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Getting to the heart of a solution

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Melbourne scientists are close to producing a new drug to stop and reduce the damage caused by heart attacks, without any side effects.

Professors from the Monash Institute of Pharmaceutical Sciences (MIPS), Arthur Christopoulos and Peter Scammells, led a team of scientists to merge molecular pharmacology and medicinal chemistry, and with this reveal an insight into a specific protein belonging to the family of G protein-coupled receptors (GPCRs).

The team successfully combined the two molecules and now are a step closer to creating a brand new class of drug that is more direct and could have minimal side effects.

GPCRs are in almost every biological process and most diseases, and almost half of all current available medications use GPCRs to achieve a healing effect.

Professor Christopoulos said current GPCR drugs worked either by fully activating or completely blocking receptors, treating the protein like a simple on-off switch.

The new research discovered alternative recognition sites on GPCRs that can be targeted by drugs to fine-tune the behaviour of the protein, an insight that enabled the breakthrough.

“When a heart attack strikes, heart cells die because of a lack of oxygen and nutrients, but even more damage is caused when the blood rushes back to the heart cells due to the release of inflammatory chemicals and damaging free radicals,” Professor Christopoulos said.

An adenosine A1 receptor, a GPCR found in the heart, is activated by current drugs that minimise damage to the heart. However, activating the A1 receptor also slows down the heart, or can even stop the heart completely.

“Correct dosage has been a serious challenge in clinical trials for A1 receptor drugs,” Professor Scammells said.

Professor Christopoulos said the Monash study focused on finding new ways to activate the protein to achieve the beneficial effects, without the side effects.

“The beauty of this protein is that if you activate it effectively, you minimise the heart attack and protect the heart cells, and that’s something that’s never been done before,” Professor Scammells said.

Sanja Novakovic