Associate Professor Micheal Kassiou
Grants
2012-2014, Glenn Hunt, Iain McGregor, Michael Kassiou. Oxytocin receptor agonists for treatment of social anxiety, National Health and Medical Research Council/Project Grants. $582,350
2011-2013. Michael Kassiou. Louis Rendina, Michael Kassiou. The Development of Carboranes as New Agents in the Diagnosis and Treatment of Brain Disease, Australian Research Council/Discovery Projects (DP). $420,000.00
2011-2013. Iain McGregor. Glenn Hunt, Michael Kassiou, Iain McGregor. Preclinical validation of oxytocin as a novel treatment for alcohol dependence, National Health and Medical Research Council/Project Grants. $500,022.00
2011-2011. Richard Payne. Mary Collins, Trevor Hambley, Katrina Jolliffe, Michael Kassiou, Richard Payne,. Preparative High-Performance Liquid Chromatography (HPLC), National Health and Medical Research Council/Equipment Grants. $74,461.00
2010 - 2012. Michael Kassiou, Trevor Hambley. Radiolabelled MMP Binding Agents for the Identification, Quantification, and Targeting of MMPs in CNS Disorders and Tumours, Australian Research Council/Discovery Projects (DP). $429,000
2010 - 2012. Maxwell Bennett, Iain McGregor, Michael Kassiou. Purinergic P2X7 Receptor as a Target for Antidepressant Drug Discovery, National Health and Medical Research Council/Project Grants. $547,500
2010 - 2012. Michael Kassiou, Lars Ittner. The translocator protein (TSPO) as a novel target for the treatment of Alzheimer's Disease, National Health and Medical Research Council/Project Grants. $607,500
2008 - 2008. Michael Kassiou, Louis Rendina. The Targeting of Brain Tumours by a New Class of Agents for Boron Neutron Capture Therapy, Cure Cancer Australia Foundation/Research Support. $75,000
2008 - 2010. Michael Kassiou. Developmnet of Novel Radiolabelled Molecular Probes for Studying Diseases of the Brain, Department of Innovation, Industry, Science and Research (Federal)/International Science Linkages (ISL) Competitive Grants. $307,785
2007 - 2007. Michael Kassiou, Jasmine Henderson. Evaluation of a selective NMDA NR1A/2B receptor antagonist as a drug treatment in an animal model of Parkinsons disease, Australian Rotary Health Research Fund/Research Support. $50,089
2005 - 2008. Richard Banati, Maxwell Bennett, Michael Kassiou, John Prineas, John Pollard, . Glial and neuroinflammatory mechanisms of neuronal degeneration and regeneration: The functional states of microglia in central nervous system and macrophages in the peripheral nervous system., Office for Science and Medical Research (NSW)/Research Support. $1,000,000
2005 - 2007. Michael Kassiou, Jasmine Henderson. Evaluation of a selective NMDA NR1A/2B receptor antagonist as a drug treatment in an animal model of Parkinsons disease., Australian Rotary Health Research Fund/Research Support. $99,000
2004 - 2007. Denis Guilloteau, Michael Kassiou. Functional in vivo imaging of neurodegenerative disorders of the brain using PET & SPECT, Department of Education, Science and Training (Federal)/Innovation Access Programme (IAP): International Science and Technology. $36,800
2003 - 2005. Michael Kassiou, Jasmine Henderson. Trishomocubanes: Potential neuroprotective drug therapies for Parkinsons disease, Brain Foundation/Annual Research Awards. $20,000
2003 - 2003. Michael Kassiou. Development of radioligands for imaging the NMDA receptor using Positron Emission Tomography (PET), Embassy of France in Australia/Research Support. $4,500
Publications
2011
Issa, F, Kassiou, M, Rendina, L M 2011, Boron in drug discovery: Carboranes as unique pharmacophores in biologically active compounds, Chemical Reviews, 111(9), 5701-5722
