Race Oncology advances RNA epigenetics with FTO drug discovery at Monash

Описание: Race Oncology Ltd (ASX:RAC, OTC:RAONF) CEO Daniel Tillett joins Proactive’s Tylah Tully to discuss the FTO drug discovery program the company has concluded at Monash University’s Fragment Platform (MFP).

The program successfully identified 39 molecular candidates (‘hits’) that bind specifically to the m6A RNA demethylase protein, FTO.

These findings were validated using NMR spectroscopy and surface plasmon resonance.

The program leverages NMR fragment screening to discover drug-like molecules that can regulate protein activity outside the enzyme's active site, offering an alternative to traditional high-throughput screening.

The identified FTO-binding chemical scaffolds create opportunities for the development of patentable, first-in-class drugs targeting the m6A RNA epigenetic pathway.

RNA epigenetics dysregulation, involving proteins like FTO, is linked to various cancers and metabolic diseases. However, selective inhibition of FTO is challenging due to structural similarities with related proteins in the ALKBH family.

Race’s use of Monash’s curated chemical fragment library enabled the identification of unique FTO-binding structures.

Race plans a ‘hit-to-lead’ campaign to refine these fragments into lead drug candidates, focusing on improving potency, selectivity, toxicity profiles, and metabolic properties. The company is currently evaluating whether to proceed with this resource-intensive phase.

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