Scientists Uncover New Active Regions on Cell Surface Receptor, Expanding Scope for Drug Targets to Treat Heart Disease
Published:13 Sep.2023    Source:City of Hope

Scientists at City of Hope, one of the largest cancer research and treatment organizations in the United States and a leading research center for diabetes and other life-threatening illnesses, have uncovered new molecular targets on a cell receptor that play a major role in cardiovascular regulation. The findings could lead to improved drugs for heart disease, an unfortunate side effect of some cancer therapies.

 
The study revealed mechanisms on a receptor called Angiotensin II type 1, or AT1R, that allow hormones and drugs to transfer information on the cell surface. Unraveling these communication pathways enable scientists to take the next step in designing targeted therapies for cardiovascular disease. The study used a combination of computational methods and experiments to identify newer drug binding sites in the receptor AT1R that significantly expands the scope of potential targets for drug development, particularly new therapeutics that influence the activity of the receptor in heart disease.
 
Current medicines act on the AT1R receptor to elicit specific cellular responses, but, until now, scientists have not decoded the mechanisms behind them. In this study, the team blended computational modeling with leading-edge approaches in structural biology and pharmacology to detect signaling within AT1R that dictates the receptor's responses to key intracellular pathways. Understanding the nuances behind this interaction will lay the foundation