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Highlights
- Race Oncology discovers unique FTO inhibitors in RNA epigenetics research.
- Program identifies 39 molecular candidates with potential for patentable drugs.
- Novel inhibitors target m6A RNA pathway, expanding applications beyond cancer therapies.
Race Oncology (ASX:RAC) has completed a groundbreaking drug discovery program at Monash University’s Fragment Platform, targeting the fat mass and obesity-associated protein (FTO). This achievement is set to enhance the company’s capabilities in RNA epigenetics and cancer drug development.
The program employed advanced fragment-based screening using nuclear magnetic resonance (NMR) to identify molecular candidates capable of binding to the FTO protein. A total of 39 promising compounds were discovered, with their binding confirmed through multiple methods, including NMR and surface plasmon resonance. This cutting-edge technique offers an innovative alternative to conventional high-throughput screening methods, identifying drug-like molecules with potential to regulate protein activity beyond enzyme inhibition.
Advancing RNA Epigenetics Research
This discovery highlights the role of FTO-binding chemical scaffolds in developing patentable molecules. These molecules are designed to selectively target the m6A RNA epigenetic pathway, a crucial regulator in cancer and metabolic diseases. Dysregulation of RNA epigenetics is a known driver of several serious health conditions, making this breakthrough highly significant.
The FTO protein, a critical component of RNA regulation, is a key focus for pharmaceutical innovation. Developing selective inhibitors for FTO has been challenging due to its structural similarities with other proteins in the ALKBH family. Race Oncology commissioned the Monash Fragment Platform library in 2022 to perform an NMR-based screen, successfully identifying unique chemical structures targeting FTO and ALKBH5.
Pioneering Oncology Innovation
The company is now poised to develop first-in-class, structurally unique FTO inhibitors. These inhibitors, designed for precision and potency, have potential applications beyond cancer, broadening their therapeutic impact. The findings provide Race Oncology with valuable intellectual property in the rapidly evolving field of RNA epigenetics.
Next Steps in Drug Development
Race Oncology plans to move forward with a ‘hit-to-lead’ medicinal chemistry campaign. This process involves optimizing the chemical structures of validated fragments to create lead drug candidates with enhanced inhibitory potency and selectivity. The program aims to demonstrate efficacy in animal cancer models while minimizing toxicity and ensuring favorable metabolic profiles.
Race Oncology is currently evaluating the feasibility of advancing into this resource-intensive phase. If successful, this initiative could solidify the company’s position as a leader in cutting-edge oncology and epigenetic research.
