About Professor Michael Kassiou
Professor Kassiou's work aims at designing and discovering new CNS bioactive drugs that can be used in treating and better understanding human disease processes.
Professor Kassiou is an internationally recognized research leader in the chemistry of CNS bioactive drugs.
Michael Kassiou is Professor of Medicinal Chemistry, and Head of the Drug Discovery Research Unit located at the Brain and Mind Research Institute and School of Chemistry at the University of Sydney. His research interests encompass the interface between chemistry and biology. In particular the development of targeted molecular probes for neuropharmacological studies, including the development of pharmacological techniques for the study of receptor-ligand interactions and pathways affected in substance abuse, neurodegenerative and psychotic disorders. He has made fundamental contributions to the understanding of structure-activity relationships of molecules that are either active or that can label molecular sites of interest in the CNS. He has developed strong international collaborations with UCLA School of Medicine (Los Angeles, CA), the Johns Hopkins Medical Institutes (Baltimore, MD), University of Tours, (INSERM), the Department of Pharmaceutical Science University of Firenze, University of Chicago, and the Département de Recherche Médicale-CEA, Service Hospitalier Frédéric Joliot (Orsay, France) where he has been a visiting fellow. In 1996 he was awarded a Fogerty International Fellowship at the National Institutes of Health in the USA. He is the author of over 120 scientific research papers, reviews and book chapters, and is a co-inventor on 5 patents. He is a thematic editor for Current Pharmaceutical Design and serves on the editorial advisory board of several international medicinal chemistry and drug discovery journals. He is a fellow of the Royal Australian Chemical Institute and a member of five multi-disciplinary professional associations.
For further information, please see Prof Kassiou's staff profile:
http://sydney.edu.au/science/chemistry/research/kassiou.html
Selected publications
- Leaver, KR; Reynolds, A; Bodard, S; Guilloteau, D; Chalon, S; Kassiou, M. Effects of translocator Protein (18 kDa) Ligands on Microglial Activation and Neuronal Death in the Quinolinic-Acid-Injected Rat Striatum. ACS Chem. Neurosci., 3 (2), 114-119, 2012. DOI: 10.1021/cn200099e
- Issa, F; Kassiou, M and Rendina, LM. Boron in drug discovery: carboranes as unique pharmacophores in biologically active compounds. Chem. Rev., 111 (9), 5701–5722, 2011. DOI: 10.1021/cr2000866
- Banister, SD; Yoo, DT; Chua, SW; Cui, J; Mach, RH and Kassiou, M. N-arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands. Bioorganic & Medicinal Chemistry Letters, 21 (18), 5289-5292, 2011. DOI: 10.1016/j.bmcl.2011.07.028
- Moussa, IA; Banister, SD; Beinat, C; Giboureau, N; Reynolds, AJ and Kassiou, M. Design, synthesis, and structure—affinity relationships of regioisomeric N-benzyl alkyl ether poperazine derivatives as s-1 receptor ligands. J. Med. Chem., 53 (16), 6228-6239, 2010. DOI: 10.1021/jm100639f
- Reynolds, A; Hanani, R; Hibbs, D; Damont, A; Da Pozzo, E; Selleri, S; Dollé, F, Martini, C and Kassiou, M. Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). Bioorganic & Medicinal Chemistry Letters, 20 (19), 5799-5802, 2010. DOI: 10.1016/j.bmcl.2010.07.135
- Beinat, C; Banister, S; Moussa, I; Reynolds, AJ; McErlean, CSP and Kassiou, M. Insights into structure-activity relationships and CNS therapeutic applications of NR2B selective antagonists. Current Medicinal Chemistry, 17 (34), 4166-4190, 2010. DOI: 10.2174/092986710793348572
- Dolle, F; Luus, C; Reynolds, A and Kassiou, M. Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography. Current Medicinal Chemistry, 16 (22), 2899-2923, 2009. DOI: 10.2174/092986709788803150
- Banister, SD; Moussa, IA; Jordan, MJT; Coster, MJ and Kassiou, M. Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding and molecular modeling. Bioorganic & Medicinal Chemistry Letters, 20 (1), 145-148, 2010. DOI: 10.1016/j.bmcl.2009.11.019
- Gunosewoyo, H; Coster, MJ; Bennett, MR and Kassiou, M. Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening. Bioorganic & Medicinal Chemistry, 17 (14), 4861-4865, 2009. DOI: 10.1016/j.bmc.2009.05.083
- Scarf, AM; Ittner, LM and Kassiou, M. The translocator protein (18 kDa): Central nervous system disease and drug design. Journal of Medicinal Chemistry, 52 (3), 581-592, 2009. DOI: 10.1021/jm8011678