Anti-cancer drug discovery

In the continued search for more effective anti-cancer therapies, new approaches must be identified that intervene in the essential cell functions that produce tumours.

This innovation from Oxford University provides new tools for identifying drugs against novel cancer targets.

Enzyme discovery

Researchers at the University of Oxford have discovered new 2-oxoglutarate (2OG) oxygenase enzymes which modify human ribosomal proteins.

These proteins are overexpressed in various tumours, and are implicated in the pathologically relevant processes of cell proliferation, apoptosis, and invasion.

Proven ‘druggable’ target

2OG oxygenases have significant therapeutic potential, exemplified by the fact that several small molecule inhibitors are in development.

Known 2OG oxygenase inhibitors have been shown to inhibit these new enzymes, acting as validated starting points for new drug discovery programmes.

The enzymes’ utility as off-target counterscreens in projects targeting other protein family members has also been highlighted.

Targeting tumour sites

Tumours are generally hypoxic, meaning they lack oxygen. These oxygenase enzymes rely on high oxygen levels to catalyse ribosomal hydroxylations.

This opens up the new therapeutic possibility of distinguishing modified from unmodified ribosomes, thereby targeting tumour sites and reducing the potential for side effects in healthy tissue.

Selective protein modification

A further application of the enzymes is in rational peptide drug design. The enzymes have been shown to stereoselectively hydroxylate certain difficult-to-produce amino acid residues, such as 3-hydroxyprolyl and betahydroxy histidine.

This will have utility in optimising peptide-based drug properties – for example, improved binding affinity, stability, half-life, and/or solubility.

Patent status

The technology is the subject of two patent applications.

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