Development of small molecule primary sulfonamides as new drugs for malaria. Malaria is a major global health threat, causing approximately 800,000 deaths annually. Lives can be saved if patients are treated. The use of current antimalarial drugs is limited by drug resistance, low activity and poor safety. This project investigates the effectiveness of a new class of molecule as a safe drug treatment option to kill malaria parasites.
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
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
Liposaccharide based peptide and vaccine delivery systems: improving the bioavailability and immunogenicity of Luteinizing Hormone-Releasing Hormone. This project aims to develop new lipid- and sugar-based drug delivery systems for Luteinizing-hormone-releasing hormone (LHRH), a hormone which regulates the level of enzymes involved in fertility conditions and prostate cancers. This technology could be extended to significantly increase the number of drugs available on the market, such as peptide ....Liposaccharide based peptide and vaccine delivery systems: improving the bioavailability and immunogenicity of Luteinizing Hormone-Releasing Hormone. This project aims to develop new lipid- and sugar-based drug delivery systems for Luteinizing-hormone-releasing hormone (LHRH), a hormone which regulates the level of enzymes involved in fertility conditions and prostate cancers. This technology could be extended to significantly increase the number of drugs available on the market, such as peptide drugs and vaccines.Read moreRead less
Rational design of new drug candidates for the treatment of Trypanosoma cruzi infection. There is a serious shortage of safe and effective drugs to treat Chagas disease which is caused by a parasitic infection. This project aims to design and identify new drug candidates by defining the disposition profile within the body which is necessary to achieve a therapeutic effect.
Translating pharmacokinetic and pharmacodynamic data to better design new drugs for the treatment of Trypanosoma cruzi infection. New drugs to treat T. cruzi infection are urgently needed, however their design has been hampered by an incomplete understanding of complex host-parasite interactions, inadequate in vitro and in vivo tools to rigorously define activity during drug discovery, and a poor appreciation of concentration/effect relationships. This project aims to develop new and much needed ....Translating pharmacokinetic and pharmacodynamic data to better design new drugs for the treatment of Trypanosoma cruzi infection. New drugs to treat T. cruzi infection are urgently needed, however their design has been hampered by an incomplete understanding of complex host-parasite interactions, inadequate in vitro and in vivo tools to rigorously define activity during drug discovery, and a poor appreciation of concentration/effect relationships. This project aims to develop new and much needed in vitro methods to better define the kinetic and dynamic activity of new drug candidates, and will provide a rational basis for translating this information into lengthy animal models of T. cruzi infection. The outcome aims to be rationally designed drug candidates that are available in a shorter period of time and are suitable for further development.Read moreRead less
Lymphotropic prodrugs: a novel mechanism for targeted drug delivery. This project aims to design chemically modified drugs that target drug delivery specifically to white blood cells. This approach promises to maximise drug action and simultaneously reduce toxicity for diseases where lymphocytes are the major drug target. These include autoimmune disease, leukaemia, lymphoma, HIV, transplant rejection and diabetes.
Open source drug discovery for malaria. This project aims to discover a new drug for the treatment of malaria. In stark contrast to the traditional process of drug discovery, and to accelerate the project's progress, the research will be open source, meaning that anyone can participate and there will be no patents.
Screening platforms for malaria drug discovery: identification of new therapeutics. Innovative image based technologies will be developed to identify molecules which stop malaria parasite growth and its transmission to the mosquito host. As more resistance is emerging against the current drugs of choice, new molecules acting through different mechanisms are urgently needed.