Structure-based design of inhibitors of HIV-1 integrase. This project will produce compounds that block human immunodeficiency virus (HIV) replication. These compounds will benefit the 17000 Australians and more than 34 million people worldwide who are currently suffering with this terrible disease.
Developing Inhibitors Of An Essential Histidine Kinase In Staphylococcus Aureus
Funder
National Health and Medical Research Council
Funding Amount
$578,352.00
Summary
Staphylococcus aureus (Golden staph) has been termed a "superbug" because of its persistent ability to acquire resistance to a wide range of antibiotics. Once considered primarily a hospital-acquired pathogen, many patients are now being infected with antibiotic-resistant Golden staph outside of hospitals. The primary aim of this research program is to develop new antibiotics to treat antibiotic-resistant strains of Staphylococcus aureus and related pathogens.
Discovery Early Career Researcher Award - Grant ID: DE190100015
Funder
Australian Research Council
Funding Amount
$405,000.00
Summary
Global positioning system for small molecules: accelerating lead discovery. This project aims to establish a tool to accelerate lead generation from very small molecules. This will shift the paradigm in the identification of small molecules that can serve as lead compounds for the development of specific probes or drugs. This project offers a new strategy to rapidly generate lead compounds from a library of compound fragments. The new approach is expected to facilitate identification and develop ....Global positioning system for small molecules: accelerating lead discovery. This project aims to establish a tool to accelerate lead generation from very small molecules. This will shift the paradigm in the identification of small molecules that can serve as lead compounds for the development of specific probes or drugs. This project offers a new strategy to rapidly generate lead compounds from a library of compound fragments. The new approach is expected to facilitate identification and development of new lead molecules, drawing on advances made in the field of fragment-based lead discovery, which is increasingly used in the pharmaceutical industries. The tools developed can also be applied for imaging of biological processes. By developing new technologies, the project should deliver intellectual property with potential for commercialisation.Read moreRead less
Molecular Interactions with an antibiotic target in DNA replication. This project aims to develop and use new technologies to address mechanistic aspects of anti-bacterial compounds in development, and of the development of resistance to them. The project will focus on the sliding clamp subunit of the bacterial replicative polymerase by studying its association with many other proteins in vitro and in vivo, using novel techniques in solid-state NMR, single-molecule fluorescence and molecular mic ....Molecular Interactions with an antibiotic target in DNA replication. This project aims to develop and use new technologies to address mechanistic aspects of anti-bacterial compounds in development, and of the development of resistance to them. The project will focus on the sliding clamp subunit of the bacterial replicative polymerase by studying its association with many other proteins in vitro and in vivo, using novel techniques in solid-state NMR, single-molecule fluorescence and molecular microbiology. The outcomes are expected to be an increased understanding of bacterial DNA replication and mechanisms of antibiotic action and resistance. This project expects to generate new knowledge to assist in combatting antibiotic resistance in Gram-negative bacterial pathogens.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE210100139
Funder
Australian Research Council
Funding Amount
$1,240,000.00
Summary
Revitalizing facilities for nuclear magnetic resonance in South Australia. Nuclear magnetic resonance (NMR) spectroscopy is the single most powerful spectroscopic tool for determining molecular structure. Our aim is to upgrade NMR infrastructure available to researchers across South Australia with an integrated and complementary array of state-of-the-art spectrometers to diversify usage across a range of disciplines. Replacement of outdated spectrometers will modernise core NMR facilities along ....Revitalizing facilities for nuclear magnetic resonance in South Australia. Nuclear magnetic resonance (NMR) spectroscopy is the single most powerful spectroscopic tool for determining molecular structure. Our aim is to upgrade NMR infrastructure available to researchers across South Australia with an integrated and complementary array of state-of-the-art spectrometers to diversify usage across a range of disciplines. Replacement of outdated spectrometers will modernise core NMR facilities along with installation of new probes to improve sensitivity and the ability to analyze small sample quantities. Our overall strategy is to maximize capability and minimize duplication, while bringing South Australia's NMR capabilities up to a national and international standard. Read moreRead less