Moussa, I A, Banister, S D, Akladios, F N , Chua, S W, Kassiou, M 2011, Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazine sigma(1) receptor ligands, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(19), 5707-5710
Banister, S D, Moussa, I A, Jorgensen, W T , Chua, S W, Kassiou, M 2011, Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(12), 3622-3626
Banister, S D, Yoo, D T , Chua, S W, Cui, J, Mach, R, Kassiou, M 2011, N-arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (sigma) receptor ligands, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(18), 5289-5292
Ribeiro, M, Vercouillie, J, Tauber, C, Venel, Y, Baulieu, J, Maia, S, Reynolds, A J, Kassiou, M, Guilloteau, D, Corcia, P 2011, P-167 The potential interest of the PET radioligand (18)F-DPA-714 in neuroinflammation, Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S256-S256
Boucher, A A, Arnold, J C, Hunt, G E, Spiro, A, Spencer, J R, Brown, C, McGregor, I S, Bennett, M R, Kassiou, M 2011, Resilience and Reduced C-FOS Expression in P2X7 Receptor Knockout Mice Exposed to Repeated Forced Swim Test, Neuroscience, 189, 170-177
Crossley, E L, Issa, F, Scarf, A M, Kassiou, M, Rendina, L M 2011, Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells, Chemical Communications, 47(44), 12179-12181
Moussa, I A, Banister, S D, Giboureau, N, Meikle, S R, Kassiou, M 2011, Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(22), 6820-6823
Moussa, I A, Banister, S D, Giboureau, N, Meikle, S R, Kassiou, M 2011, Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N′-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ 1 receptor PET imaging agent, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, in press
Damont, A, Boisgard, R, Kuhnast, B, Lemee, F, Raggiri, G, Scarf, A M, Da Pozzo, E, Selleri, S, Martini, C, et al 2011, Synthesis of 6-[(18)F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(16), 4819-4822
Banister, S D, Moussa, I A, Beinat, C, Reynolds, A J, Schiavini, P, Jorgensen, W T , Kassiou, M 2011, Trishomocubane as a Scaffold for the Development of Selective Dopamine Transporter (DAT) Ligands, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(1), 38-41
Martin, A, Boisgard, R, Kassiou, M, Dolle, F, Tavitian, B 2011, Reduced PBR/TSPO Expression After Minocycline Treatment in a Rat Model of Focal Cerebral Ischemia: A PET Study Using [(18)F]DPA-714, Molecular Imaging and Biology, 13(1), 10-15
Scarf, A M, Kassiou, M 2011, The translocator protein, The Journal of Nuclear Medicine, 52(5), 677-680
Drake, C, Boutin, H, Jones, M, Denes, A, McColl, B, Selvarajah, J, Hulme, S, Georgiou, R, Hinz, R, et al 2011, Brain inflammation is induced by co-morbidities and risk factors for stroke, Brain, Behavior, and Immunity, 25(6), 1113-1122
2010
Conference Contributions
Fulton, R R, Meikle, S R, Kyme, A, Zhou, W V, Popovic, K, Kassiou, M, Akhtar, M 2010, Motion-corrected microPET brain imaging of conscious rats, 2009 World Molecular Imaging Conference, Online, USB drive/online
Journal Articles
Banister, S D, Clegg, J K, Hanani, R, Kassiou, M 2010, 11-{[2-(3-fluorophenyl)ethyl](methyl)-amino}pentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]-undecan-8-one, Acta Crystallographica. Section E: Structure Reports Online, 66(10), o2693-o2693
Banister, S D, Moussa, I A, Jordan, M J, Coster, M, Kassiou, M 2010, Oxo-bridged isomers of aza-trishomocubane sigma (o) receptor ligands:Synthesis, in vitro binding, and molecular modeling, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 20(1), 145-148
Fulton, R R, Meikle, S R, Kyme, A, Zhou, W V, Akhtar, M, Kassiou, M, Popovic, K, Karlsson, I J 2010, Imaging the awake rat brain with microPET, head tracking and motion correction, 5th International Conference on Imaging Technologies in Biomedical Sciences (ITBS 2009), not known , not known
