New Heart Attack Drug May Have No Side-Effects for Patients

Monash University in Australia published a study today in the journal Proceedings of the National Academy of Sciences that cites the development of a potentially effective new heart attack drug with no side effects.

The discovery was made when analyzing G protein-coupled receptors (GPCRs) through the combination of molecular pharmacology and medicinal chemistry. Professors Arthur Christopoulos and Peter Scammells of the Monash Institute of Pharmaceutical Sciences in Melbourne, Australia successfully combined two molecules that they believe target heart issues more effectively while possessing minimal-to-no side effects.

The scientists' discovery of the medications new role is significant because current GPCR drugs either fully activate or block receptors, and act as a simple "on-off" switch for the proteins. The new medication is compared to a "dimmer switch", which they believe can fine-tune the behavior of this crucial protein that plays a role in nearly every biological process as well as many disease including heart disease, obesity, and diabetes.

If proven to be effective, Christopoulos and Scammells may have discovered one of the more effective drugs for treating one of the major causes of death worldwide. GPCRs are one of the largest classes that are targeted for drug therapy. The protein signals pathways in both healthy and damaged hearts. Their signaling is activated by ligand binding to an extracellular active site of the receptor. GPCR signaling in failing hearts accounts for the majority of prescriptions for cardiovascular diseases.

Current medications that seek to minimize damage in the heart are administered to activate the adenosine A1 receptor, which is a GPCR found in the heart. The ability to monitor the protein as a "dimmer switch" is essential because if the A1 receptor isn't effectively activated it can slow down the heart, and if it is too activated it can stop the heart.

This current study can provide a breakthrough for the world of medicine and help combat one of the world's deadliest diseases.