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
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
High Pressure and Fluorous Approaches to Fostriecin Libraries: New Therapeutic Opportunities. The natural product, Fostriecin, displays considerable broad-spectrum anti-cancer activity, acting via a novel mechanism. However, this activity is tempered by its considerable instability, being too unstable to be used as a therapeutic agent. Using state-of-the-art approaches we will, rapidly generate libraries of more stable and biologically active fostriecin analogues and examine their potential to b ....High Pressure and Fluorous Approaches to Fostriecin Libraries: New Therapeutic Opportunities. The natural product, Fostriecin, displays considerable broad-spectrum anti-cancer activity, acting via a novel mechanism. However, this activity is tempered by its considerable instability, being too unstable to be used as a therapeutic agent. Using state-of-the-art approaches we will, rapidly generate libraries of more stable and biologically active fostriecin analogues and examine their potential to be used anti-cancer agents. This project represents an opportunity for Australia to take a significant, innovative lead in the development of hitherto unforseen therapeutic agents.Read moreRead less
The Design of New Integrase Inhibitors Targeting HIV-1. There is still no cure in sight for the worldwide HIV pandemic and the worsening viral resistance problem creates a need to find new and novel compounds for therapeutic use. This project aims to design and synthesize new anti-HIV drugs by targeting two separate enzymes within the HIV life-cycle. This 'dual-action' approach of designing a single molecular scaffold to target separate enzymes would enable a synergistic effect while minimizing ....The Design of New Integrase Inhibitors Targeting HIV-1. There is still no cure in sight for the worldwide HIV pandemic and the worsening viral resistance problem creates a need to find new and novel compounds for therapeutic use. This project aims to design and synthesize new anti-HIV drugs by targeting two separate enzymes within the HIV life-cycle. This 'dual-action' approach of designing a single molecular scaffold to target separate enzymes would enable a synergistic effect while minimizing development costs. The expected outcomes from this medicinal chemistry project include the discovery of new compounds with the potential for further development as therapeutic agents against HIV.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE160100218
Funder
Australian Research Council
Funding Amount
$840,000.00
Summary
A Nuclear Magnetic Resonance Facility for Modern Molecular Analysis. A nuclear magnetic resonance facility for modern molecular analysis:
This project aims to network a new 500 MHz nuclear magnetic resonance (NMR) spectrometer and new consoles for existing instruments with an automated sample changer for a 600 MHz NMR spectrometer. This designed to increase the capacity of Queensland-based researchers to undertake state-of-the-art studies in chemistry, drug design, and materials science. The ne ....A Nuclear Magnetic Resonance Facility for Modern Molecular Analysis. A nuclear magnetic resonance facility for modern molecular analysis:
This project aims to network a new 500 MHz nuclear magnetic resonance (NMR) spectrometer and new consoles for existing instruments with an automated sample changer for a 600 MHz NMR spectrometer. This designed to increase the capacity of Queensland-based researchers to undertake state-of-the-art studies in chemistry, drug design, and materials science. The new knowledge from these studies may lead to the development of new drugs, new crop protection agents and new photovoltaic materials. Read moreRead less
The Design and Development of the Next Generation Anti-HIV Drugs. This medicinal chemistry project will develop new computer-aided modelling techniques for drug design and development and will then apply them to the design of new therapeutics for the treatment of HIV-1/AIDS. Once developed, these new techniques can also be applied to other disease targets including various cancers, where specific proteins have been identified as causative. This research will also contribute to the education of y ....The Design and Development of the Next Generation Anti-HIV Drugs. This medicinal chemistry project will develop new computer-aided modelling techniques for drug design and development and will then apply them to the design of new therapeutics for the treatment of HIV-1/AIDS. Once developed, these new techniques can also be applied to other disease targets including various cancers, where specific proteins have been identified as causative. This research will also contribute to the education of young scientists, training them in cutting-edge research skills.Read moreRead less
Chemical Insights to Peptide Helix-Sheet-Nanofibre Equilibria. We live in an ageing community that is experiencing exponential growth in neurological diseases that require full time carers and place significant burdens on our health system. Many such diseases are caused by (apparently) abnormal folding of proteins that aggregate into insoluble materials. The chemistry behind these processes is not sufficiently well understood to know precisely why the diseases are caused and how they might be tr ....Chemical Insights to Peptide Helix-Sheet-Nanofibre Equilibria. We live in an ageing community that is experiencing exponential growth in neurological diseases that require full time carers and place significant burdens on our health system. Many such diseases are caused by (apparently) abnormal folding of proteins that aggregate into insoluble materials. The chemistry behind these processes is not sufficiently well understood to know precisely why the diseases are caused and how they might be treated. This project will use new strategies to control peptide folding, provide important new information relevant to understanding such processes/diseases, and teach us how to engineer important new biomaterials that can advance nanotechnology. Read moreRead less
Synthesis of novel biologically active isoflavones. Cancer and heart disease are two of the main diseases that affect our society indiscriminately and put enormous drains on our health-care resources. Therefore, discovery and development of drugs that can treat these diseases are of utmost importance. Given the established success of Novogen Ltd in the development of drugs through to human clinical trials, novel isoflavones proposed in this study may lead to the discovery of new drug leads or t ....Synthesis of novel biologically active isoflavones. Cancer and heart disease are two of the main diseases that affect our society indiscriminately and put enormous drains on our health-care resources. Therefore, discovery and development of drugs that can treat these diseases are of utmost importance. Given the established success of Novogen Ltd in the development of drugs through to human clinical trials, novel isoflavones proposed in this study may lead to the discovery of new drug leads or therapeutic agents. The project has the potential to deliver enormous commercial benefits to Australian industry and social benefits to our ageing population through provision of new, locally produced therapeutics.Read moreRead less
Disruption of Sex Pheromone Biosynthesis: A Novel Control Method for Pestiferous Fruit Flies by. Fruit flies from the genus Bactrocera are economically important worldwide. B. tryoni, (Queensland fruit fly) is the most damaging horticultural pest in Australia and B. oleae (olive fly) is a major European pest. These flies use chemicals of similar but distinct structure for communication and particularly for finding mates. This research will examine the pathways and enzymes these flies use to sy ....Disruption of Sex Pheromone Biosynthesis: A Novel Control Method for Pestiferous Fruit Flies by. Fruit flies from the genus Bactrocera are economically important worldwide. B. tryoni, (Queensland fruit fly) is the most damaging horticultural pest in Australia and B. oleae (olive fly) is a major European pest. These flies use chemicals of similar but distinct structure for communication and particularly for finding mates. This research will examine the pathways and enzymes these flies use to synthesise sex pheromones. We propose that understanding the chemical and biochemical steps employed by the flies will allow us to design inhibitors to prevent pheromone production and thus provide a novel, species specific method for controlling fruit flies.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE130100168
Funder
Australian Research Council
Funding Amount
$1,235,000.00
Summary
Adelaide Nuclear Magnetic Resonance (NMR). Nuclear Magnetic Resonance (NMR) spectroscopy is a fundamental underpinning technology for the advancement of the many sciences which require determination of the structure of molecules. This project will significantly enhance and broaden NMR capabilities in South Australia and advance world-class research in chemistry, materials science, nanotechnology and biochemistry.