Melbourne, Australia scientists are a step closer to creating a new drug to stop a heart attack in its tracks and reduce the damage caused, without any side effects. The Monash University research, published online in the early edition of PNAS, offers new hope to thousands of people who experience heart attacks and heart failure – one of the major causes of death worldwide. Professors Arthur Christopoulos and Peter Scammells from the Monash Institute of Pharmaceutical Sciences (MIPS) led a team of scientists combining molecular pharmacology and medicinal chemistry to reveal new insights into a specific protein belonging to the family of G-protein-coupled receptors (GPCRs). After successfully combining two molecules, the researchers are a step closer to creating a brand new class of drug that is more targeted and could possess minimal side effects. GPCRs play a role in virtually every biological process and most diseases, including, cardiovascular disease, obesity and diabetes, neuropsychiatric disorders, inflammation, and cancer. Almost half of all current medications available use GPCRs to achieve their therapeutic effect. Current GPCR drugs work either by fully activating or completely blocking receptors, treating the protein like a simple “on-off” switch. This new research discovered alternative recognition sites on GPCRs that can be targeted by drugs to fine-tune the behavior of the protein, basically converting the “on-off” switch into a “dimmer switch”. Professor Christopoulos said it was this insight that enabled the new breakthrough. “When a heart attack strikes, heart cells die because of a lack of oxygen and nutrients.
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