Highlights
- Discovery of 39 molecular candidates targeting the m6A RNA demethylase protein.
- Findings validated using advanced NMR spectroscopy and resonance techniques.
- Innovative drug discovery approach leveraging RNA epigenetics for disease treatment.
Race Oncology (ASX:RAC) has achieved a significant milestone in RNA epigenetics research through its collaboration with Monash University. ASX healthcare stock Race Oncology identified 39 molecular candidates targeting the m6A RNA demethylase protein, FTO, a key enzyme in RNA epigenetics. This breakthrough offers potential for innovative therapies in cancer and metabolic disorders.
The identified molecular "hits" were rigorously validated using cutting-edge techniques like nuclear magnetic resonance (NMR) spectroscopy and surface plasmon resonance. These advanced methods confirm the specificity of the molecules to FTO, highlighting their potential as a foundation for novel drug development.
Innovative Approach to Drug Discovery
Race Oncology utilized NMR fragment screening as a novel approach to uncover drug-like molecules capable of regulating protein activity. This strategy diverges from traditional high-throughput screening by identifying compounds that interact with areas outside the enzyme's active site. This innovative method provides unique opportunities for developing patentable, first-in-class drugs targeting the m6A RNA epigenetic pathway.
RNA epigenetics dysregulation, including proteins like FTO, has been linked to numerous cancers and metabolic diseases. However, selectively inhibiting FTO has historically posed challenges due to structural similarities with other proteins in the ALKBH family. The partnership with Monash enabled the use of a curated chemical fragment library, allowing the identification of unique FTO-binding chemical structures that may overcome these challenges.
Future Directions in Drug Development
Race Oncology has announced plans for a "hit-to-lead" campaign to refine these molecular fragments into lead drug candidates. This phase aims to enhance the potency, selectivity, toxicity profiles, and metabolic properties of the identified compounds. However, the company is currently evaluating whether to proceed with this next stage, given the resource-intensive nature of such development.
By advancing research in RNA epigenetics and FTO inhibition, Race Oncology continues to pave the way for innovative treatments addressing critical unmet medical needs. Its strategic approach and collaboration with Monash University demonstrate its commitment to pioneering advancements in drug discovery.