Linkage Infrastructure, Equipment And Facilities - Grant ID: LE100100142
Funder
Australian Research Council
Funding Amount
$500,000.00
Summary
An integrated liquid chromatography mass spectrometry nuclear magnetic resonance (LC-MS-NMR) facility for applications in proteomics and organic chemistry. This application completes the requested liquid chromatography mass spectrometry nuclear magnetic resonance (LCMS-NMR) facility and will allow the training of over 150 researchers, significantly enhancing their research productivity and translation of outcomes in areas of national importance. New breakthroughs in drug development, smart mate ....An integrated liquid chromatography mass spectrometry nuclear magnetic resonance (LC-MS-NMR) facility for applications in proteomics and organic chemistry. This application completes the requested liquid chromatography mass spectrometry nuclear magnetic resonance (LCMS-NMR) facility and will allow the training of over 150 researchers, significantly enhancing their research productivity and translation of outcomes in areas of national importance. New breakthroughs in drug development, smart materials, organic electronic materials and biomedical research require routine access to cutting edge technology. The LCMS-NMR augments the capabilities of our research teams at the forefront of these efforts. These include understanding the impact of the environment on plant and animal development, pest animal control, development of new biotechnology tools, new drugs and new methods for the detection of narcotics and explosives.Read moreRead less
Engineered extrasynaptic GABAA receptors: Towards novel analgesics. Engineered extrasynaptic GABAA receptors: Towards novel analgesics. This project intends to alleviate neuropathic pain by developing drugs and good tool molecules targeting GABA-A receptors. About 20% of Australian adults suffer from neuropathic pain. Delta-containing GABA-A receptors represent attractive and novel targets for developing non-opioid analgesics. However, no drugs or good tool molecules target these receptors. This ....Engineered extrasynaptic GABAA receptors: Towards novel analgesics. Engineered extrasynaptic GABAA receptors: Towards novel analgesics. This project intends to alleviate neuropathic pain by developing drugs and good tool molecules targeting GABA-A receptors. About 20% of Australian adults suffer from neuropathic pain. Delta-containing GABA-A receptors represent attractive and novel targets for developing non-opioid analgesics. However, no drugs or good tool molecules target these receptors. This project intends to develop the needed enabling technologies, including screening assays, tool molecules and radioligands; and perform brain slice electrophysiology to confirm activity in neuronal cells. This project is expected to benefit the research community and future rational drug-discovery endeavours for drugs that modulate delta-containing receptors.Read moreRead less
Discovery and development of novel insulin sensitising compounds for the treatment of Type 2 diabetes. Diabetes is one of the major health problems facing Australia today, and current treatments are proving inadequate to combat this disease. We previously discovered a new drug with potential for development for the treatment of diabetes. In this project, we will identify how this drug works to combat diabetes in cell and animal models, and use novel chemistry approaches to modify the drug to imp ....Discovery and development of novel insulin sensitising compounds for the treatment of Type 2 diabetes. Diabetes is one of the major health problems facing Australia today, and current treatments are proving inadequate to combat this disease. We previously discovered a new drug with potential for development for the treatment of diabetes. In this project, we will identify how this drug works to combat diabetes in cell and animal models, and use novel chemistry approaches to modify the drug to improve its properties and reduce potential side-effects. The outcomes of this project will be understanding of a new biological process that contributes to the development of diabetes, and the discovery and characterisation of new chemical compounds that could be developed as drugs to treat diabetes.Read moreRead less
Bioactive Peptides as Pharmacological Tools and Novel Drug Leads. Bioactive peptides are produced by all organisms and play numerous critical physiological roles, including in cellular communication, host defence and capture of prey. Peptides have huge potential as tools for studying roles of signalling pathways and as novel drugs due to their high affinity and selectivity for various therapeutically relevant targets. However their use has been limited by poor in vivo stability. This project is ....Bioactive Peptides as Pharmacological Tools and Novel Drug Leads. Bioactive peptides are produced by all organisms and play numerous critical physiological roles, including in cellular communication, host defence and capture of prey. Peptides have huge potential as tools for studying roles of signalling pathways and as novel drugs due to their high affinity and selectivity for various therapeutically relevant targets. However their use has been limited by poor in vivo stability. This project is focused on studying structural features of a range of peptides and their contributions to both activity and to resistance against degradation, with the aim to develop stabilised bioactive peptide sequences for in vivo applications, allowing the full potential of peptides as drugs to be realised.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE160100047
Funder
Australian Research Council
Funding Amount
$380,000.00
Summary
Distributed facility for fragment based drug discovery. Distributed facility for fragment based drug discovery:
The facility aims to provide researchers with the ability to generate small molecules that modulate therapeutically and biologically important protein targets. Fragment-based drug design (FBDD) provides a rational approach to generate such biologically active compounds. The facility is designed to allow researchers throughout Australia to access the necessary infrastructure to underta ....Distributed facility for fragment based drug discovery. Distributed facility for fragment based drug discovery:
