Discovery and development of novel insulin sensitising compounds for the treatment of Type 2 diabetes. Diabetes is one of the major health problems facing Australia today, and current treatments are proving inadequate to combat this disease. We previously discovered a new drug with potential for development for the treatment of diabetes. In this project, we will identify how this drug works to combat diabetes in cell and animal models, and use novel chemistry approaches to modify the drug to imp ....Discovery and development of novel insulin sensitising compounds for the treatment of Type 2 diabetes. Diabetes is one of the major health problems facing Australia today, and current treatments are proving inadequate to combat this disease. We previously discovered a new drug with potential for development for the treatment of diabetes. In this project, we will identify how this drug works to combat diabetes in cell and animal models, and use novel chemistry approaches to modify the drug to improve its properties and reduce potential side-effects. The outcomes of this project will be understanding of a new biological process that contributes to the development of diabetes, and the discovery and characterisation of new chemical compounds that could be developed as drugs to treat diabetes.Read moreRead less
Bioactive Peptides as Pharmacological Tools and Novel Drug Leads. Bioactive peptides are produced by all organisms and play numerous critical physiological roles, including in cellular communication, host defence and capture of prey. Peptides have huge potential as tools for studying roles of signalling pathways and as novel drugs due to their high affinity and selectivity for various therapeutically relevant targets. However their use has been limited by poor in vivo stability. This project is ....Bioactive Peptides as Pharmacological Tools and Novel Drug Leads. Bioactive peptides are produced by all organisms and play numerous critical physiological roles, including in cellular communication, host defence and capture of prey. Peptides have huge potential as tools for studying roles of signalling pathways and as novel drugs due to their high affinity and selectivity for various therapeutically relevant targets. However their use has been limited by poor in vivo stability. This project is focused on studying structural features of a range of peptides and their contributions to both activity and to resistance against degradation, with the aim to develop stabilised bioactive peptide sequences for in vivo applications, allowing the full potential of peptides as drugs to be realised.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
New approaches to inhibition of activity of HIV integrase. This project aims to assist in the development of novel anti-HIV drugs that will benefit the 17000 Australians and more than 33 million people worldwide who are currently suffering with this terrible disease. The project will utilise state-of-the-art approaches in structure-based drug design to identify and synthesise compounds as leads for the development of anti-HIV drugs. Furthermore, the project will provide invaluable training for t ....New approaches to inhibition of activity of HIV integrase. This project aims to assist in the development of novel anti-HIV drugs that will benefit the 17000 Australians and more than 33 million people worldwide who are currently suffering with this terrible disease. The project will utilise state-of-the-art approaches in structure-based drug design to identify and synthesise compounds as leads for the development of anti-HIV drugs. Furthermore, the project will provide invaluable training for the researchers involved and enhance the relationship between the academic and commercial collaborators.Read moreRead less
Surface ligation of nanomaterials for biomedical applications . The project aims to explore the synergistic effects co-ligands for target recognition and biofouling protection in nanoparticle surface patterns to enable practical atomic scale precision engineering of efficient and biofouling resistant nanosensors. The project will fundamentally characterise interfacial interactions and dynamics of ligated nano-surfaces and biomolecules via advanced computer modelling. Outcomes should include pra ....Surface ligation of nanomaterials for biomedical applications . The project aims to explore the synergistic effects co-ligands for target recognition and biofouling protection in nanoparticle surface patterns to enable practical atomic scale precision engineering of efficient and biofouling resistant nanosensors. The project will fundamentally characterise interfacial interactions and dynamics of ligated nano-surfaces and biomolecules via advanced computer modelling. Outcomes should include practical molecular design guidelines for functional ligands and predicted optimal patterns for combining functional and antifouling ligands on gold nanomaterials for biosensing technologies. The advanced predictive modelling capabilities will facilitate future practical engineering of efficient biomedical devices.Read moreRead less