Gunosewoyo, H, Kassiou, M 2010, P2X purinergic receptor ligands: Recently patented compounds, Expert Opinion on Therapeutic Patents, 20(5), 625-646
Luus, C A, Hanani, R, Reynolds, A J, Kassiou, M 2010, The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned?, Journal of Labelled Compounds and Radiopharmaceuticals, 53(7), 501-510
Moussa, I A, Banister, S D, Beinat, C, Giboureau, N, Reynolds, A J, Kassiou, M 2010, Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands, Journal of Medicinal Chemistry, 53(16), 6228-6239
Naidoo (Naidoo-Variawa), S, Lehnert, W, Kassiou, M, Banati, R B, Meikle, S R 2010, Attenuation correction for the large non-human primate brain imaging using microPET, Physics in Medicine and Biology, 55(8), 2351-2363
Reynolds, A J, Hanani, R, Hibbs, D E, Damont, A, Da Pozzo, E, Selleri, S, Dolle, F, Martini, C, Kassiou, M 2010, 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: the tetrahedron journal for research at the interface of chemistry and biology, 20(19), 5799-5802
2009
Conference Contributions
Fulton, R. R., Meikle, S. R., Kyme, A., Zhou, W. V., Popovic, K., Kassiou, M., and Akhtar, M., 2009, Motion corrected microPET rain imaging of conscious rats, 2009 World Molecular Imaging Conference, Montreal, Canada, 2009-09-23 , 2009-09-26
Kassiou, M., 2009, Discovery of new therapeutic immunomodulator drugs as a pathway for treating brain disease (POSTER/TALK), Plant Nutraceuticals and Bioactive Molecules: A Growth Opportunity for the Pharmaceutical Industry in Australia and India, Ootacamund, India, 2009-06-02 , 2009-06-05
Kassiou, M., 2009, Imaging immune response in the CNS - Applications for therapeutic development (POSTER/TALK), 7th AFMC International Medicinal Chemistry Symposium, Cairns, QLD Australia, 2009-08-23 , 2009-08-27
Banister, S. D., Coster, M., and Kassiou, M., 2009, A versatile polycyclic scaffold for the discovery of selective sigma (sigma) receptor ligands (POSTER/TALK), 7th AFMC International Medicinal Chemistry Symposium, Cairns, QLD Australia, 2009-08-23 , 2009-08-27
Moussa, I. A., Coster, M., and Kassiou, M., 2009, Synthesis and pharmacological evaluation of novel sigma receptor ligands (POSTER/TALK), 7th AFMC International Medicinal Chemistry Symposium, Cairns, QLD Australia, 2009-08-23 , 2009-08-27
Moussa, I. A., Coster, M., and Kassiou, M., 2009, Synthesis and pharmacological evaluation of novel sigma receptor ligands (POSTER by Moussa), 7th AFMC International Medicinal Chemistry Symposium, Cairns, QLD Australia, 2009-08-23 , 2009-08-27
Fulton, R. R., Meikle, S. R., Kyme, A., Zhou, W. V., Akhtar, M., Kassiou, M., Popovic, K., and Karlsson, I. J., 2009, Imaging the awake rat brain with microPET, head tracking and motion correction., 5th International Conference on Imaging Technologies in Biomedical Sciences, Milos, Greece, 2009-09-13 , 2009-09-16
Journal Articles
Ioppolo, J. A., Kassiou, M., and Rendina, L. M., 2009, Water-soluble phosphonium salts containing 1,12-dicarba-closo-dodecaborane(12), Tetrahedron Letters, 50[47], 6457-6461
Warraich, S. T., Allbutt, H. N., Billing, R. L., Radford, J., Coster, M., Kassiou, M., and Henderson, J. M., 2009, Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat model, Brain Research Bulletin, 78[2-3], 85-90
Dolle, F., Damont, A., Valette, H., Hinnen, F., Kuhnast, B., Saba, W., Schollhorn-Peyronneau, M., Kozikowski, A., Bottlaender, M., and Kassiou, M., 2009, ZW-102 and ZW-104, two novel fluorine-18 labelled radioligands for imaging nicotinic acetylcholine receptors with PET, Journal of Labelled Compounds and Radiopharmaceuticals, 52[S1], S364-S364
