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Intracellular lipid binding proteins as gatekeepers of drug activity. This project will explore the mechanisms by which drug molecules interact with lipid transport pathways within cells. The data obtained will provide a framework for the design of a new generation of drug candidates which have the potential to hijack intracellular transport pathways as a mechanism of targeted delivery to their sites of action.
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
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.
Novel chemoenzymatic synthesis and bioconjugation of peptides and proteins. This project aims to solve the critical difficulty of producing the complex peptide insulin and related insulin-like peptides (INSLs) and their analogues. The project will use unique, recyclable enzymes which ligate smaller peptide segments with extraordinary site and substrate selectivity. The expected outcome of the project is novel, cheaper and scalable, enzyme-mediated engineering of this critical class of peptides a ....Novel chemoenzymatic synthesis and bioconjugation of peptides and proteins. This project aims to solve the critical difficulty of producing the complex peptide insulin and related insulin-like peptides (INSLs) and their analogues. The project will use unique, recyclable enzymes which ligate smaller peptide segments with extraordinary site and substrate selectivity. The expected outcome of the project is novel, cheaper and scalable, enzyme-mediated engineering of this critical class of peptides as biological probes and potential therapeutic agents.Read moreRead less
Atomic details of antimicrobial peptides at work in live cells. This project aims to develop methods to determine the detailed structure of biologically important molecules in live cells to better understand how biomolecular structure is related to disease. The structure at the atomic level of the molecules of life is usually characterised by crystal or solution studies in model systems. However, the structure of many biologically important molecules depends on their environment. Using new instr ....Atomic details of antimicrobial peptides at work in live cells. This project aims to develop methods to determine the detailed structure of biologically important molecules in live cells to better understand how biomolecular structure is related to disease. The structure at the atomic level of the molecules of life is usually characterised by crystal or solution studies in model systems. However, the structure of many biologically important molecules depends on their environment. Using new instrumentation and labelling schemes, the project plans to use nuclear magnetic resonance methods to study antibiotics and antimicrobial peptides in live bacteria and human cells. The goal is to resolve how these molecules cross cell membranes and how biomolecular structure is related to activity, which may advance development in biotechnology and therapeutic treatments against drug-resistant infections.Read moreRead less
New Conus-derived alpha-conotoxin analgesics for the treatment of chronic pain: structure, mode of action, delivery and disposition. 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 cone snail derived peptides will provide exciting new leads for achieving effective analgesia.
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.
Innovations in peptide-based drug design. This project will aim to develop new types of drugs that fill a gap between existing small molecule drugs, which are relatively inexpensive and stable, but often have side-effects, and biologics which are very expensive and require injection. Our new generation of peptide-based drugs promise to be applicable to diseases that are not treatable by current drugs.
A combinatorial approach to creation of new epitopes with biological activity. We aim to develop and extend the Mosaic technology patented by Proxima Concepts Ltd. as a new methodolgy for dynamic combinatorial chemistry and drug delivery. The technology relies on bringing chemical structures of interest in close proximity by presenting them on the surface of a micelle type structure. These structures will also be developed at a targeted drug delivery vehicle. The technology will impact on the ....A combinatorial approach to creation of new epitopes with biological activity. We aim to develop and extend the Mosaic technology patented by Proxima Concepts Ltd. as a new methodolgy for dynamic combinatorial chemistry and drug delivery. The technology relies on bringing chemical structures of interest in close proximity by presenting them on the surface of a micelle type structure. These structures will also be developed at a targeted drug delivery vehicle. The technology will impact on the areas of drug discovery and drug delivery.Read moreRead less