The facility aims to provide researchers with the ability to generate small molecules that modulate therapeutically and biologically important protein targets. Fragment-based drug design (FBDD) provides a rational approach to generate such biologically active compounds. The facility is designed to allow researchers throughout Australia to access the necessary infrastructure to undertake FBDD projects against a range of biologically important targets. The facility aims to enable access to high-throughput nuclear magnetic resonance spectroscopy and surface plasmon resonance, and to generate the capacity for automation in chemical synthesis and sample preparation to expedite the development of novel bioactive molecules. The development of better approaches to hit development may benefit many researchers in Australia employing FBDD.Read moreRead less
New approaches to inhibition of activity of HIV integrase. This project aims to assist in the development of novel anti-HIV drugs that will benefit the 17000 Australians and more than 33 million people worldwide who are currently suffering with this terrible disease. The project will utilise state-of-the-art approaches in structure-based drug design to identify and synthesise compounds as leads for the development of anti-HIV drugs. Furthermore, the project will provide invaluable training for t ....New approaches to inhibition of activity of HIV integrase. This project aims to assist in the development of novel anti-HIV drugs that will benefit the 17000 Australians and more than 33 million people worldwide who are currently suffering with this terrible disease. The project will utilise state-of-the-art approaches in structure-based drug design to identify and synthesise compounds as leads for the development of anti-HIV drugs. Furthermore, the project will provide invaluable training for the researchers involved and enhance the relationship between the academic and commercial collaborators.Read moreRead less
Pushing The Boundaries Of Flow Chemistry – Towards New Anti-Viral Agents. Synthetic chemistry approaches to new drugs rely on access to robust reliable reactions. Traditionally these approaches are highly wasteful with the pharmaceutical industries producing five to a hundred kilograms of waste per kilogram of product. Total flow chemistry approaches will significantly reduce waste, allow rapid reaction sequence optimisation, and seamless scale up. In a collaborative effort spanning Australia, G ....Pushing The Boundaries Of Flow Chemistry – Towards New Anti-Viral Agents. Synthetic chemistry approaches to new drugs rely on access to robust reliable reactions. Traditionally these approaches are highly wasteful with the pharmaceutical industries producing five to a hundred kilograms of waste per kilogram of product. Total flow chemistry approaches will significantly reduce waste, allow rapid reaction sequence optimisation, and seamless scale up. In a collaborative effort spanning Australia, Germany and the USA, in an exemplar of a real world application, this project will produce benefits not only in enhanced and greener synthetic approaches, but also in the development of strategies for the identification of small molecules, the precursors to a new mode of action class of anti-viral drugs.Read moreRead less
Making peptides orally bioavailable. Bioactive peptides are exceptionally useful molecules, however to fully realise their exciting applications key limitations need to be overcome: they can't be delivered orally and they do not last long in the body. This project aims to develop a molecular tag that can dramatically enhance both the oral absorption and time in the body of a peptide. This will include identifying the key elements of the tag required for function, the breadth of peptide cargoes i ....Making peptides orally bioavailable. Bioactive peptides are exceptionally useful molecules, however to fully realise their exciting applications key limitations need to be overcome: they can't be delivered orally and they do not last long in the body. This project aims to develop a molecular tag that can dramatically enhance both the oral absorption and time in the body of a peptide. This will include identifying the key elements of the tag required for function, the breadth of peptide cargoes it can be applied to and the mechanisms underlying this technology. The outcomes of this project will facilitate the future development of peptides for biotechnology, pharmaceutical and veterinary applications.Read moreRead less
Understanding the molecular basis of heparanase activity. This project aims to advance our understanding of the structure and impact on biological processes of heparanase (HSPE), an enzyme of critical importance. HSPE’s ability to interact with heparan sulfate (HS), a key component of the extracellular matrix and basement membranes, makes HPSE a pivotal enzyme in many important physiological and disease-related processes ranging from angiogenesis, tumour metastasis, inflammation, hair follicle ....Understanding the molecular basis of heparanase activity. This project aims to advance our understanding of the structure and impact on biological processes of heparanase (HSPE), an enzyme of critical importance. HSPE’s ability to interact with heparan sulfate (HS), a key component of the extracellular matrix and basement membranes, makes HPSE a pivotal enzyme in many important physiological and disease-related processes ranging from angiogenesis, tumour metastasis, inflammation, hair follicle development to wrinkle formation. The knowledge gained through this project is expected to provide new insight into the interaction between HSPE and HS/HSPG to reveal new pathways to the development of inhibitors to treat diseases such as cancer and diabetes.Read moreRead less
Exploring the novel structural features of influenza virus sialidase. The outcomes of this project will provide a deeper mechanistic understanding of influenza virus sialidase and the importance of the enzyme's flexible loops in carbohydrate recognition. Specifically, this project will improve our understanding of fundamental aspects of inhibitor binding by influenza virus sialidases.