Endres, C., Pomper, M., James, M. L., Uzuner, O., Hammoud, D., Watkins, C., Reynolds, A. J., Hilton, J., Dannals, R., and Kassiou, M., 2009, Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans, The Journal of Nuclear Medicine, 50[8], 1276-1282
Reynolds, A. J., and Kassiou, M., 2009, Recent advances in the Mitsunobu reaction:; Modifications and applications to biologically active molecules, Current Organic Chemistry, 13[16], 1610-1632
Leaver, K. R., Allbutt, H. N., Creber, N. J., Kassiou, M., and Henderson, J. M., 2009, Oral pre-treatment with epigallocatechin gallate in 6-OHDA lesioned rats produces subtle symptomatic relief but not neuroprotection, Brain Research Bulletin, 80[6], 397-402
Doorduin, J., Klein, H., Dierckx, R., James, M. L., Kassiou, M., and De Vries, E., 2009, [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, Molecular Imaging and Biology, 11[6], 386-398
Edington, A. R., McKinzie, A. A., Reynolds, A. J., Kassiou, M., Ryan, R. M., and Vandenberg, R. J., 2009, Extracellular loops 2 and 4 of GLYT2 are required for N-arachidonylglycine inhibition of glycine transport, Journal of Biological Chemistry, 284[52], 36424-36430
Scarf, A. M., Ittner, L., and Kassiou, M., 2009, The translocator protein (18 kDa): Central nervous system disease and drug design, Journal of Medicinal Chemistry, 52[3], 581-592
Chauveau, F., Van Camp, N., Dolle, F., Kuhnast, B., Hinnen, F., Damont, A., Boutin, H., James, M. L., Kassiou, M., and Tavitian, B., 2009, Comparative evaluation of the translocator protein radioligands (11)C-DPA-713, (18)F-DPA-714, and (11)C-PK11195 in a rat model of acute neuroinflammation, The Journal of Nuclear Medicine, 50[3], 468-476
Kassiou, M., Banati, R. B., Holsinger, R. M., and Meikle, S. R., 2009, Challenges in molecular imaging of Parkinson's disease: A brief overview, Brain Research Bulletin, 78[2-3], 105-108
Gunosewoyo, H., Coster, M., Bennett, M. R., and Kassiou, M., 2009, Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening, Bioorganic & Medicinal Chemistry, 17[14], 4861-4865
Dolle, F., Luus, C. A., Reynolds, A. J., and Kassiou, M., 2009, Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography, Current Medicinal Chemistry, 16[22], 2899-2923
Truong, L., Allbutt, H. N., Coster, M., Kassiou, M., and Henderson, J. M., 2009, Behavioural effects of a selective NMDA NR1A/2B receptor antagonist in rats with unilateral 6-OHDA+ parafascicular lesions, Brain Research Bulletin, 78[2-3], 91-96
Damont, A., van Camp, N., Kuhnast, B., Hinnen, F., Boisgard, R., Chauveau, F., Boutin, H., Probst, K., Clark, J., Katsifis, A., and Kassiou, M., 2009, [18F]DPA-714, [18F]PBR111 and [18F]FEDAA1106 as potent PBR pet-imaging candidates: Radiosynthesis and comparative studies, Journal of Labelled Compounds and Radiopharmaceuticals, 52, S122-S122
2008
Leaver, K R, Allbutt, H N, Creber, N J, Kassiou, M, Henderson, J M 2008, Neuroprotective effects of a selective N-methyl-D-aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson's disease, Clinical and Experimental Pharmacology & Physiology, 35(11), 1388-1394
van Dijk, A, Johnston, C I, Allbutt, H N, Kassiou, M, Henderson, J M 2008, Behavioural effects of trishomocubanes in rats with unilateral 6-hydroxydopamine lesions, Behavioural Brain Research, 190(1), 14-21
James, M L, Fulton, R, Vercoullie, J, Henderson, D, Garreau, L, Chalon, S, Dolle, F, Selleri, S, Guilloteau, D, Kassiou, M 2008, DPA-714, a New Translocator Protein-Specific Ligand: Synthesis, Radiofluorination, and Pharmacologic Characterization, The Journal of Nuclear Medicine, 49(5), 814-822
Gunosewoyo, H, Liu, G J, Bennett, M R, Coster, M, Kassiou, M 2008, Cubyl amides: Novel P2X(7) receptor antagonists, Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 18(13), 3720-3723
