute of Pharmaceutical Sciences (MIPS) revealed new information about a specific protein belonging to the family of G protein-coupled receptors (GPCR), and used this data to combine two molecules that brought them a step closer to creating this new drug.

These GPCR play a role in almost every biological process and most diseases, including those that cause heart attacks. Current drugs to stop this protein treat the protein like an "on-off" switch, but the new information gained by these scientists allowed them to treat it like a "dimmer switch". Other drugs to minimise heart damage activate the adenosine A1 receptor, a GPCR, but cause the heart to slow down, and can even stop it.

The main point of these studies was to find a drug that wouldn't cause GPCR to act this way. They combined two molecules, one binding to the main site on the receptor for activation, and another binding to the alternative site for fine-tuning of the activity. The "dimmer switch" worked, resulting in a molecule that protected the heart and didn't affect heart rate. The findings in the experiment will help bring a new phase of research to develop the drug that we need.

Themes of Nature of Science:

• Science is based on evidence
• Role of credibility 
• Importance of repeatability
• Role of motivation and curiosity

http://www.biologynews.net/archives/2014/03/11/scientists_unlock_potential_heart_attack_drug_without_side_effects.html