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
Applying the CCK framework to angiogenic-based therapeutics. The aim of this project is to graft peptides involved in angiogenesis-related disorders onto a mini-protein framework. The cyclic cystine knot (CCK) framework is a plant based protein framework that has unique structural properties that make it exceptionally stable. The significance of this project is that the framework has the potential to overcome the limitations that are generally associated with peptide-based therapeutics, includin ....Applying the CCK framework to angiogenic-based therapeutics. The aim of this project is to graft peptides involved in angiogenesis-related disorders onto a mini-protein framework. The cyclic cystine knot (CCK) framework is a plant based protein framework that has unique structural properties that make it exceptionally stable. The significance of this project is that the framework has the potential to overcome the limitations that are generally associated with peptide-based therapeutics, including poor stability and bioavailability. Vastly improved therapeutic leads may be produced from this approach.Read moreRead less
What is in therapeutically prescribed herbal medicines? Phytochemical characterisation of steroidal saponins from two popular nutraceuticals, False Unicorn and Tribulus terrestris. Plants containing steroidal saponins have long been used as therapeutic products, but their active constituents remain poorly characterized. This project aims to identify and structurally characterize steroidal saponins from False Unicorn and Tribulus terrestris, two popular nutraceuticals which are currently marketed ....What is in therapeutically prescribed herbal medicines? Phytochemical characterisation of steroidal saponins from two popular nutraceuticals, False Unicorn and Tribulus terrestris. Plants containing steroidal saponins have long been used as therapeutic products, but their active constituents remain poorly characterized. This project aims to identify and structurally characterize steroidal saponins from False Unicorn and Tribulus terrestris, two popular nutraceuticals which are currently marketed in Australia. Existing knowledge of these saponin constituents is surprisingly incomplete and inaccurate. Full structural elucidation will enable the development of 'standardised' herbal saponin profiles for better control of product quality and will allow alternatives for the herbs to be chosen, which cannot be undertaken until this composition is known. A phytochemical survey of Australian Tribulus terrestris will determine whether this native sub-species is suitable for commercial harvest.Read moreRead less
Australian Marine Biodiversity As A Source Of New Drugs To Control Neurodegenerative Disease. With the aging of Australia's population the impact of neurodegenerative diseases such as Alzheimer's and Parkinson's is rapidly on the rise. There is an urgent need to develop new and better drugs to treat the symptoms and underlying cause of these debilitating diseases. Historically, the majority of the world's pharmaceuticals have been drawn from biodiversity (ie plants, microbes and animals). As one ....Australian Marine Biodiversity As A Source Of New Drugs To Control Neurodegenerative Disease. With the aging of Australia's population the impact of neurodegenerative diseases such as Alzheimer's and Parkinson's is rapidly on the rise. There is an urgent need to develop new and better drugs to treat the symptoms and underlying cause of these debilitating diseases. Historically, the majority of the world's pharmaceuticals have been drawn from biodiversity (ie plants, microbes and animals). As one of the few megabiodiverse nations, Australia is ideally positioned to accelerate and focus the search for drugs from nature. This project will explore an exceptionally promising pool of Australian biodiversity, its marine ecosystems, as a source of inspiration for the development of new drugs to treat neurodegenerative diseases. Read moreRead less
Synthesis and evaluation of anti-microbial porphyrin adducts for the targeted inhibition of Porphyromonas gingivalis. At present the effectiveness of therapy for inflammatory disease of the gum tissue (periodontitis) is limited by the lack of a selective anti-microbial agent. The investigators have discovered a novel mechanism of binding of the blood product porphyrin by a unique receptor of a key pathogen implicated in this disease. By exploiting this knowledge a modified porphyrin linked to an ....Synthesis and evaluation of anti-microbial porphyrin adducts for the targeted inhibition of Porphyromonas gingivalis. At present the effectiveness of therapy for inflammatory disease of the gum tissue (periodontitis) is limited by the lack of a selective anti-microbial agent. The investigators have discovered a novel mechanism of binding of the blood product porphyrin by a unique receptor of a key pathogen implicated in this disease. By exploiting this knowledge a modified porphyrin linked to an antibiotic was shown to have a selective effect on the target organism. Refinement of this complex has the potential to provide a clinically useful, selective agent.Read moreRead less
Development of a Diversity-Oriented Synthesis Platform. Genomic, proteomic and other studies of the molecular basis of disease are providing a constant stream of biomolecular targets for drug discovery. Identifying suitable drugs candidates to affect these targets centres around procuring a suitable library of compounds for screening. This application addresses some of the key issues related to the development of appropriate compound libraries for such screening programs.
