Elucidating the Mode of Action of Nicotinic Receptor Ligands. Changes in brain function can cause human diseases such as epilepsy, schizophrenia and Alzheimer's disease. To develop new medicines to treat these conditions we need to study how drugs act in the brain. This project will use new methods of chemistry to make drugs, which will then be tested for biological activity at important brain receptors. This will tell us which compounds are most effective as potential drugs and also exactly whe ....Elucidating the Mode of Action of Nicotinic Receptor Ligands. Changes in brain function can cause human diseases such as epilepsy, schizophrenia and Alzheimer's disease. To develop new medicines to treat these conditions we need to study how drugs act in the brain. This project will use new methods of chemistry to make drugs, which will then be tested for biological activity at important brain receptors. This will tell us which compounds are most effective as potential drugs and also exactly where they act in the brain. Read moreRead less
Elucidating the Mode of Action of Nicotinic Receptor Ligands. Changes in brain function can cause human diseases such as epilepsy, schizophrenia and Alzheimer's disease. To develop new medicines to treat these conditions we need to study how drugs act in the brain. This project will use new methods of chemistry to make drugs, which will then be tested for biological activity at important brain receptors. This will tell us which compounds are most effective as potential drugs and also exactly whe ....Elucidating the Mode of Action of Nicotinic Receptor Ligands. Changes in brain function can cause human diseases such as epilepsy, schizophrenia and Alzheimer's disease. To develop new medicines to treat these conditions we need to study how drugs act in the brain. This project will use new methods of chemistry to make drugs, which will then be tested for biological activity at important brain receptors. This will tell us which compounds are most effective as potential drugs and also exactly where they act in the brain. Read moreRead less
Development of Pyrrolopyrimidines as Inhibitors of ATP-Binding Proteins. This project seeks to generate analogues of natural products that have been found to be active against cancer cells and tropical parasites. The new materials produced by this project will aid in the study of biochemical processes involved in diseases such as cancer and lymphatic filariasis, thus leading the way to development of these compounds as potential treatments for such diseases.
New Methodology for the Stereoselective Construction of Oxygen Heterocycles and Rare Sugar Analogues. The overall goal of this research is to develop new synthetic methods, particularly ones that exhibit high levels of stereocontrol. Current research efforts are directed towards the stereoselective construction of oxygen heterocycles and rare sugar analogues both in their racemic and chiral forms utilising 1,2-dioxines containing tethered hydroxyl moieties as the key chemical precursors. It is e ....New Methodology for the Stereoselective Construction of Oxygen Heterocycles and Rare Sugar Analogues. The overall goal of this research is to develop new synthetic methods, particularly ones that exhibit high levels of stereocontrol. Current research efforts are directed towards the stereoselective construction of oxygen heterocycles and rare sugar analogues both in their racemic and chiral forms utilising 1,2-dioxines containing tethered hydroxyl moieties as the key chemical precursors. It is envisaged that these investigations will lead to the development of simple experimental protocols for the synthesis of new bioactive organics.Read moreRead less
Chemical Synthesis of Bioactive Metabolites and Analogues from Marine Sources and Myxobacteria. This project could result in the production of a new type of anticancer compound. The proposal will study the synthesis of novel natural product analogues that could possess superior biological activities to the natural compounds. In addition, new chemistry may be developed which could be utilised to synthesise a number of related molecules.
