ACRF Rational Drug Discovery Facility

An interstate collaboration between a team of scientists from St Vincent’s Institute, Melbourne and Hanson Institute, Adelaide, has unravelled the structure of a cell-signalling receptor which will lead to the discovery of new, less invasive drugs to treat leukaemia. Both institutes were separately awarded grants from ACRF.

A $900,000 Australian Cancer Research Foundation grant provided St. Vincent’s Institute with an extensive upgrade of cancer drug discovery technologies to accelerate progress in converting basic cancer discoveries into promising lead molecules for cancer treatment.

The ACRF Rational Drug Discovery Facility at St Vincent’s Institute was officially opened by The Hon. John Brumby, MP, Minister for Innovation, Victoria, on 1 March 2007.

Specifically, the upgrades are:

1. A new X-ray crystallography facility. Visualising the 3D atomic structures of proteins involved in cancer is essential for fully understanding their function and allows structure-based discovery of novel drugs to combat the disease. The structures are determined by shooting X-rays at protein crystals to generate X-ray scattering patterns that can be converted into 3D images using computers. Housed in a $200K, purpose-built laboratory the new X-ray facility is five times faster than its predecessor and will allow SVI to maintain internationally competitive research

2. Virtual screening facility. Once the 3D atomic structure of a cancer protein is elucidated, the structure is screened against a database containing the structures of more than 4 million compounds using fast computers with aim of finding drug-like molecules that are predicted to bind to the protein structure and inhibit cancer-causing properties. The new facility will include more powerful software and hardware to considerably speed up the search for these molecules.

3. Medium throughput screening facility. Compounds identified through the virtual screening facility are either purchased or synthesized. The compounds are then tested in biological assays to establish their suitability. The new facility will enable a larger number of compounds to be tested more rapidly.

Lead Researchers: Professor Tom Kay, Professor Michael Parker, A/Professor Matthew Gillespie