Linkage Infrastructure, Equipment And Facilities - Grant ID: LE0238397
Funder
Australian Research Council
Funding Amount
$550,000.00
Summary
A ROBOTIC NMR SPECTROMETER FOR ACCELERATED DRUG DISCOVERY. The aim is to establish a facility that will use a robotic NMR instrument to help in the characterisation of drug-protein interactions and in the discovery of new drugs or agrichemicals. The significance is that with the wealth of new information arising on protein sequences from genomics programs there is an urgent need to accelerate the rate of discovery of ligands that bind to these proteins. Such ligands may provide useful drug lea ....A ROBOTIC NMR SPECTROMETER FOR ACCELERATED DRUG DISCOVERY. The aim is to establish a facility that will use a robotic NMR instrument to help in the characterisation of drug-protein interactions and in the discovery of new drugs or agrichemicals. The significance is that with the wealth of new information arising on protein sequences from genomics programs there is an urgent need to accelerate the rate of discovery of ligands that bind to these proteins. Such ligands may provide useful drug leads or help in defining the function of newly discovered proteins. The outcomes will be new knowledge on protein structure and function, and potentially, new bio-active molecules.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE0453671
Funder
Australian Research Council
Funding Amount
$133,770.00
Summary
NMR Facility for Natural Products Research. The aim is to establish a facility that will use high-field NMR and LC-NMR equipment to help in the characterisation of unknown compounds from natural products and in the discovery of new drugs and agrichemicals. The significance is that the facility will accelerate the rate of discovery of new bioactive molecules and will provide a wealth of new information on plant biodiversity. The outcomes will be new knowledge in natural products chemistry, and po ....NMR Facility for Natural Products Research. The aim is to establish a facility that will use high-field NMR and LC-NMR equipment to help in the characterisation of unknown compounds from natural products and in the discovery of new drugs and agrichemicals. The significance is that the facility will accelerate the rate of discovery of new bioactive molecules and will provide a wealth of new information on plant biodiversity. The outcomes will be new knowledge in natural products chemistry, and potentially, new bioactive molecules.Read moreRead less
Large Scale Production of Stemona Alkaloids for Agricultural Applications and New Drug Discovery. The Stemona alkaloids form a large group of natural products that have significant potential as agricultural and pharmaceutical drugs. Extracts of these natural products have many applications in traditional medicine and as insecticides in Asia. We propose to develop innovative methods for the large scale production and synthesis of these bioactive alkaloids. The methodology and products developed ....Large Scale Production of Stemona Alkaloids for Agricultural Applications and New Drug Discovery. The Stemona alkaloids form a large group of natural products that have significant potential as agricultural and pharmaceutical drugs. Extracts of these natural products have many applications in traditional medicine and as insecticides in Asia. We propose to develop innovative methods for the large scale production and synthesis of these bioactive alkaloids. The methodology and products developed may have potential pharmaceutical and agricultural applications from which the country could benefit in the future. This project would help develop skilled people who may produce innovative outcomes in the future, especially in the developing pharmaceutical and biotechnology industries in Australia.Read moreRead less
The discovery and validation of novel drug classes against parasites with the potential for major economic impacts. This project will develop a quality scientific and technological program in national priority areas, leading to a strong basic research, new concepts and the enhanced international collaborative links; strengthen links between basic and applied research, and academia and industry; develop excellence via pan-Australian collaborations, resulting in a more efficient use of resources i ....The discovery and validation of novel drug classes against parasites with the potential for major economic impacts. This project will develop a quality scientific and technological program in national priority areas, leading to a strong basic research, new concepts and the enhanced international collaborative links; strengthen links between basic and applied research, and academia and industry; develop excellence via pan-Australian collaborations, resulting in a more efficient use of resources in a national and international context; enhance the skills-base in biology, biotechnology and chemistry; increase global visibility with increased investment in Australian science; improve animal welfare and production via improved control of infectious diseases; producing commercial products with benefits to agricultural producers in regional & rural communities.Read moreRead less
