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Professor Michael Kassiou

Professor
Pharmacology, School of Medical Sciences
Brain & Mind Research Institute

M02 - Mallet Street Campus
The University of Sydney
NSW 2006 Australia

T:+61 2 9351 0849
F:+61 2 9351 9146
E:

Biographical details

Michael Kassiou is Professor of Medicinal Chemistry at the University of Sydney and Head of the Drug Discovery Research Unit at the Brain and Mind Research Institute. Professor Kassiou has been responsible for fundamental contributions in a number of areas which encompass the interface between chemistry and biology. His group 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. [More...]

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Research interests

Drug discovery, Rationale CNS drug design and evaluation, Medicinal Chemistry, Structure-activity relationships of CNS bioactive molecules, Techniques for studying neuroreceptor-ligand interactions.

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Current national competitive grants*

2011

The Development of Carboranes as New Agents in the Diagnosis and Treatment of Brain Disease
Kassiou M, Rendina L
ARC Discovery Project ($420,000 over 3 years)

2010

Purinergic P2X7 Receptor as a Target for Antidepressant Drug Discovery
Kassiou M, McGregor I, Bennett M
NHMRC Project Grant ($547,500 over 3 years)

* Grants administered through the University of Sydney

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Keywords

Medicinal chemistry; Drug design; Pharmacology

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Publications

2011 | 2010 | 2009 | 2008 | 2007 | 2006

2011

  
  • Crossley, E., Issa, F., Scarf, A., Kassiou, M., Rendina, L. 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 (Cambridge, England). 2011; 47:12179-81. [Abstract]
  • Moussa, I., Banister, S., Giboureau, N., Meikle, S., Kassiou, M. Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel ?1 receptor PET imaging agent. Bioorganic & medicinal chemistry letters. 2011; 21:6820-3. [Abstract]
  • Moussa, I., Banister, S., Akladios, F., Chua, S., Kassiou, M. Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazine ??(1) receptor ligands. Bioorganic & medicinal chemistry letters. 2011; 21:5707-10. [Abstract]
  • Banister, S., Yoo, D., Chua, S., Cui, J., Mach, R., Kassiou, M. N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (??) receptor ligands. Bioorganic & medicinal chemistry letters. 2011; 21:5289-92. [Abstract]
  • Issa, F., Kassiou, M., Rendina, L. Boron in Drug Discovery: Carboranes as Unique Pharmacophores in Biologically Active Compounds. Chemical reviews. 2011; 111:5701-22. [Abstract]
  • Boucher, A., Arnold, J., Hunt, G., Spiro, A., Spencer, J., Brown, C., McGregor, I., Bennett, M., Kassiou, M. Resilience and reduced c-Fos expression in P2X7 receptor knockout mice exposed to repeated forced swim test. Neuroscience. 2011; 189:170-7. [Abstract]
  • Drake, C., Boutin, H., Jones, M., Denes, A., McColl, B., Selvarajah, J., Hulme, S., Georgiou, R., Hinz, R., Gerhard, A., Vail, A., Prenant, C., Julyan, P., Maroy, R., Brown, G., Smigova, A., Herholz, K., Kassiou, M., Crossman, D., Francis, S., Proctor, S., Russell, J., Hopkins, S., Tyrrell, P., Rothwell, N., Allan, S. Brain inflammation is induced by co-morbidities and risk factors for stroke. Brain, Behavior, and Immunity. 2011; 25:1113-1122. [Abstract]
  • Banister, S., Moussa, I., Jorgensen, W., Chua, S., Kassiou, M. 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 (??) receptor ligands modulates off-target activity and subtype selectivity. Bioorganic & medicinal chemistry letters. 2011; 21:3622-6. [Abstract]
  • Scarf, A., Kassiou, M. The Translocator Protein. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2011; 52:677-80. [Abstract]
  • Martín, A., Boisgard, R., Kassiou, M., Dollé, F., Tavitian, B. 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. 2011; 13:10-15. [Abstract]
  • Banister, S., Moussa, I., Beinat, C., Reynolds, A., Schiavini, P., Jorgensen, W., Kassiou, M. Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands. Bioorganic & medicinal chemistry letters. 2011; 21:38-41. [Abstract]

