Natural Product-derived Proteomics Probes for Specific Detection of Protein Kinase C Activities. Better health care depends on how well diseases are understood and how accurately disease analysis and diagnosis can be carried out. This is not only important to disease treatment but also prevention. This project will first generate new compounds that could have improved therapeutic value in cancer treatment. In addition, these compounds will be further engineered to provide a new technology of ....Natural Product-derived Proteomics Probes for Specific Detection of Protein Kinase C Activities. Better health care depends on how well diseases are understood and how accurately disease analysis and diagnosis can be carried out. This is not only important to disease treatment but also prevention. This project will first generate new compounds that could have improved therapeutic value in cancer treatment. In addition, these compounds will be further engineered to provide a new technology of tracing the molecular signature of diseases such as cancer for early detection and better preventative care and treatment. This will create new economic advantage and contributes to the transformation of Australian health care industry.Read moreRead less
Synthesis of new heterocyclic analogues of isoflavones. Intake of high dietary isoflavonoid phytoestrogens has been linked to low prevalence of hormone-dependent cancers such as breast and prostate cancer, and heart disease. The isoflavones resemble endogenous estradiol in structure, and have been shown to display weak estrogenic activity. Novogen Limited is pioneering the development of novel drug candidates based on isoflavones. This collaborative research project deals with the development o ....Synthesis of new heterocyclic analogues of isoflavones. Intake of high dietary isoflavonoid phytoestrogens has been linked to low prevalence of hormone-dependent cancers such as breast and prostate cancer, and heart disease. The isoflavones resemble endogenous estradiol in structure, and have been shown to display weak estrogenic activity. Novogen Limited is pioneering the development of novel drug candidates based on isoflavones. This collaborative research project deals with the development of synthetic methodologies for the preparation of new analogues of isoflavone metabolites as potential drug candidates. The target compounds will be evaluated for possible therapeutic use by the industry partner.Read moreRead less
Synthesis of pyrroloquinoline analogues of isoflavone metabolites. Cancer and heart disease are the two main diseases that affect our society indiscriminately and put enormous drains on healthcare resources. The intake of high dietary isoflavonoid phytoestrogens has been linked to low prevalence of cancers and heart disease. Novogen Limited is pioneering the development of novel drug candidates based on phytoestrogen metabolites. This collaborative research project deals with the development ....Synthesis of pyrroloquinoline analogues of isoflavone metabolites. Cancer and heart disease are the two main diseases that affect our society indiscriminately and put enormous drains on healthcare resources. The intake of high dietary isoflavonoid phytoestrogens has been linked to low prevalence of cancers and heart disease. Novogen Limited is pioneering the development of novel drug candidates based on phytoestrogen metabolites. This collaborative research project deals with the development of synthetic methodologies for the preparation of new analogues of phytoestrogen metabolites as potential drug candidates. The target compounds will be evaluated for possible therapeutic use by the industry partner.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
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
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.
The Baylis-Hillman Reaction: Asymmetric Organocatalysis and Applications. Many drugs come in two chiral mirror images (enantiomers) where the therapeutic effect is usually associated with only one while the other has no effect or can be harmful as was the case with thalidomide. Chemical reactions that yield just the desired mirror image, or enantiomer, and not the other are therefore in great demand and heavily pursued by the pharmaceutical, fine chemical and materials industries as a frontier ....The Baylis-Hillman Reaction: Asymmetric Organocatalysis and Applications. Many drugs come in two chiral mirror images (enantiomers) where the therapeutic effect is usually associated with only one while the other has no effect or can be harmful as was the case with thalidomide. Chemical reactions that yield just the desired mirror image, or enantiomer, and not the other are therefore in great demand and heavily pursued by the pharmaceutical, fine chemical and materials industries as a frontier technology. This project will result in the development of novel catalytic reactions that allow the synthesis of chiral chemicals in a cost-efficient and green manner needed by many industries, and also training of students with highly desirable synthetic skills to lead the next wave in pharmaceuticals and biotechnology.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
Praziquantel: a unique pharmaceutical challenge. Generating effective and affordable drugs for the treatment of tropical diseases is a huge public health challenge. We will pioneer an open source approach to collaborative research in drug discovery. We aim to discover an inexpensive route to an important pharmaceutical so that it can be greatly improved and distributed to the affected populations for a realistic price. Success in this project will improve the lives of millions of sufferers of th ....Praziquantel: a unique pharmaceutical challenge. Generating effective and affordable drugs for the treatment of tropical diseases is a huge public health challenge. We will pioneer an open source approach to collaborative research in drug discovery. We aim to discover an inexpensive route to an important pharmaceutical so that it can be greatly improved and distributed to the affected populations for a realistic price. Success in this project will improve the lives of millions of sufferers of this disease, and demonstrate a new way of doing research on drugs for related diseases such as malaria. Read moreRead less