Elucidating the Mode of Action of Nicotinic Receptor Ligands. Changes in brain function can cause human diseases such as epilepsy, schizophrenia and Alzheimer's disease. To develop new medicines to treat these conditions we need to study how drugs act in the brain. This project will use new methods of chemistry to make drugs, which will then be tested for biological activity at important brain receptors. This will tell us which compounds are most effective as potential drugs and also exactly whe ....Elucidating the Mode of Action of Nicotinic Receptor Ligands. Changes in brain function can cause human diseases such as epilepsy, schizophrenia and Alzheimer's disease. To develop new medicines to treat these conditions we need to study how drugs act in the brain. This project will use new methods of chemistry to make drugs, which will then be tested for biological activity at important brain receptors. This will tell us which compounds are most effective as potential drugs and also exactly where they act in the brain. Read moreRead less
Development of Pyrrolopyrimidines as Inhibitors of ATP-Binding Proteins. This project seeks to generate analogues of natural products that have been found to be active against cancer cells and tropical parasites. The new materials produced by this project will aid in the study of biochemical processes involved in diseases such as cancer and lymphatic filariasis, thus leading the way to development of these compounds as potential treatments for such diseases.
ARC Centre of Excellence for Innovations in Peptide and Protein Science. The ARC Centre of Excellence for Innovations in Peptide and Protein Science (CIPPS) strives to build a critical understanding of peptides and proteins in order to unleash the potential of these biomolecules for human benefit. We will discover nature’s untapped reservoir of peptides and proteins, decode their structures and functions, and
develop enhanced synthetic technologies to address biology’s next grand challenge—the d ....ARC Centre of Excellence for Innovations in Peptide and Protein Science. The ARC Centre of Excellence for Innovations in Peptide and Protein Science (CIPPS) strives to build a critical understanding of peptides and proteins in order to unleash the potential of these biomolecules for human benefit. We will discover nature’s untapped reservoir of peptides and proteins, decode their structures and functions, and
develop enhanced synthetic technologies to address biology’s next grand challenge—the design of peptides and proteins for targeted scientific, agricultural, biotechnology, animal health and pharmaceutical applications. CIPPS will assemble leading researchers from diverse disciplines to create a sustainable national entity that will drive new Australian industries and train next generation researchers.Read moreRead less
High Pressure and Fluorous Approaches to Fostriecin Libraries: New Therapeutic Opportunities. The natural product, Fostriecin, displays considerable broad-spectrum anti-cancer activity, acting via a novel mechanism. However, this activity is tempered by its considerable instability, being too unstable to be used as a therapeutic agent. Using state-of-the-art approaches we will, rapidly generate libraries of more stable and biologically active fostriecin analogues and examine their potential to b ....High Pressure and Fluorous Approaches to Fostriecin Libraries: New Therapeutic Opportunities. The natural product, Fostriecin, displays considerable broad-spectrum anti-cancer activity, acting via a novel mechanism. However, this activity is tempered by its considerable instability, being too unstable to be used as a therapeutic agent. Using state-of-the-art approaches we will, rapidly generate libraries of more stable and biologically active fostriecin analogues and examine their potential to be used anti-cancer agents. This project represents an opportunity for Australia to take a significant, innovative lead in the development of hitherto unforseen therapeutic agents.Read moreRead less
Fluorous Chemistry: New tagging agents and heterocyclic-based fluorous surfactants. Fluorous chemistry is emerging as a powerful adjunct to areas of conventional parallel and combinatorial organic syntheses, and its introduction has revolutionised separation technologies. In this project two new fluorous tagging strategies will be investigated in an effort to broaden the scope of reagents that can used in synthesis. Efforts will be directed to chiral auxiliaries and to fluorous catalyst ligands. ....Fluorous Chemistry: New tagging agents and heterocyclic-based fluorous surfactants. Fluorous chemistry is emerging as a powerful adjunct to areas of conventional parallel and combinatorial organic syntheses, and its introduction has revolutionised separation technologies. In this project two new fluorous tagging strategies will be investigated in an effort to broaden the scope of reagents that can used in synthesis. Efforts will be directed to chiral auxiliaries and to fluorous catalyst ligands. In addition, a novel class of fluorous surfactant will be investigated, for its surface properties (including its ability to self assemble) and for its utility in two specific applications, selective membrane-bound protein extraction (relevant to proteomics) and ophthalmics (biomaterials).Read moreRead less