2010

  
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  • Morrison, D., Issa, F., Bhadbhade, M., Groebler, L., Witting, P., Kassiou, M., Rutledge, P., Rendina, L. Boronated phosphonium salts containing arylboronic acid, closo-carborane, or nido-carborane: synthesis, X-ray diffraction, in vitro cytotoxicity, and cellular uptake. Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry. 2010; 15:1305-18. [Abstract]
  • Reynolds, A., Hanani, R., Hibbs, D., Damont, A., Pozzo, E., Selleri, S., Dollé, F., Martini, C., Kassiou, M. Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18kDa translocator protein (TSPO). Bioorganic & medicinal chemistry letters. 2010; 20:5799-802. [Abstract]
  • Moussa, I., Banister, S., Beinat, C., Giboureau, N., Reynolds, A., Kassiou, M. Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands. Journal of Medicinal Chemistry. 2010; 53:6228-6239. [Abstract]
  • Gunosewoyo, H., Kassiou, M. P2X purinergic receptor ligands: recently patented compounds. Expert opinion on therapeutic patents. 2010; 20:625-46. [Abstract]
  • Naidoo-Variawa, S., Lehnert, W., Kassiou, M., Banati, R., Meikle, S. Attenuation correction for the large non-human primate brain imaging using microPET. Physics in Medicine and Biology. 2010; 55:2351-2363. [Abstract]
  • Banister, S., Clegg, J., Hanani, R., Kassiou, M. 11-{[2-(3-Fluorophenyl)ethyl](methyl)-amino}pentacyclo[5.4.0.02,6.03,10.05,9]-undecan-8-one. Acta Crystallographica. Section E: Structure Reports Online. 2010; 66:o2693.
  • Luus, C., Hanani, R., Reynolds, A., Kassiou, M. The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned?. Journal of Labelled Compounds and Radiopharmaceuticals. 2010; 53:501-510.
  • Giboureau, N., Aumann, K., Beinat, C., Kassiou, M. Development of Vesicular Acetylcholine Transporter Ligands: Molecular Probes for Alzheimer's Disease. Current Bioactive Compounds. 2010; 6:129-155.
  • Martin, A., Boisgard, R., Theze, B., Van Camp, N., Kuhnast, B., Damont, A., Kassiou, M., Dolle, F., Tavitian, B. Evaluation of the PBR/TSPO radioligand F-18 DPA-714 in a rat model of focal cerebral ischemia. Journal of Cerebral Blood Flow and Metabolism. 2010; 30:230-241. [Abstract]
  • Beinat, C., Banister, S., Moussa, I., Reynolds, A., McErlean, C., Kassiou, M. Insights into Structure-Activity Relationships and CNS Therapeutic Applications of NR2B Selective Antagonists. Current medicinal chemistry. 2010; 17:4166-90. [Abstract]
  • Giboureau, N., Som, I., Boucher-Arnold, A., Guilloteau, D., Kassiou, M. PET Radioligands for the Vesicular Acetylcholine Transporter (VAChT). Current Topics in Medicinal Chemistry. 2010; 10:1569-1583. [Abstract]
  • Banister, S., Moussa, I., Jordan, M., Coster, M., Kassiou, M. Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling. Bioorganic & medicinal chemistry letters. 2010; 20:145-148. [Abstract]

2009

  
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  • Edington, A., McKinzie, A., Reynolds, A., Kassiou, M., Ryan, R., Vandenberg, R. Extracellular loops 2 and 4 of GLYT2 are required for N-arachidonyl-glycine inhibition of glycine transport. The Journal of biological chemistry. 2009; 284:36424-30. [Abstract]
  • Leaver, K., Allbutt, H., Creber, N., Kassiou, M., Henderson, J. Oral pre-treatment with epigallocatechin gallate in 6-OHDA lesioned rats produces subtle symptomatic relief but not neuroprotection. Brain Research Bulletin. 2009; 80:397-402. [Abstract]
  • Valette, H., Xiao, Y., Peyronneau, M., Damont, A., Kozikowski, A., Wei, Z., Kassiou, M., Kellar, K., Dollé, F., Bottlaender, M. 18F-ZW-104: A New Radioligand for Imaging Neuronal Nicotinic Acetylcholine Receptors--In Vitro Binding Properties and PET Studies in Baboons. Journal of nuclear medicine. 2009; 50:1349-1355. [Abstract]
  • Endres, C., Pomper, M., James, M., Uzuner, O., Hammoud, D., Watkins, C., Reynolds, A., Hilton, J., Dannals, R., Kassiou, M. Initial Evaluation of 11C-DPA-713, a Novel TSPO PET Ligand, in Humans. Journal of nuclear medicine. 2009; 50:1276-1282. [Abstract]
  • Gunosewoyo, H., Coster, M., Bennett, M., Kassiou, M. Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening. Bioorganic & medicinal chemistry. 2009; 17:4861-5. [Abstract]
  • Kassiou, M., Banati, R., Holsinger, R., Meikle, S. Challenges in molecular imaging of Parkinson's disease: A brief overview. Brain research bulletin. 2009; 78:105-8. [Abstract]
  • Warraich, S., Allbutt, H., Billing, R., Radford, J., Coster, M., Kassiou, M., Henderson, J. Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat model. Brain research bulletin. 2009; 78:85-90. [Abstract]
  • Henderson, J., Lanciego, J., Smith, Y., Gundlach, A., Kassiou, M., , O. Proceedings of the 2007 International Brain Research Organisation Satellite Meeting "Movement Disorders: Focus on the Thalamus and Basal Ganglia" held in Sydney, Australia, 10-11 July, 2007. Brain research bulletin. 2009; 78:53-4. [Abstract]
  • Truong, L., Allbutt, H., Coster, M., Kassiou, M., Henderson, J. Behavioural effects of a selective NMDA NR1A/2B receptor antagonist in rats with unilateral 6-OHDA+parafascicular lesions. Brain research bulletin. 2009; 78:91-6. [Abstract]
  • Scarf, A., Ittner, L., Kassiou, M. The translocator protein (18 kDa): central nervous system disease and drug design. Journal of Medicinal Chemistry. 2009; 52:581-592. [Abstract]
  • Ioppolo, J., Kassiou, M., Rendina, L. Water-soluble phosphonium salts containing 1,12-dicarba-closo-dodecaborane(12). Tetrahedron Letters. 2009; 50:6457-6461. [Abstract]
  • Doorduin, J., Klein, H., Dierckx, R., James, M., Kassiou, M., de Vries, E. [C-11]-DPA-713 and [F-18]-DPA-714 as New PET Tracers for TSPO: A Comparison with [C-11]-(R)-PK11195 in a Rat Model of Herpes Encephalitis. Molecular Imaging and Biology. 2009; 11:386-398. [Abstract]
  • Chauveau, F., Van Camp, N., Dolle, F., Kuhnast, B., Hinnen, F., Damont, A., Boutin, H., James, M., Kassiou, M., 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. 2009; 50:468-476. [Abstract]
  • Dollé, F., Luus, C., Reynolds, A., Kassiou, M. Radiolabelled Molecules for Imaging the Translocator Protein (18 kDa) Using Positron Emission Tomography. Current medicinal chemistry. 2009; 16:2899-2923. [Abstract]

