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Academic staff: Michael Kassiou

Associate Professor

Address:

Brain and Mind Research Institute and
School of Chemistry, Building F11
The University of Sydney
NSW, 2006, Australia
E-mail: m.kassiou@chem.usyd.edu.au
Telephone: +61-2-9351-2745
Fax: +61-2-9351-3329
Home Page: http://www.chem.usyd.edu.au/~kassiou

Career Profile:

• BSc (HONS) 1988 PhD 1992 University of NSW
• Research Scientist ANSTO 1991-1996
• Visiting Scientist The Johns Hopkins Medical Institutes (USA) 1993
• Visiting Scientist SHFJ-CEA Life Sciences group (France) 1993
• NIH Fogarty Fellow (National Institute on Drug Abuse USA) 1996
• Principal Hospital Scientist RPAH 1996

Areas of Research:

• Rationale CNS drug design and evaluation
• Medicinal Chemistry, structure-activity relationships of CNS bioactive molecules
• Techniques for studying neuroreceptor-ligand interactions
• Non-invasive imaging of the living brain using functional imaging

Research:

Research in my group is multidisciplinary and at the interface between chemistry and biology. The research is primarily concerned with the understanding of drug-protein and drug-binding site interactions in order to obtain structure-activity relationships of bioactive CNS molecules. This allows the rationale design of more efficacious treatments for diseases of the brain. In addition by using molecular imaging techniques within these fields we are able to better understand the living brain through in vivo studies.

For current research activities and opportunities please visit our home page: http://www.chem.usyd.edu.au/~kassiou

Publications (2007 to 2009):

  1. Leaver, KR; Allbutt, HN; Creber, NJ; Kassiou, M and Henderson, JM. Oral pre-treatment with epigallocatechin gallate in 6-OHDA lesioned rats produces subtle symptomatic relief but not neuroprotection. Brian Research Bulletin, 80 (6), 397-402, 2009. DOI: 10.1016/j.brainresbull.2009.08.013

  2. Doorduin, J; Klein, HC; Dierckx, RA; James, M; Kassiou, M and de Vries, EFJ. [11C]-DPA-713 and [18F]-DPA-714 as new PET tracers for TSPO: A comparison with [11C]-(R)-PK11195 in a rat model of herpes encephalitis. Mol. Imaging Biol., 11 (6), 386-398, 2009. DOI: 10.1007/s11307-009-0211-6

  3. Reynolds, AJ and Kassiou, M. Recent advances in the Mitsunobu reaction: Modifications and applications to biologically active molecules. Current Organic Chemistry, 13 (16), 1610-1632, 2009. DOI: 10.2174/138527209789578144

  4. Ioppolo, JA; Kassiou, M and Rendina, LM. Water-soluble phosphonium salts containing 1,12-dicarba-closo-dodecaborane(12). Tetrahedron Letters, 50 (47), 6457-6461, 2009. DOI: 10.1016/j.tetlet.2009.08.112

  5. Valette, H; Xiao, Y; Peyronneau, M-A; Damont, A; Kozikowski, AP; Wei, Z-L; Kassiou, M; Kellar, KJ; Dolle, F and Bottlaender, M. 18F-ZW-104: A new radioligand for imagning neuronal nicotinic acetylcholine receptors - in vitro binding properties and PET studies in baboons. The Journal of Nuclear Medicine, 50 (8), 1349-1355, 2009. DOI: 10.2967/jnumed.108.061374

  6. Endres, CJ; Pomper, MG; James, M; Uzuner, O; Hammoud, DA; Watkins, CC; Reynolds, A; Hilton, J; Dannals, RF and Kassiou, M. Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans. The Journal of Nuclear Medicine, 50 (8), 1276-1282, 2009. DOI: 10.2967/jnumed.109.062265

  7. 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

  8. 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

  9. Chauveau, F; Van Camp, N; Dolle, F; Kuhnast, B; Hinnen, F; Damont, A; Boutin, H; James, M; Kassiou, M and Tavitian, B. Comparative evaluation of the translocator protein radioligands C-11-DPA-713, F-18-DPA-714, and C-11-PK11195 in a rat model of acute neuroinflammation. Journal of Nuclear Medicine, 50 (3), 468-476, 2009. DOI: 10.2967/jnumed.108.058669