Synthesis and evaluation of anti-microbial porphyrin adducts for the targeted inhibition of Porphyromonas gingivalis. At present the effectiveness of therapy for inflammatory disease of the gum tissue (periodontitis) is limited by the lack of a selective anti-microbial agent. The investigators have discovered a novel mechanism of binding of the blood product porphyrin by a unique receptor of a key pathogen implicated in this disease. By exploiting this knowledge a modified porphyrin linked to an ....Synthesis and evaluation of anti-microbial porphyrin adducts for the targeted inhibition of Porphyromonas gingivalis. At present the effectiveness of therapy for inflammatory disease of the gum tissue (periodontitis) is limited by the lack of a selective anti-microbial agent. The investigators have discovered a novel mechanism of binding of the blood product porphyrin by a unique receptor of a key pathogen implicated in this disease. By exploiting this knowledge a modified porphyrin linked to an antibiotic was shown to have a selective effect on the target organism. Refinement of this complex has the potential to provide a clinically useful, selective agent.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE0236167
Funder
Australian Research Council
Funding Amount
$580,000.00
Summary
The Sydney Combinatorial Research Facility. The proposal is to establish a multidisciplinary inter-institutional research facility for solution-phase combinatorial chemistry synthesis and analysis, and medium to high throughput biological evaluation of lead compounds through fluorescence detection methods. This will be the first and only multi-user facility of its type in Sydney. It will provide through its synthetic node at NSW and Macquarie Universities and biological screening node at Univers ....The Sydney Combinatorial Research Facility. The proposal is to establish a multidisciplinary inter-institutional research facility for solution-phase combinatorial chemistry synthesis and analysis, and medium to high throughput biological evaluation of lead compounds through fluorescence detection methods. This will be the first and only multi-user facility of its type in Sydney. It will provide through its synthetic node at NSW and Macquarie Universities and biological screening node at University of Sydney an essential resource that will enable modern combinatorial techniques to be applied to chemical and drug-lead development studies in the region.Read moreRead less
Chemical synthesis of cancer-associated glycoproteins. Glycosylation of proteins is an extremely common event which plays an important role in a variety of biological processes. Aberrant glycosylation and over-production of glycoproteins is associated with numerous cancer types (including breast, prostate, ovarian and small lung) and are recognised as promising agents for disease diagnosis and vaccine development. A range of cancer-associated glycoproteins will be synthesised in this research p ....Chemical synthesis of cancer-associated glycoproteins. Glycosylation of proteins is an extremely common event which plays an important role in a variety of biological processes. Aberrant glycosylation and over-production of glycoproteins is associated with numerous cancer types (including breast, prostate, ovarian and small lung) and are recognised as promising agents for disease diagnosis and vaccine development. A range of cancer-associated glycoproteins will be synthesised in this research program using a number of novel chemical technologies. These glycoproteins will be used to develop cancer vaccines and diagnostics. Cancer is a severe burden on the Australian community and on the economy, therefore this research will be of significant benefit to Australia.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE0561203
Funder
Australian Research Council
Funding Amount
$110,000.00
Summary
Microwave Assisted Chemistry - new approaches to molecular diversity. This project will support the establishment of a multi-user, fully automated microwave reactor facility that will be the first of its kind in an academic laboratory in Australia. The equipment will support a wide range of synthetic chemistry research by providing microwave acceleration to otherwise slow reactions and in some cases promotion of reactions that do not normally proceed under conventional conditions. The automation ....Microwave Assisted Chemistry - new approaches to molecular diversity. This project will support the establishment of a multi-user, fully automated microwave reactor facility that will be the first of its kind in an academic laboratory in Australia. The equipment will support a wide range of synthetic chemistry research by providing microwave acceleration to otherwise slow reactions and in some cases promotion of reactions that do not normally proceed under conventional conditions. The automation capability will be used to create diverse compound libraries and to investigate and optimise reaction conditions.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE0238898
Funder
Australian Research Council
Funding Amount
$352,000.00
Summary
Novel Optical Microprobes - fluorescence excitation, lifetime and surface enhanced Raman spectroscopies. State-of-the-art technologies in microscopy will be combined with the versatility and diagnostic power of spectroscopy for the analysis and identification of materials by methods sensitive to chemical structure as well as spatial inhomogeneity. The proposed systems will operate within an existing multi-user optical characterisation facility at Macquarie University thus supporting the research ....Novel Optical Microprobes - fluorescence excitation, lifetime and surface enhanced Raman spectroscopies. State-of-the-art technologies in microscopy will be combined with the versatility and diagnostic power of spectroscopy for the analysis and identification of materials by methods sensitive to chemical structure as well as spatial inhomogeneity. The proposed systems will operate within an existing multi-user optical characterisation facility at Macquarie University thus supporting the research of an established and expanding network of researchers in the Sydney area and in Melbourne. The suite of instruments will provide new and exciting avenues for interdisciplinary research between the physical and biological sciencesRead moreRead less