2008

  
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  • Leaver, K., Allbutt, H., Creber, N., Kassiou, M., Henderson, J. 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. 2008; 35:1388-94. [Abstract]
  • Besret, L., Dollé, F., Hérard, A., Guillermier, M., Demphel, S., Hinnen, F., Coulon, C., Ottaviani, M., Bottlaender, M., Hantraye, P., 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. 2008; 97:2811-2819. [Abstract]
  • Gunosewoyo, H., Guo, J., Bennett, M., Coster, M., Kassiou, M. Cubyl amides: Novel P2X(7) receptor antagonists. Bioorganic & medicinal chemistry letters. 2008; 18:3720-3. [Abstract]
  • van Dijk, A., Johnston, C., Allbutt, H., Kassiou, M., Henderson, J. Behavioural effects of trishomocubanes in rats with unilateral 6-hydroxydopamine lesions. Behavioural Brain Research. 2008; 190:14-21. [Abstract]
  • James, M., Fulton, R., Vercoullie, J., Henderson, D., Garreau, L., Chalon, S., Dolle, F., Selleri, S., Guilloteau, D., Kassiou, M. DPA-714, a New Translocator Protein-Specific Ligand: Synthesis, Radiofluorination, and Pharmacologic Characterization. Journal of nuclear medicine. 2008; 49:814-822. [Abstract]
  • Damont, A., Hinnen, F., Kuhnast, B., Schollhorn-Peyronneau, M., James, M., Luus, C., Tavitian, B., Kassiou, M., Dolle, F. Radiosynthesis of [F-18]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) with PET. Journal of Labelled Compounds & Radiopharmaceuticals. 2008; 51:286-292. [Abstract]
  • Dollé, F., Langle, S., Roger, G., Fulton, R., Lagnel-de Bruin, B., Henderson, D., Hinnen, F., Paine, T., Coster, M., Valette, H., Bottlaender, M., Kassiou, M. Synthesis and In-Vivo Evaluation of [11C]p-PVP-MEMA as a PET Radioligand for Imaging Nicotinic Receptors. Australian Journal of Chemistry. 2008; 61:438–445.
  • Guenther, K., Hambley, T., Kassiou, M. Radiolabelled probes for imaging multidrug resistance using single photon emission tomography (SPECT) and positron emission tomography (PET). In: Multidrug Resistance: Biological and Pharmaceutical Advances in Antitumour Treatment. India: Research Signpost 2008. p. 291-320.