The development of a rapid diagnostic test for heparanase activity. Heparanase is an enzyme that has been implicated in a number of disease states such as cancer, arthritis, multiple sclerosis and other inflammatory diseases. Characterisation of this enzyme has been slow, due in part to the lack of a reliable direct activity assay. Using a multi-disciplinary approach, this project seeks to establish a rapid assay that will provide easy determination of heparanase activity. Furthermore, this a ....The development of a rapid diagnostic test for heparanase activity. Heparanase is an enzyme that has been implicated in a number of disease states such as cancer, arthritis, multiple sclerosis and other inflammatory diseases. Characterisation of this enzyme has been slow, due in part to the lack of a reliable direct activity assay. Using a multi-disciplinary approach, this project seeks to establish a rapid assay that will provide easy determination of heparanase activity. Furthermore, this assay could provide a useful diagnostic tool in a clinical environment that would allow for the rapid assessment of these diseases, their progression and indeed response to therapy.Read moreRead less
The Synthesis and Pharmacological Evaluation of Novel Bivalent Dopamine D2 and Adenosine A2A Ligands for the Treatment of Parkinson's Disease. This program will significantly contribute to the training of highly qualified personnel in the area of organic and medicinal chemistry where there is currently a national shortage. Other benefits are the capacity to advance this critical research in PD and potentially provide substantial national competitive advantages and growth opportunities in the glo ....The Synthesis and Pharmacological Evaluation of Novel Bivalent Dopamine D2 and Adenosine A2A Ligands for the Treatment of Parkinson's Disease. This program will significantly contribute to the training of highly qualified personnel in the area of organic and medicinal chemistry where there is currently a national shortage. Other benefits are the capacity to advance this critical research in PD and potentially provide substantial national competitive advantages and growth opportunities in the global anti-Parkinsonian therapeutics market.Read moreRead less
Applications of the Polonovski Reaction in the Synthesis of Bioactive Opiates. This program will contribute to the training of highly qualified personnel in the area of organic and medicinal chemistry. It will also address the development of improved processes for the large scale preparation of semi-synthetic pharmaceutical opiates in support of one of Australia's important export industries. Furthermore, a greater understanding of the structure-activity relationships of noscapine will make a ....Applications of the Polonovski Reaction in the Synthesis of Bioactive Opiates. This program will contribute to the training of highly qualified personnel in the area of organic and medicinal chemistry. It will also address the development of improved processes for the large scale preparation of semi-synthetic pharmaceutical opiates in support of one of Australia's important export industries. Furthermore, a greater understanding of the structure-activity relationships of noscapine will make a contribution to the overall search for improved anti-cancer agents.Read moreRead less
Novel strategies in the design and development of antivirals against dengue virus. Globally, there are 50-100 million cases of dengue fever, with 500,000 cases of the more severe dengue haemorrhagic fever, each year. Australia has between 100 and 900 cases of dengue infection annually, often from travellers, but disease outbreaks occur in northern Australia. Effective anti-viral treatment will reduce disease burden. The project contributes to an evidence-based drug design program in collaboratio ....Novel strategies in the design and development of antivirals against dengue virus. Globally, there are 50-100 million cases of dengue fever, with 500,000 cases of the more severe dengue haemorrhagic fever, each year. Australia has between 100 and 900 cases of dengue infection annually, often from travellers, but disease outbreaks occur in northern Australia. Effective anti-viral treatment will reduce disease burden. The project contributes to an evidence-based drug design program in collaboration with Australia's leading biotechnology industries. As a biotechnology industry project developing treatments for an emerging disease, it contributes to the national research priorities of Frontier technologies for building and transforming Australian industries, Promoting and maintaining good health and Safeguarding Australia.Read moreRead less