Total chemical synthesis of a redesigned enzyme, HIV-1 PR, containing an artificial tunable catalytic apparatus. The research project proposed represents a novel approach using total chemical synthesis to study the enzyme action of the HIV-1 PR, an aspartyl protease essential for the replication of AIDS virus. The redesign of the catalytic apparatus will allow us to investigate molecular aspects of its action. The synthetic polypeptide chain will be folded and characterised for the correct folde ....Total chemical synthesis of a redesigned enzyme, HIV-1 PR, containing an artificial tunable catalytic apparatus. The research project proposed represents a novel approach using total chemical synthesis to study the enzyme action of the HIV-1 PR, an aspartyl protease essential for the replication of AIDS virus. The redesign of the catalytic apparatus will allow us to investigate molecular aspects of its action. The synthetic polypeptide chain will be folded and characterised for the correct folded structure by NMR, and assayed for enzymatic activity. It can be expected that significant new insights into the molecular basis of the properties of the HIV-1 PR will be obtained. This will be an important contribution to biomedical research.Read moreRead less
Synthesis of Myxobacteria Metabolites and Analogues. The proposal will study the synthesis of novel natural product analogues that could possess superior biological activities to the natural compounds. In addition, new chemistry may be developed which could be utilised to synthesise a number of bioactive molecules from myxobacteria.
CHARACTERISATION OF NOVEL BIOACTIVES FROM AUSTRALIAN HONEY WITH THERAPEUTIC POTENTIAL. Honey from specific Australian flowering plants has been identified that contain significant therapeutic properties in wound healing and other treatments. The research project proposed will identify and fully characterise the bioactive components of selected Australian honey (Medihoney) with antibiotic and growth promoting activites. These aims will be supported by high resolution mass spectrometry interfaced ....CHARACTERISATION OF NOVEL BIOACTIVES FROM AUSTRALIAN HONEY WITH THERAPEUTIC POTENTIAL. Honey from specific Australian flowering plants has been identified that contain significant therapeutic properties in wound healing and other treatments. The research project proposed will identify and fully characterise the bioactive components of selected Australian honey (Medihoney) with antibiotic and growth promoting activites. These aims will be supported by high resolution mass spectrometry interfaced with HPLC and or affinity chip surfaces, 750 MHz NMR analysis and a range of relevant bioassays on specific organisms and cell lines. These outcomes will not only enhance the value of current honey-based products but have the potential to identify new therapeutic lead molecules.Read moreRead less
New Chemistry for the Total Synthesis of Pyrone Containing Marine Natural Products. The project will produce a range of compounds in the laboratory that have been identified from marine organisms. These compounds, which have potential as new medicines, are produced in minute quantities by the organisms, and synthesis in the laboratory is a way to produce significant quantities for biological evaluation. The new methods developed for the preparation of complex polypropionates compounds, can be a ....New Chemistry for the Total Synthesis of Pyrone Containing Marine Natural Products. The project will produce a range of compounds in the laboratory that have been identified from marine organisms. These compounds, which have potential as new medicines, are produced in minute quantities by the organisms, and synthesis in the laboratory is a way to produce significant quantities for biological evaluation. The new methods developed for the preparation of complex polypropionates compounds, can be applied to the preparation of known medicinally active compounds. The grant will allow a PhD student and post doctoral worker to receive first-rate training in organic and medicinal chemistry, which are areas in great demand to support the increasing number of start-up biotechnology and niche pharmaceutical companies.Read moreRead less
Microprobe and Nanoprobe Studies on Intracellular Disease Processes and Their Treatment. Breakthrough microprobe and nanoprobe technologies, involving X-ray, visible and infrared light can focus into different components of mammalian cells in order to interrogate the biochemistry that is occurring therein. Each of the different wavelengths of light provides complementary biochemical information that enables a deeper understanding of changes in cells that occur as a function of drug treatments an ....Microprobe and Nanoprobe Studies on Intracellular Disease Processes and Their Treatment. Breakthrough microprobe and nanoprobe technologies, involving X-ray, visible and infrared light can focus into different components of mammalian cells in order to interrogate the biochemistry that is occurring therein. Each of the different wavelengths of light provides complementary biochemical information that enables a deeper understanding of changes in cells that occur as a function of drug treatments and disease processes. This will provide unprecedented information as to where drugs go and how they are transformed inside cells that, in turn, may revolutionalise the way in which new drugs are designed that have higher specificity and fewer side effects.Read moreRead less