Linkage Infrastructure, Equipment And Facilities - Grant ID: LE120100170
Funder
Australian Research Council
Funding Amount
$580,000.00
Summary
Bioaffinity mass spectrometry infrastructure to identify small molecules binding to therapeutic targets. The development of anti-infective therapies is challenging because the underlying biology and biochemistry of pathogen virulence is not yet completely understood. This mass spectrometer facility will be used to identify small molecules suited for development into new therapies for malaria, tuberculosis and HIV.
Development of small molecule primary sulfonamides as new drugs for malaria. Malaria is a major global health threat, causing approximately 800,000 deaths annually. Lives can be saved if patients are treated. The use of current antimalarial drugs is limited by drug resistance, low activity and poor safety. This project investigates the effectiveness of a new class of molecule as a safe drug treatment option to kill malaria parasites.
Understanding allosteric modulation and functional selectivity at G Protein-Coupled Receptors (GPCRs). GPCRs are an important superfamily of proteins that are involved in a myriad of physiological processes and a wide range of serious illnesses. This project seeks to gain a more detailed understanding of new mechanisms of GPCR modulation and function that will be of direct relevance to drug discovery.
Movement of mitochondria between cells. This project aims to characterise how mitochondria move between cells into grafted cells with dysfunctional mitochondrial function. How mitochondria reach the acceptor cell and how they move from the donor cell is not known. The project will use a 'bottom-up' approach, starting from a reconstituted system, via in vitro, co-culture stage to a relevant biological model, increasing complexity and biological relevance. It will document that the process of mito ....Movement of mitochondria between cells. This project aims to characterise how mitochondria move between cells into grafted cells with dysfunctional mitochondrial function. How mitochondria reach the acceptor cell and how they move from the donor cell is not known. The project will use a 'bottom-up' approach, starting from a reconstituted system, via in vitro, co-culture stage to a relevant biological model, increasing complexity and biological relevance. It will document that the process of mitochondrial intercellular movement is dependent on intercellular bridges and a specific mobility system. The project is of high relevance for cell biology.Read moreRead less
Subtype selectivity and functional bias of receptor positive allosteric modulators for understanding models of pulmonary disease. G-protein-coupled receptors (GPCRs) are an important superfamily of proteins that are involved in a myriad of physiological processes and a wide range of serious illnesses. This project seeks to gain a more detailed understanding of new mechanisms of GPCR modulation and function that will be of direct relevance to drug discovery.
Innovations in peptide-based drug design. This project will aim to develop new types of drugs that fill a gap between existing small molecule drugs, which are relatively inexpensive and stable, but often have side-effects, and biologics which are very expensive and require injection. Our new generation of peptide-based drugs promise to be applicable to diseases that are not treatable by current drugs.
Fragment based screening to deliver drugs targeting tuberculosis and the gametocyte and liver stages of Plasmodium. This project will identify natural products that bind to critical proteins in malaria and tuberculosis to discover new ways to treat these diseases.
Engineered extrasynaptic GABAA receptors: Towards novel analgesics. Engineered extrasynaptic GABAA receptors: Towards novel analgesics. This project intends to alleviate neuropathic pain by developing drugs and good tool molecules targeting GABA-A receptors. About 20% of Australian adults suffer from neuropathic pain. Delta-containing GABA-A receptors represent attractive and novel targets for developing non-opioid analgesics. However, no drugs or good tool molecules target these receptors. This ....Engineered extrasynaptic GABAA receptors: Towards novel analgesics. Engineered extrasynaptic GABAA receptors: Towards novel analgesics. This project intends to alleviate neuropathic pain by developing drugs and good tool molecules targeting GABA-A receptors. About 20% of Australian adults suffer from neuropathic pain. Delta-containing GABA-A receptors represent attractive and novel targets for developing non-opioid analgesics. However, no drugs or good tool molecules target these receptors. This project intends to develop the needed enabling technologies, including screening assays, tool molecules and radioligands; and perform brain slice electrophysiology to confirm activity in neuronal cells. This project is expected to benefit the research community and future rational drug-discovery endeavours for drugs that modulate delta-containing receptors.Read moreRead less
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