Australian Laureate Fellowships - Grant ID: FL150100146
Funder
Australian Research Council
Funding Amount
$2,977,310.00
Summary
Taking Australia from the farm to the pharm. Taking Australian from the farm to the pharm: This fellowship project aims to design novel drugs based on cyclic peptides that will be expressed in the seeds of plants to produce bio-pills — saving money for patients and the health care system. Plants produce unique cyclic peptides (mini-proteins) to protect themselves from pests and pathogens. This project aims to chemically redesign these peptides to produce stable protein-based pharmaceuticals that ....Taking Australia from the farm to the pharm. Taking Australian from the farm to the pharm: This fellowship project aims to design novel drugs based on cyclic peptides that will be expressed in the seeds of plants to produce bio-pills — saving money for patients and the health care system. Plants produce unique cyclic peptides (mini-proteins) to protect themselves from pests and pathogens. This project aims to chemically redesign these peptides to produce stable protein-based pharmaceuticals that can be eaten. It is hoped that these designer pharmaceuticals will be inexpensive, effective, easy to ingest and without the side effects of traditional drugs. The outcomes of this project are anticipated to be high-value drugs and agri-chemicals which will open up new high-value crops for Australian farmers and a new Australian ‘pharming’ industry.Read moreRead less
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE210100130
Funder
Australian Research Council
Funding Amount
$1,000,000.00
Summary
New Biomolecular Capabilities for the Melbourne Magnetic Resonance Facility. The project aims to integrate new instrumentation, which does not currently exist in Australia, into the Melbourne Biomolecular Nuclear Magnetic Resonance (NMR) facility. This will introduce new capabilities to the Australian NMR community to characterise important biological molecular interactions at low concentrations. This project expects to support existing areas of research strength with new approaches across inter ....New Biomolecular Capabilities for the Melbourne Magnetic Resonance Facility. The project aims to integrate new instrumentation, which does not currently exist in Australia, into the Melbourne Biomolecular Nuclear Magnetic Resonance (NMR) facility. This will introduce new capabilities to the Australian NMR community to characterise important biological molecular interactions at low concentrations. This project expects to support existing areas of research strength with new approaches across interdisciplinary research programs in biochemistry, structural biology, medicinal and natural product chemistry. Expected outcomes from a range of research with a variety of partners will underpin new, potentially commercially valuable, applications across the chemical, pharmaceutical, agricultural or manufacturing industries.Read moreRead less
Mixing the jigsaw pieces of natural products: new molecules-new properties. This project aims to examine the capacity of exploiting the bacterial biosynthetic machinery to fast-track access to analogues of natural products. Due to increased drug resistance, new reservoirs of natural products are needed for evaluation as future drugs. Desferrioxamine B will be used as a model natural product to establish the biosynthesis of new analogues in bacterial culture supplemented with unsaturated, fluorin ....Mixing the jigsaw pieces of natural products: new molecules-new properties. This project aims to examine the capacity of exploiting the bacterial biosynthetic machinery to fast-track access to analogues of natural products. Due to increased drug resistance, new reservoirs of natural products are needed for evaluation as future drugs. Desferrioxamine B will be used as a model natural product to establish the biosynthesis of new analogues in bacterial culture supplemented with unsaturated, fluorinated or deuterated building blocks. The intended outcomes are to deliver advances in methods for generating structurally diverse pools of natural products, new label-free probes, knowledge of natural product biosynthesis, and excellence in training research students in frontier methods in chemical biology and drug discovery.Read moreRead less
Improving the function of GABA-A receptors is a key property of several classes of clinically important drugs including benzodiazepines and many anticonvulsants. However, the binding sites and molecular mechanisms of these drugs remain poorly understood. Using compounds similar to those in green tea, we will determine the molecular mechanism of these drugs. This understanding will lead to the development of better drugs for treatment of anxiety, depression, epilepsy, insomnia & schizophrenia.
Discovery Early Career Researcher Award - Grant ID: DE130101650
Funder
Australian Research Council
Funding Amount
$375,000.00
Summary
Rational design of novel metal-based chaperones for tumour-selective drug delivery. This work aims to develop new drug delivery systems based on transition metal complexes for selective delivery and release of a drug in the tumour.