Facilitating drug synthesis, development and detection: the enzymatic synthesis of beta-glucuronides. This project will develop new catalysts to aid the development of pharmaceuticals and help fight the war against drugs.
Harnessing molecular strain for drug discovery and bioconjugation. Peptides and proteins are increasingly important therapies for the treatment of disease. Nevertheless, the synthesis and optimisation of these high-value compounds still relies primarily on technologies developed decades ago. There is a desperate need for modern strategies to unlock the full potential of peptides and proteins for diverse applications in drug discovery. This interdisciplinary research aims to develop new tools for ....Harnessing molecular strain for drug discovery and bioconjugation. Peptides and proteins are increasingly important therapies for the treatment of disease. Nevertheless, the synthesis and optimisation of these high-value compounds still relies primarily on technologies developed decades ago. There is a desperate need for modern strategies to unlock the full potential of peptides and proteins for diverse applications in drug discovery. This interdisciplinary research aims to develop new tools for the construction and modification of peptides and proteins by harnessing the energy in a unique class of strained molecules. A focus on peptide-based inhibitors of the proteasome, a critical target for modern cancer treatments, should provide future health and economic benefits for the Australian community.Read moreRead less
New Protocols for the Chemical Synthesis of Biologically Relevant Systems. Enzyme- and metal-catalysed processes will be developed and exploited for the purpose of establishing concise syntheses of biologically active and otherwise inaccessible natural products and their analogues. The range of structures to be targeted is structurally diverse and these have the potential to act as agrochemicals and/or as therapeutic agents for the treatment of a range of disease states in mammals including bact ....New Protocols for the Chemical Synthesis of Biologically Relevant Systems. Enzyme- and metal-catalysed processes will be developed and exploited for the purpose of establishing concise syntheses of biologically active and otherwise inaccessible natural products and their analogues. The range of structures to be targeted is structurally diverse and these have the potential to act as agrochemicals and/or as therapeutic agents for the treatment of a range of disease states in mammals including bacterial and viral infections, neuro-degenerative conditions and impaired cognitive function. Anti-angiogenic compounds that control otherwise unregulated cellular growth may also arise from these studies. The generation of new, homochiral metabolites for use in chemoenzymatic synthesis should also emerge from this project.Read moreRead less
Harnessing strain for chemical synthesis: The cyclopropane angle. This project aims to develop new reaction pathways of cyclopropanes, the smallest and most strained monocyclic ring systems, but which are also stable and easily prepared. Cyclopropanes have unique capacities to serve as highly effective building blocks in the synthesis of a wide range of otherwise difficult to access and biologically active molecular frameworks. This project will use cyclopropanes to rapidly assemble biologically ....Harnessing strain for chemical synthesis: The cyclopropane angle. This project aims to develop new reaction pathways of cyclopropanes, the smallest and most strained monocyclic ring systems, but which are also stable and easily prepared. Cyclopropanes have unique capacities to serve as highly effective building blocks in the synthesis of a wide range of otherwise difficult to access and biologically active molecular frameworks. This project will use cyclopropanes to rapidly assemble biologically active systems, especially pharmaceutically or agrochemically valuable natural products and relevant analogues.Read moreRead less
Enabling Methodologies for the Synthesis of Biologically Active Compounds. This project seeks to establish flexible methods of chemical synthesis for creating new molecular scaffolds capable of achieving selective enzyme inhibition. The approach aims to exploit the vast and biologically-programmed structural diversity associated with natural products. Unique, small molecule organic compounds will be obtained that reveal details of the operation of key enzymes in bacterial and mammalian systems. ....Enabling Methodologies for the Synthesis of Biologically Active Compounds. This project seeks to establish flexible methods of chemical synthesis for creating new molecular scaffolds capable of achieving selective enzyme inhibition. The approach aims to exploit the vast and biologically-programmed structural diversity associated with natural products. Unique, small molecule organic compounds will be obtained that reveal details of the operation of key enzymes in bacterial and mammalian systems. Such new knowledge would allow for the design of highly selective therapeutic agents relevant to the treatment of a range of diseases including bacterial infections, diabetes and cancer. The high-end scientific training and privileged forms of matter arising from this work would provide major benefit to the biotech sector.Read moreRead less
