Linkage Infrastructure, Equipment And Facilities - Grant ID: LE0453400
Funder
Australian Research Council
Funding Amount
$110,040.00
Summary
The Roboocyte™: a medium-throughput, secondary functional, screening facility. Changes in ion channel function have been implicated in a wide variety of human diseases. For this reason many researchers are studying ion channels to understand how they work and how they can develop new drug treatments. The slowest step in evaluating the biological activity of compounds is testing them against the ion channels and the current technology requires much tedious manual handling and extensive operator e ....The Roboocyte™: a medium-throughput, secondary functional, screening facility. Changes in ion channel function have been implicated in a wide variety of human diseases. For this reason many researchers are studying ion channels to understand how they work and how they can develop new drug treatments. The slowest step in evaluating the biological activity of compounds is testing them against the ion channels and the current technology requires much tedious manual handling and extensive operator expertise. The Roboocyte facility will triple testing productivity by allowing for the rapid and automated screening of large libraries of compounds. Such a facility will be unique to the Southern Hemisphere.Read moreRead less
Structural modification of conus-derived venom peptides- A route to new therapeutics. Current product deficiencies in the area of pain management are forcing the pharmaceutical industry to develop new strategies for achieving analgesia and reduce their dependence on traditional, addictive opiate-based products. Structural modification of Conus derived peptides will provide exciting new leads for achieving effective analgesia.
Allosteric modulators as novel probes of G-Protein coupled receptor function. This research will provide novel mechanistic understanding on the function of one of the largest protein families in the mammalian genome, and the most important family with respect to drug targets. The insights gained thus have direct relevance to drug discovery. The discovery of novel G protein-coupled receptor (GPCR) allosteric enhancers will not only lead to potentially new therapeutic agents, but can significant ....Allosteric modulators as novel probes of G-Protein coupled receptor function. This research will provide novel mechanistic understanding on the function of one of the largest protein families in the mammalian genome, and the most important family with respect to drug targets. The insights gained thus have direct relevance to drug discovery. The discovery of novel G protein-coupled receptor (GPCR) allosteric enhancers will not only lead to potentially new therapeutic agents, but can significantly value-add to other national research efforts focusing on GPCR structural biology.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
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
Alpha-Conotoxins: Selective Probes For Nicotinic Receptor Subtype Structure And Function. Marine snails from the waters off the Australian coast produce an amazing variety of mini-proteins in their venoms called conotoxins that they use to capture prey. These conotoxins bind very specifically to receptors in our body associated with the transmission of nerve signals. We will use natural and synthetically modified conotoxins to selectively block particular types of neuronal 'receptors' to gain a ....Alpha-Conotoxins: Selective Probes For Nicotinic Receptor Subtype Structure And Function. Marine snails from the waters off the Australian coast produce an amazing variety of mini-proteins in their venoms called conotoxins that they use to capture prey. These conotoxins bind very specifically to receptors in our body associated with the transmission of nerve signals. We will use natural and synthetically modified conotoxins to selectively block particular types of neuronal 'receptors' to gain a greater understanding of how the nervous system functions. This knowledge will help in the design of new drugs to treat a variety of diseases and disorders. Essentially we will use a chemical armoury developed by the cone snail to design state-of-the-art mini-protein drugs.Read moreRead less
Conotoxins: Novel probes for ion channel structure and function. Voltage-dependent and ligand-gated ion channels are intrinsic membrane proteins that play a central role in communication in excitable cells, particularly in the nervous system. The primary goals of this project are (i) to define at a molecular level, the structural and functional determinants of ion channel/conotoxin interactions and (ii) develop new probes that advance neurophysiological research. The diversity and distribution o ....Conotoxins: Novel probes for ion channel structure and function. Voltage-dependent and ligand-gated ion channels are intrinsic membrane proteins that play a central role in communication in excitable cells, particularly in the nervous system. The primary goals of this project are (i) to define at a molecular level, the structural and functional determinants of ion channel/conotoxin interactions and (ii) develop new probes that advance neurophysiological research. The diversity and distribution of ion channel types and subtypes being uncovered through the use of molecular biology and conotoxin probes presents an exciting opportunity for the future development of novel ion channel therapeutics.Read moreRead less
New modulators of voltage-gated sodium channel subtypes from Australian Tarantula venoms. The venoms of Australian tarantula spiders provide a unique and untapped source of bioactive molecules. From a large stock of venom, and in collaboration with Australian pharmaceutical company Xenome, we will develop a comprehensive library of venom components suitable for drug screening. Potential national benefits from this work include a huge reduction in the healthcare bill deriving from a new treatmen ....New modulators of voltage-gated sodium channel subtypes from Australian Tarantula venoms. The venoms of Australian tarantula spiders provide a unique and untapped source of bioactive molecules. From a large stock of venom, and in collaboration with Australian pharmaceutical company Xenome, we will develop a comprehensive library of venom components suitable for drug screening. Potential national benefits from this work include a huge reduction in the healthcare bill deriving from a new treatment for pain, as well as substantial royalty returns from drugs sales. Discoveries from the program are also likely to lead to an enhancement in Australia's reputation in the neurosciences and to the development of new diagnostic research tools. The major community benefit will be a reduction in the suffering of chronic pain patients.Read moreRead less
Defining mechanisms of action of novel alpha-conotoxins at nicotinic receptor-channels. Marine snails from the waters off the Australian coast produce an amazing variety of mini-proteins in their venoms called conotoxins that they use to capture prey. These conotoxins bind very specifically to receptors in our body associated with the transmission of nerve signals. We will use natural and synthetically modified conotoxins to selectively block particular types of neuronal 'receptors' to gain a gr ....Defining mechanisms of action of novel alpha-conotoxins at nicotinic receptor-channels. Marine snails from the waters off the Australian coast produce an amazing variety of mini-proteins in their venoms called conotoxins that they use to capture prey. These conotoxins bind very specifically to receptors in our body associated with the transmission of nerve signals. We will use natural and synthetically modified conotoxins to selectively block particular types of neuronal 'receptors' to gain a greater understanding of how the nervous system functions. This knowledge will help in the design of new drugs to treat a variety of diseases and disorders. Essentially we will use a chemical armoury developed by the cone snail to design state-of-the-art mini-protein drugs.Read moreRead less
Synthetic Endonucleases: Novel DNA Cleaving Agents for Cancer Chemotherapy. Cancer is a common disease in our society, with more than 1 in 4 of us dieing from it. The current survival rate is 50%, and has been so for the past 5 decades. Thus, there is clearly an urgent need for better forms of therapy. Chemotherapy is the mainstay of treatment once the disease has spread from its original site. The National Benefits from the development of a new class of effective cancer drug are two-fold. Firs ....Synthetic Endonucleases: Novel DNA Cleaving Agents for Cancer Chemotherapy. Cancer is a common disease in our society, with more than 1 in 4 of us dieing from it. The current survival rate is 50%, and has been so for the past 5 decades. Thus, there is clearly an urgent need for better forms of therapy. Chemotherapy is the mainstay of treatment once the disease has spread from its original site. The National Benefits from the development of a new class of effective cancer drug are two-fold. Firstly, much relief will come to people suffering from cancer, as some will live longer, and some will be cured. Secondly, the economic benefits are extensive, since the world market in cancer drugs is measured in billions $US, and significant monies will flow to those who hold the intellectual property rights. Read moreRead less