Improving the function of GABA-A receptors is a key property of several classes of clinically important drugs including benzodiazepines and many anticonvulsants. However, the binding sites and molecular mechanisms of these drugs remain poorly understood. Using compounds similar to those in green tea, we will determine the molecular mechanism of these drugs. This understanding will lead to the development of better drugs for treatment of anxiety, depression, epilepsy, insomnia & schizophrenia.
Escaping Bio-Assay Guided Isolation: Nature's Tools for Chemical Biology. The project aims to transform the approach to identify novel biologically active compounds that occur in nature. For decades, natural product chemistry has centred on bio-assay guided isolation, but it has become increasingly difficult to isolate novel compounds. While de-replication strategies detect the presence of known compounds using databases, more impact would be achieved by directly detecting novel compounds. Nucle ....Escaping Bio-Assay Guided Isolation: Nature's Tools for Chemical Biology. The project aims to transform the approach to identify novel biologically active compounds that occur in nature. For decades, natural product chemistry has centred on bio-assay guided isolation, but it has become increasingly difficult to isolate novel compounds. While de-replication strategies detect the presence of known compounds using databases, more impact would be achieved by directly detecting novel compounds. Nuclear magnetic resonance (NMR) spectroscopy detects every molecule that has a proton and is quantitative. This project plans to develop a NMR technique to escape bio-assay guided isolation by analysing a fraction library. Biotechnology innovation is dependent on novel compounds to provide new products. Replacing ‘grind and find’ with a technique that never lies would be transformational.Read moreRead less
The Pharmacology And Toxicity Of Synthetic Cannabinoids
Funder
National Health and Medical Research Council
Funding Amount
$744,808.00
Summary
Synthetic cannabinoids (SCs) have been recently linked to many deaths and hospitalizations but there is limited data available that addresses these issues. We have identified SCs which display unprecedented cannabinoid receptor function, unusual selectivity, and SCs with high activity at cannabinoid receptors. This project will define the role of CB receptors in the actions of SCs, and provide an evidence-based rationale for treating SC overdoses.
The Inhibition Of Biotin Protein Ligase As A New Source Of Antibiotics
Funder
National Health and Medical Research Council
Funding Amount
$750,167.00
Summary
We have become so accustomed to treating bacterial infections with antibiotics that it is hard to imagine life without them. However, the emergence of drug-resistance is creating a global health care crisis. Recently, there has not been enough attention paid to replacing old antibiotics with new products to combat drug resistance. Our team is addressing this challenge. We have discovered a new class of antibiotic that is unlike any other drug in clinical use.
Optimisation Of A Potent And Fast Acting Antimalarial Class That Is Orally Efficacious In Vivo
Funder
National Health and Medical Research Council
Funding Amount
$683,916.00
Summary
Malaria is a devastating disease that results in 600 000 deaths annually. Current therapeutics used to combat malaria have a limited duration of use in the clinic due to the onset of resistance. We have identified a highly active antimalarial series that we propose to further develop to meet the prerequisites required for partnership with the Medicines for Malaria Venture (MMV) for progression into the clinic.
Towards an influenza virus glycan interaction map (Glycointeractome). This project will use nuclear magnetic resonance (NMR) spectroscopy to map carbohydrate interaction used by the virus to cause infection and spread. This information will provide new direction in anti-influenza drug discovery.
Oxytocin Receptor Agonists For Treatment Of Social Anxiety
Funder
National Health and Medical Research Council
Funding Amount
$459,844.00
Summary
At any one time, about 3% of the population suffers from crippling social anxiety disorder, characterized by excessive fear of exposure to situations that involve potential scrutiny by others. Current medications for treating social anxiety are of limited use. This project will develop new drug like molecules that could provide breakthroughs in the effective treatment of social anxiety.
Evaluation Of Novel Pyrrolo/Iminoquinone Antimalarial Compounds
Funder
National Health and Medical Research Council
Funding Amount
$614,250.00
Summary
The development of new antimalarial drugs is an unmet global health priority. In this project we will investigate novel compounds that have been found to display promising in vitro antimalarial activity. We will modify these compounds to make them more drug-like, and assess their efficacy in vivo using malaria animal models. These studies have the potential to identify compounds that may result in a new therapy for malaria, the worlds' most significant tropical infectious disease.
Novel Therapeutics For The Remediation Of Social Deficits In Psychiatric Illness
Funder
National Health and Medical Research Council
Funding Amount
$597,719.00
Summary
Many psychiatric disorders feature a disruption of social behaviour as a central feature of the illness. Examples includes autism, social anxiety disorder, schizophrenia and the addictions. Existing therapies for these disorders rarely improve these core social deficits. We have recently discovered a new molecule (called SOC-1) that stimulates social behaviour in animals. The current project will study how SOC-1 produces these effects and will develop it as a medication for human use.
DYRK1A As A Novel Target For Glioblastoma Therapies
Funder
National Health and Medical Research Council
Funding Amount
$620,294.00
Summary
Glioblastoma is a form of brain cancer that is currently incurable. We have discovered that switching-off an enzyme called DYRK1A (using ‘DYRK1A inhibitors’) kills glioblastoma cells. This therapeutic advantage is even greater when combined with drugs approved for other cancers. This project will develop new DYRK1A inhibitors and examine a novel combination treatment for glioblastoma patients. This could initiate a novel therapy that could significantly extend patients’ lives.