Kassiou, Michael - University of Sydney

研究领域

Medicinal Chemistry and Drug Discovery Structure-activity relationships of CNS bioactive molecules Rationale CNS drug design and evaluation Heterocyclic Chemistry Research in my group is interdisciplinary and built around the key themes of medicinal chemistry and drug discovery. Our research group utilises modern organic chemistry techniques to rationally design and synthesise novel compounds for a range of CNS targets which are associated with neuropathologie ssuch as Parkinson’s disease, schizophrenia, anxiety and depression. In this domain understanding drug-protein and drug-binding site interactions is a key component which allows us to obtain structure-activity relationships of bioactive CNS molecules. In addition by using molecular imaging techniques within these fields we are able to better understand the living brain in normal and diseased states through in vivo studies.

近期论文

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Thomas, C., Vercouillie, J., Domene, A., Tauber, C., Kassiou, M., Guilloteau, D., Destrieux, C., Serriere, S., Chalon, S. (2016). Detection of neuroinflammation in a rat model of subarachnoid hemorrhage using [18F]DPA-714 PET imaging. Molecular Imaging, 15, 1-8. [More Information] Przybyla, M., Stevens, C., Hoven, J., Harasta, A., Bi, M., Ittner, A., Hummel, A., Hodges, J., Piguet, O., Karl, T., Kassiou, M., et al (2016). Disinhibition-like behavior in a P301S mutant tau transgenic mouse model of frontotemporal dementia. Neuroscience Letters, 631, 24-29. [More Information] Jorgensen, W., Gulliver, D., Werry, E., Reekie, T., Connor, M., Kassiou, M. (2016). Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors. European Journal of Medicinal Chemistry, 108, 730-740. [More Information] Coughlin, J., Wang, Y., Ambinder, E., Ward, R., Minn, I., Vranesic, M., Kim, P., Ford, C., Higgs, C., Hayes, L., Kassiou, M., et al (2016). In vivo markers of inflammatory response in recent-onset schizophrenia: a combined study using [11C]DPA-713 PET and analysis of CSF and plasma. Translational Psychiatry, 6, 1-8. [More Information] Dupont, A., Guilloteau, D., Kassiou, M., Ribeiro, M., Vercouillie, J., Katsifis, A., Arlicot, N. (2016). Radiopharmaceuticals for PET imaging of neuroinflammation. Medecine Nucleaire, 40(1), 72-81. [More Information] Longworth, M., Banister, S., Mack, J., Glass, M., Connor, M., Kassiou, M. (2016). The 2-alkyl-2H-indazole regioisomers of synthetic cannabinoids AB-CHMINACA, AB-FUBINACA, AB-PINACA, and 5F-AB-PINACA are possible manufacturing impurities with cannabimimetic activities. Forensic Toxicology, 34(2), 286-303. [More Information] Katte, T., Reekie, T., Jorgensen, W., Kassiou, M. (2016). The formation of seven-membered heterocycles under mild Pictet-Spengler conditions: A route to pyrazolo[3,4]benzodiazepines. The Journal of Organic Chemistry, 81(11), 4883-4889. [More Information] Beinat, C., Banister, S., Herrera, M., Kassiou, M. (2016). The recent development of α7 nicotinic acetylcholine receptor (nAChR) ligands as therapeutic candidates for the treatment of central nervous system (CNS) diseases. Current Pharmaceutical Design, 22(14), 2134-2151. [More Information] Serriere, S., Tauber, C., Vercouillie, J., Mothes, C., Pruckner, C., Guilloteau, D., Kassiou, M., Domene, A., Garreau, L., Page, G., et al (2015). Amyloid load and translocator protein 18 kDa in APPswePS1-dE9 mice: a longitudinal study. Neurobiology of Aging, 36(4), 1639-1652. [More Information] Wilkinson, S., Banister, S., Kassiou, M. (2015). Bioisosteric fluorine in the clandestine design of synthetic cannabinoids. Australian Journal of Chemistry, 68(1), 4-8. [More Information] Austin, C., Moir, M., Kahlert, J., Smith, J., Jamie, J., Kassiou, M., Rendina, L. (2015). Carborane-containing hydroxyamidine scaffolds as novel inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1). Australian Journal of Chemistry, 68(12), 1866-1870. [More Information] Abbassi, R., Johns, T., Kassiou, M., Munoz, L. (2015). DYRK1A in neurodegeneration and cancer: Molecular basis and clinical implications. Pharmacology & Therapeutics, 151, 87-98. [More Information] Banister, S., Stuart, J., Kevin, R., Edington, A., Longworth, M., Wilkinson, S., Beinat, C., Buchanan, A., Hibbs, D., Glass, M., McGregor, I., Kassiou, M., et al (2015). Effects of Bioisosteric Fluorine in Synthetic Cannabinoid Designer Drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135. ACS Chemical Neuroscience, 6(8), 1445-1458. [More Information] Banister, S., Beinat, C., Wilkinson, S., Shen, B., Bartoli, C., Selleri, S., Da Pozzo, E., Martini, C., Chin, F., Kassiou, M. (2015). Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO). European Journal of Medicinal Chemistry, 93, 392-400. [More Information] Santiago-Ribeiro, M., Vercouillie, J., Cottier, J., Debiais, S., Bonnaud, I., Annan, M., Maia, S., Kassiou, M., Arlicot, N., Guilloteau, D. (2015). Evaluation en TEP de l'activation microgliale apres un accident vasculaire cerebral. Medecine Nucleaire, 39(3), 210-210. [More Information] Narlawar, R., Werry, E., Scarf, A., Hanani, R., Chua, S., King, V., Barron, M., Martins, R., Ittner, L., Rendina, L., Kassiou, M. (2015). First demonstration of positive allosteric-like modulation at the human wild type translocator protein (TSPO). Journal of Medicinal Chemistry, 58(21), 8743-8749. [More Information] Lee, D., Yue, X., Ibrahim, W., Lentz, M., Peterson, K., Jagoda, E., Kassiou, M., Maric, D., Reid, W., Hammoud, D. (2015). Lack of neuroinflammation in the HIV-1 transgenic rat: an [18F]-DPA714 PET imaging study. Journal of Neuroinflammation, 12(171), 1-11. [More Information] Coughlin, J., Wang, Y., Munro, C., Ma, S., Yue, C., Chen, S., Airan, R., Kim, P., Adams, A., Garcia, C., Kassiou, M., et al (2015). Neuroinflammation and brain atrophy in former NFL players: An in vivo multimodal imaging pilot study. Neurobiology of Disease, 74, 58-65. [More Information] Munoz, L., Kavanagh, M., Phoa, A., Heng, B., Dzamko, N., Chen, E., Doddareddy, M., Guillemin, G., Kassiou, M. (2015). Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation. European Journal of Medicinal Chemistry, 95, 29-34. [More Information] Banister, S., Moir, M., Stuart, J., Kevin, R., Wood, K., Longworth, M., Wilkinson, S., Beinat, C., Buchanan, A., Glass, M., McGregor, I., Kassiou, M., et al (2015). Pharmacology of indole and indazole synthetic cannabinoid designer drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA, ADB-PINACA, 5F-AB-PINACA, 5F-ADB-PINACA, ADBICA, and 5F-ADBICA. ACS Chemical Neuroscience, 6(9), 1546-1559. 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