Identifying and characterising new drugs and drug-like molecules.
It is widely acknowledged that the current drug discovery pipeline by the major pharmaceutical companies is in crisis. As a consequence, novel approaches around drug discovery are increasingly developed by academia as well as the resulting small spin-off companies outside the restraints of rigid, dogmatic development regimens. We see this global trend as an opportunity and our centre works towards providing novel lead compounds for a variety of indications that are based on novel approaches, unique biological resources and out-of-the-box-thinking.
Humble coffee machine helps speed up research for new drugsRead more at Research to Reality
The drug-discovery group works on the identification and characterisation of new drugs and drug-like molecules with therapeutic activity. These molecules are either synthesized de novo, are isolated from natural sources, are modified versions of known molecules or are based on the re-profiling of known drug molecules. We have the capacity to take a molecule from its first synthesis or isolation, via cell-free and cell-based assays all the way to proof of concept testing in pre-clinical in vivo models of human disorders. At the same time, we also characterize molecular and cellular events triggered by exposure to drugs, which support mode of action studies and illuminate toxic liabilities of individual compounds. To facilitate drug screens for other users, we store a selection of drugs, drug-like compounds and novel molecules in a small library format that can be interrogated in a variety of different assays. In addition, our group constantly develops new assays that are optimized for use in multi-well plates to work towards medium-throughput screening. We aim to use cutting edge drug design to identify new pharmacological entities but more importantly our work is intended to provide patent protected drug candidates for the real world that can attract interest by the pharmaceutical industry.
Specialist Fields and Areas of Investigation
Based on the expertise of the individual team members, we aim to discover novel molecules or re-profile old molecules for a variety of indications incl. cancer, chronic pain, neurodegeneration, psychiatric conditions and mitochondrial disorders. Broad profiling of drugs and drug-like molecules allows not only the rational optimization of drug characteristics for a particular indication; it also provides an opportunity for serendipity findings that can give rise to useful drug derivatives for novel indications.
Major achievements or grants
- 2015: Fucoidan and cell cycle regulation, Marinova Pty
- 2015: Fucoidan and stem cell mobilization, Marinova Pty
- 2015: Fucoidan and gut health, Department of Industry and Science
- 2015: Non-anticoagulant molecules of heparin for the management of ulcerative colitis, Royal Hobart Hospital Research Foundation (RHHRF)
- Gueven N and Chhetri J (2015), 2014904633 - Minimizing Iatrogenic Effects of Clioquinol in the Treatment of Neurodegenerative Disease
Organic & Biomolecular Chemistry cover article:
Practical isolation of polygodial from Tasmannia lanceolata: a viable scaffold for synthesisRead the abstract at pubs.rcs.org
- Lean QY, Eri RD, Fitton JH, Patel RP, Gueven N. Fucoidan extracts ameliorate acute colitis. PLOS ONE (2015) 10(6): e0128453. doi:10.1371/journal.pone.0128453
- Shastri MD, Stewart N, Horne J, Zaidi STR, Sohal SS, Peterson GM, Korner H, Gueven N, Patel RP. Non-Anticoagulant Fractions of Enoxaparin Suppress Inflammatory Cytokine Release from Peripheral Blood Mononuclear Cells of Allergic Asthmatic Individuals. PLOS ONE (2015) 10(6): e0128803. doi:10.1371/journal.pone.0128803
- Shastri MD, Stewart N, Eapen M, Peterson GM, Zaidi STR, Gueven N, Sohal SS, Patel RP. Opposing Effects of Low Molecular Weight Heparins on the Release of Inflammatory Cytokines from Peripheral Blood Mononuclear Cells of Asthmatics. PLOS ONE (2015) 10(3): e0118798.
- Shastri MD, Stewart N, Horne J, Peterson GM, Gueven N, Sohal SS, Patel RP. In-Vitro Suppression of IL-6 and IL-8 Release from Human Pulmonary Epithelial Cells by Non-Anticoagulant Fraction of Enoxaparin. PLOS ONE (2015) 10(5): e0126763. doi:10.1371/journal.pone.0126763
- Yin X, Gueven N, Dietis N. Opioids in depression: not quite there yet. UK Journal of Pharmaceutical and Biosciences (2015) 3(1):12-17.
- Gueven N, Woolley K, Smith J. Border between natural product and drug: Comparison of the related benzoquinones idebenone and coenzyme Q10 Redox Biology(2015) 4:289-295.
- Paul A, Gueven N, Dietis N. Opioid receptor-dependent modulation of insulin-release in pancreatic beta-cells. UK J Pharmaceut Biosci (2014) 2(6):22-31
- Lean QY, Patel R, Stewart N, Sohal SS, Gueven N. Identification of pro-and anti-proliferative oligosaccharides of enoxaparin. Integr Biol (2014) 6(1):90-99
- Dietis N, McDonald J, Molinari S, Calo G, Guerrini R, Rowbotham JD, Lambert GD (2012) Pharmacological characterization of the bifunctional opioid ligand H-Dmt-Tic-Gly-NH-Bzl (UFP-505). Br J Anaesth.
Current PhD Students
- Jamuna Chhetri
- Bianca Deans
- Jeremy Just
- Hsien Lee
- Monila Nadikudi
- Alok Paul
- Tahani Saeedi
- Krystel Woolley
- Xin Yin
Name: Drug Discovery Group
Research group head:
Chemistry/Pharmacy building, Sandy Bay, 7005, Tasmania, Australia
Phone: 6226 1715