Experimental Charge Density Studies of Hydrogen Bonding. Hydrogen bonds, vital to all biological systems, exhibit extreme variation in chemical properties. Experimental analysis of hydrogen bonds, independent from previous theories and hypotheses, by using an expansion of current high resolution, ultra-low temperature X-ray crystallography is now possible. This allows experimental observation of electronic and electrostatic properties of previously unstudied hydrogen bonds, including weak hydrog ....Experimental Charge Density Studies of Hydrogen Bonding. Hydrogen bonds, vital to all biological systems, exhibit extreme variation in chemical properties. Experimental analysis of hydrogen bonds, independent from previous theories and hypotheses, by using an expansion of current high resolution, ultra-low temperature X-ray crystallography is now possible. This allows experimental observation of electronic and electrostatic properties of previously unstudied hydrogen bonds, including weak hydrogen bonds and those involving metal atoms. Comparison of experimental observations with predictions from high-level theoretical calculations and finally incorporation of these parameters into a prototype force field for computational chemistry will allow better predictions to be made in a range of areas including medicinal and materials chemistry.Read moreRead less
Inhibitors of enzymes in the lysine biosynthetic pathway. Recent reports of increasing bacterial resistance to antibiotics highlight the need for continual development of new antibacterial agents. Inhibitors of the biosynthesis of the amino acid lysine - an essential component of bacterial proteins and cell wall - may provide a novel class of antibiotics. This project describes investigations of the mechanism of the first two enzymes in the lysine biosynthetic pathway and the design and synthesi ....Inhibitors of enzymes in the lysine biosynthetic pathway. Recent reports of increasing bacterial resistance to antibiotics highlight the need for continual development of new antibacterial agents. Inhibitors of the biosynthesis of the amino acid lysine - an essential component of bacterial proteins and cell wall - may provide a novel class of antibiotics. This project describes investigations of the mechanism of the first two enzymes in the lysine biosynthetic pathway and the design and synthesis of inhibitors of these enzymes.Read moreRead less
The Design of New Integrase Inhibitors Targeting HIV-1. There is still no cure in sight for the worldwide HIV pandemic and the worsening viral resistance problem creates a need to find new and novel compounds for therapeutic use. This project aims to design and synthesize new anti-HIV drugs by targeting two separate enzymes within the HIV life-cycle. This 'dual-action' approach of designing a single molecular scaffold to target separate enzymes would enable a synergistic effect while minimizing ....The Design of New Integrase Inhibitors Targeting HIV-1. There is still no cure in sight for the worldwide HIV pandemic and the worsening viral resistance problem creates a need to find new and novel compounds for therapeutic use. This project aims to design and synthesize new anti-HIV drugs by targeting two separate enzymes within the HIV life-cycle. This 'dual-action' approach of designing a single molecular scaffold to target separate enzymes would enable a synergistic effect while minimizing development costs. The expected outcomes from this medicinal chemistry project include the discovery of new compounds with the potential for further development as therapeutic agents against HIV.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
Gas Phase Dynamics of a Biological Molecular Machine: Fundamentals, Stoichiometries and Stabilities. Over the last twenty years advanced molecular measurement techniques have enabled the characterization of individual biological molecules (proteins and DNA) within different types of cells and diseased tissues. This project uses a new technique that literally "weighs" groups of proteins and/or DNA to help us understand how such large molecules fit together and function within cells (sometimes ref ....Gas Phase Dynamics of a Biological Molecular Machine: Fundamentals, Stoichiometries and Stabilities. Over the last twenty years advanced molecular measurement techniques have enabled the characterization of individual biological molecules (proteins and DNA) within different types of cells and diseased tissues. This project uses a new technique that literally "weighs" groups of proteins and/or DNA to help us understand how such large molecules fit together and function within cells (sometimes referred to as molecular machinery). More detailed knowledge of processes such as those involved in copying DNA when new cells are produced will, in the long term, improve our understanding and treatment of conditions or diseases that result from errors in molecular machinery. 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