CT200: Checkpoint reactivation in tumours

CT200 is a mechanism-based pre-clinical compound that targets a critical enzyme involved in checkpoint and proliferation control. A key target for CT200 is the E2F pathway of proliferation control.

Cell cycle checkpoints are disabled in tumour cells. In normal cells, checkpoints act in quality control functions and are responsible for stimulating apoptosis (cell death) in response to for example abnormalities or mutations in DNA. If the quality control function of checkpoints is disabled, cells continue to grow even if there are major defects in their DNA.

Celleron’s Founders have unearthed a new pathway that allows checkpoints to be reinstated in tumour cells. A key enzyme which blocks checkpoint activity, has been identified. Inactivation of the enzyme in tumour cells reinstates checkpoint activity and results in apoptosis, whilst normal cells are spared the killing effect. This is because cancer cells contain many oncogenic changes and irreparable DNA rearrangements.


A lead compound docked into the enzyme active site.

CT300: Inhibitors of new protein phosphokinases

CT300 is focussed on a novel group of compounds that block the activity of a new protein kinase implicated in cancer cell proliferation.

Celleron is working with structural biologists to elucidate new inhibitors of protein kinases. One particular area of interest concerns a protein kinase which is involved with the regulation of cell division, specifically allowing proper mitosis to occur.

In human cell lines, the enzyme is required for the normal alignment of chromosomes during metaphase. Depletion of the enzyme by RNA interference leads to cell cycle arrest and death.

Celleron has validated the enzyme as a viable cancer target and identified novel inhibitors using a structure-based focussed chemistry approach

An inhibitor docked into the haspin enzyme active site