Guenther, K J, Hambley, T W, Kassiou, M 2008, Radiolabelled probes for imaging multidrug resistance using single photon emission tomography (SPECT) and positron emission tomography (PET), Multidrug Resistance: Biological and Pharmaceutical Advances in Antitumour Treatment, Research Signpost, India, 1, 291-320
Dolle, F, Langle, S, Roger, G, Fulton, R, Lagnel, B, Henderson, D, Hinnen, F, Paine, T L, Coster, M, Valette, H, Bottlaender, M, Kassiou, M 2008, Synthesis and In-Vivo Evaluation of [(11)C]p-PVP-MEMA as a PET Radioligand for Imaging Nicotinic Receptors, Australian Journal of Chemistry: an international journal for chemical science, 61(6), 438-445
Damont, A, Hinnen, F, Kuhnast, B, Schollhorn-Peyronneau, M, James, M L, Luus, C A, Tavitian, B, Kassiou, M, Dolle, F 2008, Radiosynthesis of [(18)F]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) PET, Journal of Labelled Compounds and Radiopharmaceuticals, 51(7-8), 286-292
Besret, L, Dolle, F, Herard, A, Guillermier, M, Demphel, S, Hinnen, F, Coulon, C, Ottaviani, M, Bottlaender, M, Hantraye, P, Kassiou, M 2008, Dopamine D1 Receptor Imaging in the Rodent and Primate Brain Using the Isoquinoline (+)-[(11)C]A-69024 and Positron Emission Tomography, Journal of Pharmaceutical Sciences, 97(7), 2811-2819
2007
Gunosewoyo, H, Coster, M, Kassiou, M 2007, Molecular probes for P2X7 receptor studies, Current Medicinal Chemistry, 14(14), 1505-1523
Banister, S D, Clegg, J K, Coster, M, Jolliffe, K A, Kassiou, M 2007, (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(0), o92-o93
Boutin, H, Chauveau, F, Thominiaux, C, Gregoire, M, James, M, Trebossen, R, Hantraye, P, Dolle, F, Tavitian, B, Kassiou, M 2007, 11C-DPA-713: A novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation, The Journal of Nuclear Medicine, 48(4), 573-581
Cagnin, A, Kassiou, M, Meikle, S R, Banati, R B 2007, Positron emission tomography imaging of neuroinflammation, Neurotherapeutics, 4(3), 443-452
Giboureau, N, Emond, P, Fulton, R, Henderson, D, Chalon, S, Garreau, L, Roselt, P, Eberl, S, Mavel, S, Bodard, S, Fulham, M, Guilloteau, D, Kassiou, M 2007, 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), 962-670
Kozikowski, A, Chellappan, S, Henderson, D J, Fulton, R R, Giboureau, N, Xiao, Y, Wei, Z, Guilloteau, D, Emond, P, Dolle, F, Kellar, K, Kassiou, M 2007, Acetylenic pyridines for use in PET imaging of nicotinic receptors, ChemMedChem: chemistry enabling drug discovery, 2(0), 54-57
Liu, X, Banister, S D, Christie, M J, Banati, R B, Meikle, S R, Coster, M, Kassiou, M 2007, Trishomocubanes: Novel sigma ligands modulate cocaine-induced behavioural effects, European Journal of Pharmacology, 555(1), 37-42
Naidoo-Variawa, S, Hey Cunningham, AJ, Lehnert, W, Kench, P L, Kassiou, M, Banati, R B, Meikle, S R 2007, High-resolution imaging of the large non-human primate brain using microPET: a feasibility study, Physics in Medicine and Biology, 52(22), 6627-6638
Emond, P, Mavel, S, Zea-Ponce, Y, Kassiou, M, Garreau, L, Bodard, S, Drossard, M, Chalon, S, Guilloteau, D 2007, (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter, Nuclear Medicine and Biology, 34(8), 967-971
Quinlivan, M O, Chalon, S, Vergote, J, Henderson, J M, Katsifis, A, Kassiou, M, Guilloteau, D 2007, Decreased vesicular acetylcholine transporter and alpha-4beta-2 nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning, Neuroscience Letters, 415(0), 97-101
2006
Liu, X, Banister, S D, Christie, M J, Banati, R B, Meikle, S R, Coster, M, Kassiou, M 2006, Trishomocubanes: Novel Sigma ligands modulate cocaine-induced behavioural effects, European Journal of Pharmacology, 555(1), 37-42
Cagnin, A, Kassiou, M, Meikle, S R, Banati, R B 2006, In vivo evidence for microglial activation in neurodegenerative dementia, Acta Neurologica Scandinavica, 114(Supplement 185), 107-114