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.
New methodology for the manufacture of opioid pharmaceuticals and the discovery of novel opiate receptor ligands. Semi-synthetic opiates are important analgesic agents and are used in the treatment of alcohol and opiate dependence. This project will focus on the application of new, greener and more efficient methods for the preparation of these medicinal agents.
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.
Engineered Hydroxamic Acids for Zirconium-89 Positron Emission Tomography (PET) Imaging of Prostate Cancer. Positron emission tomography (PET) using a zirconium-89-ligand complex bound to a prostate-specific membrane antigen is used to detect and monitor prostate cancer. The hydroxamic acid-based ligand bound to zirconium has a high affinity towards iron, which can cause metal exchange in vivo and loss of radiotracer. The project will prepare new ligands with a higher specificity towards zirconi ....Engineered Hydroxamic Acids for Zirconium-89 Positron Emission Tomography (PET) Imaging of Prostate Cancer. Positron emission tomography (PET) using a zirconium-89-ligand complex bound to a prostate-specific membrane antigen is used to detect and monitor prostate cancer. The hydroxamic acid-based ligand bound to zirconium has a high affinity towards iron, which can cause metal exchange in vivo and loss of radiotracer. The project will prepare new ligands with a higher specificity towards zirconium over iron, and measure immuno-PET imaging activity. A second series of macrocyclic zirconium-specific ligands will be prepared to establish the relationship between variable water-lipid solubility and pharmacokinetic properties. The results will increase the capability of immuno-PET for prostate cancer detection and improve survival outcomes.Read moreRead less