student profile: Mr Michael Moir


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Thesis work

Thesis title: The design and synthesis of novel selective cannabinoid receptor type 2 ligands

Supervisors: Michael KASSIOU , Louis RENDINA

Thesis abstract:

The endocannabinoid system is involved in a variety of physiological processes, including appetite, pain-sensation, mood and memory.1 The system comprises of two cell membrane receptors, CB1 and CB2, which are part of the G protein-coupled receptor superfamily.2 The CB2 receptor is expressed mainly in the cells of the immune system, such as astrocytes and microglia, and are responsible for immunomodulatory actions.1 Changes in cannabinoid receptor activity and endocannabinoid levels have been detected in almost all diseases that effect humans.1 It is thought that during cell or tissue damage, CB2 receptors are up-regulated. This activation plays an important protective role.2 The psychoactive effects associated with activation of cannabinoid type 1 (CB1) receptors, however, has plagued the progression of cannabinoid drugs. In light of this, much effort has been devoted to the development of selective CB2 receptor agonists, which would be devoid of such psychoactive side effects. The CB1 and CB2 receptors have high sequence homology, however minor variations in each receptor have been identified.3 A wide range of chemotypes have been reported to be potent and selective CB2 agonists. However, a comprehensive study that compares chemotypes and elucidates the structural features that drive potency and selectivity, has not been conducted. By comparing the structures of the most potent and selective ligands reported in the literature, certain common structural features have been identified. This study will elucidate the structural features that drive the potency and selectivity of high affinity CB2 ligands and identify novel ligands for future drug-lead development.

References

[1] Malfitano, A. M.; Basu, S.; Maresz, K.; Bifulco, M.; Dittel, B. N. Semin. Immunol. 2004 , 26 , 369-379.

[2] Pacher, P.; Mechoulam, R. Prog. Lipid Res. 2011, 50, 193-211.

[3] Munro, S.; Thomas, K. L.; Abu-Shaar, M. Nature 1993 , 365 (6441), 61–65.

Selected publications

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Journals

  • Kevin, R., Wood, K., Stuart, J., Mitchell, A., Moir, M., Banister, S., Kassiou, M., McGregor, I. (2017). Acute and residual effects in adolescent rats resulting rrom exposure to the novel synthetic cannabinoids AB-PINACA and AB-FUBINACA. Journal of Psychopharmacology, 31(6), 757-769. [More Information]
  • Moir, M., Chua, S., Reekie, T., Martin, A., Ittner, A., Ittner, L., Kassiou, M. (2017). Ring-opened aminothienopyridazines as novel tau aggregation inhibitors. MedChemComm (Medicinal Chemistry Communications), 8(6), 1275-1282. [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]
  • 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. [More Information]

2017

  • Kevin, R., Wood, K., Stuart, J., Mitchell, A., Moir, M., Banister, S., Kassiou, M., McGregor, I. (2017). Acute and residual effects in adolescent rats resulting rrom exposure to the novel synthetic cannabinoids AB-PINACA and AB-FUBINACA. Journal of Psychopharmacology, 31(6), 757-769. [More Information]
  • Moir, M., Chua, S., Reekie, T., Martin, A., Ittner, A., Ittner, L., Kassiou, M. (2017). Ring-opened aminothienopyridazines as novel tau aggregation inhibitors. MedChemComm (Medicinal Chemistry Communications), 8(6), 1275-1282. [More Information]

2015

  • 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]
  • 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. [More Information]

Note: This profile is for a student at the University of Sydney. Views presented here are not necessarily those of the University.