G protein-coupled receptor drug discovery

G protein-coupled receptors (GPCRs) are the largest superfamily of all receptors. They are the target of 40 – 50% of currently marketed drugs. So understanding their molecular functionality is highly relevant, both clinically and commercially.

Medicinal Chemistry works collaboratively on GPCRs with MIPS Drug Discovery Biology. The recent clarification of the X-ray structure of GPCRs has also opened new research opportunities, which we're strongly pursuing with our Drug Discovery Biology colleagues.

In addition to traditional medicinal chemistry programs around GPCR drug discovery, we also work in frontier areas such as allosteric modulators of GPCRs, as well as bitopic and bivalent GPCR ligands. The adenosine, dopamine, muscarinic acetylcholine and sphingosine-1-phosphate receptors are the focus of these studies.

This research is currently funded by the Australian Research Council and the National Health and Medical Research Council.

Principal investigators