  10. Warraich, ST; Allbutt, HN; Billing, R; Radford, J; Coster, MJ; Kassiou, M and Henderson, JM. Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDAlesion rat model. Brain Research Bulletin, 78 (2-3), (Special Issue), 85-90, 2009. DOI: 10.1016/j.brainresbull.2008.08.023

  11. Truong, L; Allbutt, HN; Coster, MJ; Kassiou, M and Henderson, JM. Behavioural effects of a selective NMDA NR1A/2B receptor antagonist in rats with unilateral 6-OHDA + parafascicular lesions. Brain Research Bulletin, 78 (2-3), (Special Issue), 91-96, 2009. DOI: 10.1016/j.brainresbull.2008.10.004

  12. Kassiou, M; Banati, R; Holsinger, RMD and Meikle, S. Challenges in molecular imaging of Parkinson's disease: A brief overview. Brain Research Bulletin, 78 (2-3), (Special Issue), 105-108, 2009. DOI: 10.1016/j.brainresbull.2008.08.006

  13. 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

  14. Leaver, KR; Allbutt, HN; Creber, NJ; Kassiou, M and Henderson, JM. Neuroprotective effects of a selective N-methyl-D--aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson's desease. Clinical and Experimental Pharmacology and Physiology, 35 (11), 1388-1394, 2008. DOI: 10.1111/j.1440-1681.2008.05046.

  15. Damont, A; Hinnen, F; Kuhnast; B; Schollhorn-Peyronneau, MA; James, M; Luus, C; Tavitian, B; Kassiou, M and Dolle, F. Radiosynthesis of [18F]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) with PET. Journal of Labelled Compounds & Radiopharmaceuticals, 51 (7-8), 286-292, 2008. DOI: 10.1002/jlcr.1523

  16. Besret, L; Dolle, F; Herard, AS; Guillermier, M; Demphel, S; Hinnen, F; Coulon, C; Ottaviani, M; Bottlaender, M; Hantraye, P and Kassiou, M. Dopamine D1 receptor imaging in the rodent and primate brain using the isoquinoline (+)-[11C]A-69024 and positron emission tomography. Journal of Pharmaceutical Sciences, 97 (7), 2811-2819, 2008. DOI: 10.1002/jps.21168

  17. Dolle, F; Langle, S; Roger, G; Fulton, RR; Lagnel-de Bruin, B; Henderson, DJ; Hinnen, F; Paine, T; Coster, MJ; Valette, H; Bottlaender, M and Kassiou, M. Synthesis and in-vivo evaluation of [11C]p-PVP-MEMA as a PET radioligand for imaging nicotinic receptors. Australian Journal of Chemistry, 61 (6), 438-445, 2008. DOI: 10.1071/CH08083

  18. Gunosewoyo, H; Guo, JL; Bennett, MR; Coster, MJ and Kassiou, M. Cubyl amides: Novel P2X7 receptor antagonists. Bioorganic & Medicinal Chemistry Letters, 18 (13), 3720-3723, 2008. DOI: 10.1016/j.bmcl.2008.05.062

  19. James, ML; Fulton, RR; Vercoullie, J; Henderson, DJ; Garreau, L; Chalon, S; Dolle, F; Selleri, S; Guilloteau, D and Kassiou, M. DPA-714, a new translocator protein-specific ligand: Synthesis, radiofluorination, and pharmacologic characterization. Journal of Nuclear Medicine, 49 (5), 814-822, 2008. DOI: 10.2967/jnumed.107.046151

  20. van Dijk, A; Johnston, C; Allbutt, H; Kassiou, M and Henderson, J. Behavioural effects of trishomocubanes in rats with unilateral 6-hydroxydopamine lesions. Behavioural Brain Research, 190 (1), 14-21, 2008. DOI: 10.1016/j.bbr.2008.02.034

  21. Guenther, K; Hambley, TW and Kassiou, M. Radiolabelled probes for imaging multidrug resistance using single photon emission tomography (SPECT) and positron emission tomography (PET). Book chapter in: Multidrug Resistance: Biological and Pharmaceutical Advances in Antitumour Treatment. ISBN: 978-81-308-0258-9, Editor: Nicola Antonio Colabufo, Publisher: Research Signpost, Volume 1, 291-320, 2008.