Ultrasound-assisted fabrication of biofunctional materials. The project aims to develop a fundamental understanding of the mechanism involved in the synthetic process in order to control the physical and functional properties of core-shell biomaterials. Biofunctional core-shell materials are of scientific interest due to their potential use in a variety of applications including food manufacturing. Among existing methodologies for the synthesis of core-shell biomaterials, ultrasonic technology o ....Ultrasound-assisted fabrication of biofunctional materials. The project aims to develop a fundamental understanding of the mechanism involved in the synthetic process in order to control the physical and functional properties of core-shell biomaterials. Biofunctional core-shell materials are of scientific interest due to their potential use in a variety of applications including food manufacturing. Among existing methodologies for the synthesis of core-shell biomaterials, ultrasonic technology offers versatility and a wider choice of core and shell materials possessing specific biofunctionality. The outcomes of this project may include the establishment of a versatile technology for the fabrication of tailor-made biofunctional materials suitable for specific applications.Read moreRead less
Industrial Transformation Training Centres - Grant ID: IC180100021
Funder
Australian Research Council
Funding Amount
$4,163,359.00
Summary
ARC Training Centre for the Development of Tools for Fragment Based Design. The ARC Training Centre for the Development of Tools for Fragment Based Design aims to inspire the next generation of drug discovery research leaders. It plans to provide direct experience with industry partners, training and master classes in early stage drug-discovery from industry experts. The Centre is expected to accelerate research translation and industry engagement by providing an efficient strategy for the scree ....ARC Training Centre for the Development of Tools for Fragment Based Design. The ARC Training Centre for the Development of Tools for Fragment Based Design aims to inspire the next generation of drug discovery research leaders. It plans to provide direct experience with industry partners, training and master classes in early stage drug-discovery from industry experts. The Centre is expected to accelerate research translation and industry engagement by providing an efficient strategy for the screening of a biological target and early medicinal chemistry for optimisation. The expected outcome of the Centre is to equip the trainees with the skills to make key contributions to the sustainability and growth of the sector and to provide significant capacity to address global challenges for 21st century pharmaceutical innovation.Read moreRead less
Discovery Early Career Researcher Award - Grant ID: DE140100550
Funder
Australian Research Council
Funding Amount
$358,248.00
Summary
Quantum refinement of DNA X-ray structures. DNA carries the genetic map of life and refinement of its x-ray structures is a key tool to understand its functions. Standard refinement, however, relies strongly on empirical geometry constraints, and it is known that these can induce unphysical features. Quantum mechanical (QM) methods have now evolved to a level that offers an intriguing way out of this dilemma. In this project, state-of-the-art QM methods will be applied to DNA x-ray structures, a ....Quantum refinement of DNA X-ray structures. DNA carries the genetic map of life and refinement of its x-ray structures is a key tool to understand its functions. Standard refinement, however, relies strongly on empirical geometry constraints, and it is known that these can induce unphysical features. Quantum mechanical (QM) methods have now evolved to a level that offers an intriguing way out of this dilemma. In this project, state-of-the-art QM methods will be applied to DNA x-ray structures, and a unique quantum refinement scheme will be developed. Such a scheme will provide crystallographers with a new tool to determine DNA structures with greater accuracy and it will offer benefits to many areas of the life sciences that depend on such accurate structures.Read moreRead less
Nicotinic receptor structure and function probed with conotoxins. Nicotinic receptors are intrinsic membrane proteins that play a role in communication in excitable cells, particularly in the nervous system. The primary goals of this project are to define the structural and functional determinants of nicotinic-conotoxin interactions at a molecular level, and develop new selective probes that advance neurophysiological research. The diversity and distribution of nicotinic receptor subtypes being ....Nicotinic receptor structure and function probed with conotoxins. Nicotinic receptors are intrinsic membrane proteins that play a role in communication in excitable cells, particularly in the nervous system. The primary goals of this project are to define the structural and functional determinants of nicotinic-conotoxin interactions at a molecular level, and develop new selective probes that advance neurophysiological research. The diversity and distribution of nicotinic receptor subtypes being uncovered through molecular biology and selective conotoxin probes presents an exciting opportunity for the discovery of new therapeutic agents.Read moreRead less
The mechanism of membrane disruption by antimicrobial peptides. Bacterial resistance to antibiotics is a growing crisis in modern medicine. Antibacterial peptides from Australian frogs represent a new class of potent and selective antibacterial agents. Understanding how these peptides kill bacteria but not vertebrate cells could lead to the design of new drugs for pharmaceutical and/or clinical purposes.