2010 Annual Report - Institute for Molecular Bioscience - University ...

imb annual report 2010
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DAVID FAIRLIE
CHEMISTRY AND HUMAN THERAPEUTICS
OUR GROUP WORKS AT THE interface
of chemistry, biology and disease to better
understand molecular mechanisms of life,
ageing, disease and death.
Chemistry researchers develop expertise
in: organic, medicinal or biological
chemistry; computer-aided drug design;
organic synthesis; structure determination
using 2D NMR; and interactions between
small molecules, proteins, RNA and DNA.
Outcomes are new compounds/structures,
chemical reactions/mechanisms, enzyme
inhibitors, protein agonists/antagonists,
and structural mimics of protein surfaces.
Biology researchers use our novel
compounds to interrogate human
protein, cellular and animal function
and to elucidate mechanisms of protein
activation, biological/physiological
processes, disease development, and
drug action. Researchers gain insights to
processes pivotal to human physiology or
aberrant in disease, and develop skills in
pharmacology, enzymology, biochemistry,
immunology, virology, oncology or
neurobiology.
RESEARCH PROJECTS
(http://fairlie.imb.uq.edu.au/)
• Drug discovery (for inflammatory
disorders, cancers, viral infections,
neurodegeneration, obesity and
metabolic dysfunction)
• Organic and medicinal chemistry
• Pharmacology: molecular (cellular) and
experimental (animal models)
• Structures by 2D NMR spectroscopy
• Enzymes, GPCRs & protein-protein
interactions
• Mimicry of protein surfaces
KEY PUBLICATIONS
Barry, G.D., Suen, J.Y., Le, G.T., Cotterell,
A., Reid, R.C., and Fairlie, D.P. (2010).
Novel Agonists and Antagonists for
Human Protease Activated Receptor 2.
Journal of Medicinal Chemistry 53: 7428-
7440.
Harrison, R.S., Shepherd, N.E., Hoang,
H.N., Abbenante, G., Reid, R.C., and
Fairlie, D.P. (2010). Downsizing Human,
Bacterial and Viral Proteins To Short
Water-Stable Alpha Helices That Maintain
Biological Potency. Proceedings of the
National Academy of Sciences USA 107:
11686-11691.
Harrison, R.S., Ruiz-Gómez, G., Hill, T.A.,
Chow, S.Y., Shepherd, N.E., Lohman,
R.J., Abbenante, G., Hoang, H.N.,
and Fairlie, D.P. (2010). Novel Helix-
Constrained Nociceptin Derivatives Are
Potent Agonists and Antagonists of ERK
Phosphorylation and Thermal Analgesia
in Mice. Journal of Medicinal Chemistry
Epub ahead of print November 10.
Iyer, A., Fairlie, D.P., Prins, J.B.,
Hammock, B.D., and Brown, L. (2010).
Inflammatory lipid mediators in adipocyte
function and obesity. Nature Reviews
Endocrinology 6: 71-82.
Shepherd, N.E., Hoang, H.N., Abbenante,
G., and Fairlie, D.P. (2009). Left- and
Right-Handed Alpha-Helical Turns
in Homo- and Hetero-Chiral Helical
Scaffolds. Journal of the American
Chemical Society 131: 15877-15886.
Stoermer, M.J., Chappell, K.J., Liebscher,
S., Jensen, C.M., Gan, C.H., Gupta, P.K.,
Xu, W.J., Young, P.R., and Fairlie, D.P.
(2008). Potent cationic inhibitors of West
Nile virus NS2B-NS3 protease with serum
stability, cell permeability and antiviral
activity. Journal of Medicinal Chemistry
51: 5714-5721.
Blakeney, J.S., Reid, R.C., Le, G.T., and
Fairlie, D.P. (2007). Nonpeptidic Ligands
For Peptide-Activated GPCRs. Chemical
Reviews 107: 2960-3041.
Kahnberg, P., Lucke, A.J., Glenn, M.P.,
Boyle, G.M., Tyndall, J.D., Parsons, P.G.,
and Fairlie, D.P. (2006). Design, Synthesis,
Potency and Cytoselectivity Of Anticancer
Agents Derived By Parallel Synthesis
From Alpha-Aminosuberic Acid. Journal of
Medicinal Chemistry 49: 7611-7622.
Levick, S., Loch, D., Rolfe, B., Reid, R.C.,
Fairlie, D.P., Taylor, S.M., and Brown, L.
(2006). Antifibrotic Activity of an Inhibitor
of Group IIa Secretory Phospholipase A 2
in Young Spontaneously Hypertensive
Rats. Journal of Immunology 176: 7000-
7007.
LAB MEMBERS
Senior Research Officers: Dr Ligong Liu,
Dr Robert Reid, Dr Martin Stoermer
Research Officers: Dr Jade Blakeney,
Dr Frederik Diness, Dr Tim Hill, Dr Huy
Hoang, Dr Fredrik Lindahl, Dr Rink-Jan
Lohman, Dr Andrew Lucke, Dr Praveen
Madala, Dr Gloria Ruiz-Gómez, Dr Conor
Scully, Dr Jacky Suen
Research Assistant: Adam Cotterell
PhD Students: Sheila Barbero, Shaio
Chow, Anh Do, Russell Driver, Praveer
Gupta, Maria Halili, Rose Harrison,
Junxian Lim, Ranee Singh, Vernon Seow
Masters Student: Annika Yau
Honours Students: Peifei Chu, Johan
Hamidon
Undergraduate Students: Sok Lin Foo,
Lisa Redlingshoefer, Annette Spierings,
Benjamin Wong
Occupational Trainee: Daniel Nielsen
Office Manager: Barbara Feenstra/
Lyn Fairlie