April 24, 2024

Modifying Brain Molecule Relaxin-3 for Targeted Treatment of Anxiety, Depression, and More

A recent study led by Professor Gavin Dawe from the National University of Singapore (NUS Medicine) has discovered a potential breakthrough in the treatment of conditions such as anxiety, depression, and eating disorders. The research focused on modifying relaxin-3, a neuropeptide found in the human brain and nervous system, to target specific functions within the body, thereby reducing the likelihood of adverse side effects associated with current medications.

Relaxin-3 plays a crucial role in regulating various physiological functions, including stress responses, appetite, mood, and pain perception, by binding to the receptor RXFP3 in the brain. However, the activation of multiple signaling pathways by RXFP3 can lead to unwanted side effects when using drugs to treat specific conditions. By modifying relaxin-3 to selectively activate certain signaling pathways of RXFP3, the research team was able to achieve biased agonism, allowing for more targeted treatments with reduced adverse effects.

The team utilized a technique called peptide stapling to modify the B-chain of relaxin-3, stabilizing its shape for more efficient binding and activation of RXFP3. This process enhances the interaction between relaxin-3 and RXFP3, triggering specific signaling pathways that impact the body’s physiological functions. The findings suggest that by designing drugs that selectively activate specific functions within the body, it may be possible to develop more effective treatments for a range of conditions.

Dr. Tharindunee Jayakody, the first author of the study, highlighted the significance of the research in advancing the understanding of proteins like RXFP3 at a molecular level. While the study is in its early stages, the promising outcomes point towards the potential development of tailored drugs for anxiety, depression, eating disorders, and addiction. Collaborative efforts are underway to further investigate the molecular properties of proteins like RXFP3 and explore the use of biased agonists in drug development.

Looking ahead, the research team plans to explore the effects of different stapled peptides on the body’s physiological functions and human behavior, furthering the understanding of how interactions between relaxin-3 and RXFP3 impact overall health and well-being. This groundbreaking research paves the way for the development of more targeted and effective treatments for mental health and behavioral disorders, offering hope for improved patient outcomes and quality of life.

1. Source: Coherent Market Insights, Public sources, Desk research
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