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
Nicotinic receptor structure and function probed with conotoxins. Nicotinic receptors are intrinsic membrane proteins that play a role in communication in excitable cells, particularly in the nervous system. The primary goals of this project are to define the structural and functional determinants of nicotinic-conotoxin interactions at a molecular level, and develop new selective probes that advance neurophysiological research. The diversity and distribution of nicotinic receptor subtypes being ....Nicotinic receptor structure and function probed with conotoxins. Nicotinic receptors are intrinsic membrane proteins that play a role in communication in excitable cells, particularly in the nervous system. The primary goals of this project are to define the structural and functional determinants of nicotinic-conotoxin interactions at a molecular level, and develop new selective probes that advance neurophysiological research. The diversity and distribution of nicotinic receptor subtypes being uncovered through molecular biology and selective conotoxin probes presents an exciting opportunity for the discovery of new therapeutic agents.Read moreRead less
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
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
Computational enzymology: exploring the free energy landscape of enzymatic catalysis. Most biochemical reactions depend on enzyme catalysis and understanding how enzymes work at the molecular level remains a central question. This project will develop a suite of computational models to study the mechanisms of enzyme-catalysed reactions and such knowledge holds promise for technological benefits in the form of new drugs and novel catalysts.
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