Discovery of Phosphodiesterase-4 Inhibitors: Serendipity and Rational Drug Design

Susanne C. Feil is a research officer in the Structural Biology Laboratory and the ACRF Rational Drug Discovery Centre at St Vincent’s Institute of Medical Research in Fitzroy, Victoria, Australia. She received her Ph.D. from the University of Melbourne in 2003 for her work on crystallographic studies of pore-forming toxins. In 2006, she obtained a four-year Industry Fellowship in conjunction with an Australian Biotech company known for its world-leading antiviral drug discoveries. Her main projects are in the field of infectious diseases involving crystallisation and structural studies.

Jessica K. Holien is a research officer in the Structural Biology Laboratory and the ACRF Rational Drug Discovery Centre at St Vincent’s Institute of Medical Research in Fitzroy, Victoria, Australia. She currently works on a range of molecular modelling projects with a strong focus on cancer, infection, and neurological diseases. Jessica completed her Ph.D. in 2010 in the Department of Medicinal Chemistry, Monash University, using multi-faceted structure-based drug design techniques including molecular modelling, chemical synthesis, and biological assays. She has recently been awarded a joint Cure Cancer/Leukaemia Foundation Post-Doctoral Fellowship.

Dr Craig Morton is a senior research officer at St Vincent’s Institute and an adjunct senior lecturer at the Department of Biochemistry and Molecular Biology, Monash University. An experienced research scientist with a strong track record in structural biology and drug discovery, Craig was employed in the Australian biotechnology industry for more than a decade, where he was involved in the discovery and development of drugs for various infectious diseases. His current interests are focused on combining structural biology with computational approaches for understanding protein–ligand interactions.

Nancy C. Hancock has a Master’s degree in cell and molecular biology from San Francisco State University and has extensive experience as a senior research assistant in the pharmaceutical and biotechnology industries in the USA. Her work in the Structural Biology Group at St Vincent’s Institute involves the critical sequential steps of cloning, expression, purification, and crystallisation of proteins in order to achieve the successful 3D structure determination of specific medically important proteins.

Philip Thompson is Associate Professor in medicinal chemistry at the Monash Institute of Pharmaceutical Sciences. His research interests have two main foci – the development of cell signalling pathway inhibitors and peptide science. In the area of signalling, he has worked for many years on the PI3 kinase family of enzymes, first as a scientist at Thrombogenix/Kinacia, an Australian start-up company that developed the first PI3Kβ-selective inhibitors as antithrombotics. He also works on phosphodiesterases. In peptide science, his group is attempting to develop peptide chemistry to yield compounds with improved utility. His current targets of interest are antibacterial cyclic lipopeptides, peptide GPCRs, and aminopeptidase inhibitors.

Michael W. Parker is Deputy Director of St Vincent’s Institute where he heads its Structural Biology Laboratory and the ACRF Rational Drug Discovery Centre. He is an NHMRC Research Fellow and a Professorial Fellow at the Bio21 Institute, Melbourne University. He has published more than 300 papers and has been recognised with numerous awards, including the 2011 Lemberg Medal of the Australian Society for Biochemistry and Molecular Biology and the 2012 Federation of Asian and Oceanian Biochemists and Molecular Biologists Award for Research Excellence. He was elected a Fellow of the Australian Academy of Science in 2010.