Discovery Early Career Researcher Award - Grant ID: DE180100092
Funder
Australian Research Council
Funding Amount
$418,107.00
Summary
A radical approach to unnatural amino acids and peptide-based antibiotics. This project aims to develop a new synthetic approach to valuable amino acid derivatives and their rapid incorporation into peptide analogues, including promising new antibiotic candidates. This project expects to generate knowledge in the chemical and biological sciences and build scientific capacity to address the global rise of antimicrobial resistance. It is anticipated that this will provide direct health and economi ....A radical approach to unnatural amino acids and peptide-based antibiotics. This project aims to develop a new synthetic approach to valuable amino acid derivatives and their rapid incorporation into peptide analogues, including promising new antibiotic candidates. This project expects to generate knowledge in the chemical and biological sciences and build scientific capacity to address the global rise of antimicrobial resistance. It is anticipated that this will provide direct health and economic benefits by establishing a powerful platform for peptide drug design.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE130100213
Funder
Australian Research Council
Funding Amount
$840,000.00
Summary
Multinuclear 700 MHz Nuclear Magnetic Resonance (NMR) spectrometer for advanced molecular analysis. Nuclear Magnetic Resonance (NMR) spectroscopy is the most important analytical tool in chemistry. A new 700 MHz NMR spectrometer is to replace three outdated NMR spectrometers at the NMR Facility to enable new multinuclear experiments, while serving the analytical needs of over 20 research groups in chemical and biological research.
An Open Source Approach to Understanding an Important Parasite Ion Pump. This project plans to synthesise new compounds that bind the protein ATP4, an essential ion pump in the malaria parasite. It plans to generate a three-dimensional map to understand how these compounds stop ATP4 from working. Several promising new medicines for malaria target ATP4, yet we do not understand properly how they do so. The project’s intended aims will be achieved using new methods in synthetic chemistry and membr ....An Open Source Approach to Understanding an Important Parasite Ion Pump. This project plans to synthesise new compounds that bind the protein ATP4, an essential ion pump in the malaria parasite. It plans to generate a three-dimensional map to understand how these compounds stop ATP4 from working. Several promising new medicines for malaria target ATP4, yet we do not understand properly how they do so. The project’s intended aims will be achieved using new methods in synthetic chemistry and membrane biology, and by leveraging global scientific inputs through online research methods allowing anyone to participate.Read moreRead less
Discovery Early Career Researcher Award - Grant ID: DE170101438
Funder
Australian Research Council
Funding Amount
$360,000.00
Summary
Application of boronate ester-appended scaffolds in drug-discovery. This project aims to improve carbohydrate synthesis. Glycochemistry is an increasingly important chemical science that combines organic synthesis with biology. This project will develop methodologies that incorporate boronate ester residues onto selected carbons of monosaccharides and transform them to obtain hitherto inaccessible scaffolds for drug discovery. This strategy can be used in the controlled assembly of other biologi ....Application of boronate ester-appended scaffolds in drug-discovery. This project aims to improve carbohydrate synthesis. Glycochemistry is an increasingly important chemical science that combines organic synthesis with biology. This project will develop methodologies that incorporate boronate ester residues onto selected carbons of monosaccharides and transform them to obtain hitherto inaccessible scaffolds for drug discovery. This strategy can be used in the controlled assembly of other biologically important compounds, including azacycles, oxacycles and inositols. The methods for the controlled diversification of carbohydrates are expected to be broadly applicable to scientific endeavours ranging from glycobiology to medicine. Successful execution will provide new drug-discovery tools and ensure Australia secures a competitive position in this rapidly expanding discipline.Read moreRead less
Synthesis and Biological Evaluation of Australian Sponge Metabolites. The development of concise and flexible syntheses of Australian marine natural products and analogues of ecological/therapeutic significance will emerge. Such activities will lead to the identification and evaluation of molecular entities of value in managing marine environments and help to enhance chemical synthesis capacity in Australia.