  22. Naidoo-Variawa, S; Hey-Cunningham, AJ; Lehnert, W; Kench, PL; Kassiou, M; Banati, R and Meikle, SR. High-resolution imaging of the large non-human primate brain using microPET: A feasibility study. Physics in Medicine and Biology, 52 (22), 6627-6638, 2007. DOI: 10.1088/0031-9155/52/22/005

  23. Giboureau, N; Emond, P; Fulton, RR; Henderson, DJ; Chalon, S; Garreau, L; Roselt, P; Eberl, S; Mavel, S; Bodard, S; Fulham, MJ; Guilloteau, D and Kassiou, M. Ex vivo and in vivo evaluation of (2R,3R)-5-[18F]-fluoroethoxy- and fluoropropoxy-benzovesamicol, as PET radioligands for the vesicular acetylcholine transporter. Synapse, 61 (12), 962-970, 2007. DOI: 10.1002/syn.20450

  24. Cagnin, A; Kassiou, M; Meikle, SR and Banati, RB. Positron emission tomography imaging of neuroinflammation. Neurotherapeutics, 4 (3), 443-452, 2007. DOI: 10.1016/j.nurt.2007.04.006

  25. Gunosewoyo, H; Coster, MJ and Kassiou, M. Molecular probes for P2X(7) receptor studies. Current Medicinal Chemistry, 14 (14), 1505-1523, 2007.

  26. Quinlivan, M; Chalon, S; Vergote, J; Henderson, J; Katsifis, A; Kassiou, M and Guilloteau, D. Decreased vesicular acetylcholine transporter and alpha4beta2 nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning. Neuroscience Letters, 415 (2), 97-101, 2007. DOI: 10.1016/j,neulet.2006.08.065

  27. Boutin H; Chauveau, F; Thominiaux, C; Gregoire, MC; James, ML; Trebossen, R; Hantraye, P; Dolle, F; Tavitian, B and Kassiou, M. 11C-DPA-713: A novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. Journal of Nuclear Medicine, 48 (4), 573-581, 2007. DOI: 10.2967/jnumed.106.036764

  28. Liu, X; Banister, SD; Christie, MJ; Banati, R; Meikle, S; Coster, MJ and Kassiou, M. Trishomocubanes: Novel sigma ligands modulate cocaine-induced behavioural effects. European Journal of Pharmacology, 555 (1), 37-42, 2007.

  29. Kassiou, M. Molecular imaging in drug development. Current Pharmaceutical Design, 13 (1), 1-1, 2007. DOI: 10.2174/138161207779313803

  30. Collier, TL; Waterhouse, RN and Kassiou, M. Imaging sigma receptors: Applications in drug development. Current Pharmaceutical Design, 13 (1), 51-72, 2007.

  31. Banister, SD; Clegg, JK; Coster, MJ; Jolliffe. KA and Kassiou, M. (1R,2S,3R,6S,7R,8S)-Tricyclo[6.2.1.02,7]-undeca-4,9-diene-3,6-diol. Acta Crystallographica Section E-Structure Reports Online, E63, o92-o93, 2007. DOI: 10.1107/S1600536806051002

  32. Emond, P; Mavel, S; Zea-Ponce, Y; Kassiou, M; Garreau, L; Bodard, S; Drossard, M-L; Chalon, S and Guilloteau, D. (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter. Nuclear Medicine and Biology, 34, 967-971, 2007. DOI: 10.1016/j.nucmedbio.2007.07.011

  33. Kozikowski, A; Chellappan, SK; Henderson, D; Fulton, R; Giboureau, N; Xiao, Y; Wei, Z-L; Guilloteau, D; Emond, P; Dolle, F; Kellar, KJ and Kassiou, M. Acetylenic pyridines for use in PET imaging of nicotinic receptors. ChemMedChem, 2, 54-57, 2007. DOI: 10.1002/cmdc.200600220
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