2007

  
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  • Naidoo-Variawa, S., Hey-Cunningham, A., Lehnert, W., Kench, P., Kassiou, M., Banati, R., Meikle, S. High-resolution imaging of the large non-human primate brain using microPET: a feasibility study. Physics in medicine and biology. 2007; 52:6627-38. [Abstract]
  • Quinlivan, M., Chalon, S., Vergote, J., Henderson, J., Katsifis, A., Kassiou, M., Guilloteau, D. Decreased vesicular acetylcholine transporter and alpha(4)beta(2) nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning. Neuroscience letters. 2007; 415:97-101. [Abstract]
  • Liu, X., Banister, S., Christie, M., Banati, R., Meikle, S., Coster, M., Kassiou, M. Trishomocubanes: Novel sigma ligands modulate cocaine-induced behavioural effects. European journal of pharmacology. 2007; 555:37-42. [Abstract]
  • Banister, S., Clegg, J., Coster, M., Jolliffe, K., Kassiou, M. (1R,2S,3R,6S,7R,8S)-Tricyclo[6.2.1.0(2,7)]-undeca-4,9-diene-3,6-diol. ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE. 2007; 63:O92-O93. [Abstract]
  • Roselt, P., Kassiou, M., Guilloteau, D., Fulham, M., Bodard, S., Eberl, S., Garreau, L., Chalon, S., Henderson, D., Fulton, R., Emond, P., Giboureau, N., Mavel, S. Ex vivo and in vivo evaluation of (2R,3R)-5-[F-18]-fluoroethoxy- and fluoropropoxy-benzovesamicol, as PET radioligands for the vesicular acetylcholine transporter. SYNAPSE. 2007; 61:962-970. [Abstract]
  • Tavitian, B., Kassiou, M., Dolle, F., Hantraye, P., Trebossen, R., Gregoire, M., Thominiaux, C., Chauveau, F., Boutin, H., James, M. C-11-DPA-713: A novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. JOURNAL OF NUCLEAR MEDICINE. 2007; 48:573-581. [Abstract]
  • Kassiou, M., Meikle, S., Cagnin, A., Banati, R. Positron emission tomography imaging of neuroinflammation. Neurotherapeutics. 2007; 4:443-452. [Abstract]
  • Gunosewoyo, H., Coster, M., Kassiou, M. Molecular probes for P2X7 receptor studies. Current medicinal chemistry. 2007; 14:1505-1523. [Abstract]
  • Collier, T., Waterhouse, R., Kassiou, M. Imaging sigma receptors: applications in drug development. Current pharmaceutical design. 2007; 13:51-72. [Abstract]

2006

  
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  • Assaad, T., Mavel, S., Parsons, S., Kruse, S., Galineau, L., Allouchi, H., Kassiou, M., Chalon, S., Guilloteau, D., Emond, P. Synthesis and in vitro evaluation of N-substituted aza-trozamicol analogs as vesicular acetylcholine transporter ligands. Bioorganic & Medicinal Chemistry Letters. 2006; 16:2654-2657. [Abstract]
  • Thominiaux, C., Dolle, F., James, M., Bramoulle, Y., Boutin, H., Besret, L., Gregoire, M., Valette, H., Bottlaender, M., Tavitian, B., Hantraye, P., Selleri, S., Kassiou, M. Improved synthesis of the peripheral benzodiazepine receptor ligand C-11 DPA-713 using C-11 methyl triflate. Applied Radiation and Isotopes. 2006; 64:570-573. [Abstract]
  • Truong, L., Allbutt, H., Kassiou, M., Henderson, J. Developing a preclinical model of Parkinson's disease: a study of behaviour in rats with graded 6-OHDA lesions. Behavioural brain research. 2006; 169:1-9. [Abstract]
  • Thominiaux, C., de Bruin, B., Bramoulle, Y., Hinnen, F., Demphel, S., Valette, H., Bottlaender, M., Besret, L., Kassiou, M., Dolle, F. Radiosynthesis of (E)-N-(2- C-11 methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor antagonist. Applied Radiation and Isotopes. 2006; 64:348-354. [Abstract]
  • Vercouillie, J., Mavel, S., Galineau, L., Ragusa, T., Innis, R., Kassiou, M., Chalon, S., Dolle, F., Besnard, J., Guilloteau, D., Emond, P. Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands. Bioorganic & Medicinal Chemistry Letters. 2006; 16:1297-1300. [Abstract]
  • Cagnin, A., Kassiou, M., Meikle, S., Banati, R. In vivo evidence for microglial activation in neuro degenerative dementia. Acta Neurologica Scandinavica. 2006; 114:107-114. [Abstract]
  • Issa, F., Kassiou, M., Chan, H., McLeod, M. Synthesis and radiolabelling of ipratropium and tiotropium for use as PET ligands in the study of inhaled drug deposition. Australian Journal of Chemistry. 2006; 59:53-58. [Abstract]
  • James, M., Selleri, S., Kassiou, M. Development of ligands for the peripheral benzodiazepine receptor. Current medicinal chemistry. 2006; 13:1991-2001. [Abstract]