ETS2300

Telomerase was identified as the enzyme responsible for maintaining telomeres (specialised complexes that 'protect' the ends of chromosomes). Telomerase is expressed in 90% of cancers, being required for replicative immortality, but is absent in most normal cells making it of interest as a target for anti-cancer drug discovery. Our approach has been to target multiple networks mediating the regulation of telomerase, its expression, activity, localisation and functional effects.

Telomerase: potent small molecule anti-proliferatives

Telomerase is expressed in 90% of cancers, being required for replicative immortality, but is absent in most normal cells making it of interest as a target for anti-cancer drug discovery. It exists as part of a highly regulated protein complex in the nucleus, but more recently has been revealed to have additional functions elsewhere in the cell. Our approach has been to target multiple networks mediating the regulation of telomerase, its expression, activity, localisation and functional effects.

Telomerase Figure

Our lead compounds are small molecules with:

  • cellular potency about 10 times greater than Imetelstat, and 100 times greater than the most potent small molecule previously known (e.g. BRACO19)
  • good variability in chemotypes
  • synthetic tractability
  • good drug-like characteristics
  • good selectivity for TERT+ cancer cells over TERT- fibroblasts