AustCancer finds cancer jammer molecule

Perth-based cancer therapeutics developer Australian Cancer Technology's (ASX:ACU) joint discovery project with Cambridge-based BioFocus (AIM:BIO) has designed a tiny spanner to jam the molecular works of cancer cells that evade conventional chemotherapy and radiotherapy.

AustCancer, which already has its promising broad-spectrum cancer vaccine, Pentrix, in early-phase clinical trials, has been working with the BioFocus to identify compounds capable of blocking a key enzyme involved in the early stages of cell division.

The protein kinase Chk1 operates at the first checkpoint in the cell cycle, providing the 'go' signal for cell division.

The enzyme's activity allows fast-dividing cancer cell to evade a routine genetic health check by a tumoUr-suppressor gene that would normally force them into apoptosis - programmed cell death.

AusCancer's chairman, Dr Roger Aston, says kinase inhibitors are regarded among the most promising of the new wave of experimental anti-cancer therapies.

BioFocus, based in Cambridge, is a service company with expertise in medicinal chemistry and cellular assays for drug activity. AustCancer and BioFocus have two joint projects - the Chk 1 kinase project, and another on breast cancer.

"We provide the money, they provide the expertise," says AusCancer CEO Dr Alistair Cowden.

"Biofocus was really keen to get into the kinase-inhibitor area. They synthesised 8000 compounds, from first principles, incorporating structures that they thought might have interesting activity."

"They got a number hits, then went back and played around with the structures to see if they could enhance their potency and efficacy."

Cowden says BioFocus was looking for compounds that were highly selective for the Chk1 kinase boosted the cell-killing efficacy of conventional cancer treatments like radiation therapy, and standard chemotherapy agents like cis-platin.

Several promising candidates emerged from the assays; despite differences in chemistry, they have similar structure-activity relationships, indicating they were on the right track

The partners have selected the most potent of these as a lead compound, and are now synthesising other molecules around its molecular theme, to maximise its potency and selectivity.

AustCancer and BioFocus have now decided to focus their resources on the Chk1 project, because of its potential to deliver commercial outcomes in the near term.

Cowden says the partners will patent the new molecules, and believe they will have little difficulty finding partners to take them into clinical trials.