Development Of Fragment Hits Into Effective Antimalarials; Targeting Malaria Eradication
Funder
National Health and Medical Research Council
Funding Amount
$676,798.00
Summary
We have used a novel method that samples the diversity of natural products with a small sub-set of compounds, and observed direct interaction between these compounds and proteins important in the malaria parasite life cycle. This project will develop these identified active compounds towards the goal of producing a drug to fight stages of the malaria parasite’s life cycle that are not targeted by currently available antimalarial drugs.
Discovery Of New And Better Treatments For Human African Trypanosomiasis
Funder
National Health and Medical Research Council
Funding Amount
$837,615.00
Summary
Sleeping sickness, or human African trypanosomiasis, is present in 36 countries where there are 60 million people at risk of infection, with 50,000-70,000 new cases and 48,000 deaths per annum. Transmitted by the bite of the tsetse fly, this disease is caused by the protozoan parasite Trypanosoma brucei, and without treatment, death is inevitable. We have discovered some compounds that weakly inhibit T.brucei and the aim of this project is to make them potent enough to become drug candidates.
Small Molecule Therapeutics: From Infectious And Parasitic Diseases To Cancers
Funder
National Health and Medical Research Council
Funding Amount
$763,845.00
Summary
I will lead a team of medicinal chemists to discover better treatments of diseases focused in two major domains. On one hand, I will discover new drugs to treat certain parasitic diseases such as Sleeping Sickness, Chagas disease and malaria, all caused by protozoal parasites. On the other hand, I will discover new drugs to treat certain cancers, in particular acute myeloid leukemia and Burkitt’s lymphoma, caused by dysfunction of certain types of enzymes called histone acetyltransferases.
Development Of Small Molecule Modulators Of Apoptosis
Funder
National Health and Medical Research Council
Funding Amount
$621,558.00
Summary
Cancers rely on the deregulation of key cellular pathways. Along with biological and genetic tools, small molecules are powerful probes to understand these mechanisms. During the course of this research program, we will develop new and drug-like molecules that reinstate the cell death process to combat malignancies. This research will bring important advances for potential chemotherapies and create probes to better understand the biology of programmed cell death processes.
Non-Haemolytic Friulimicins For The Treatment Of Multi-Drug Resistant Bacteria
Funder
National Health and Medical Research Council
Funding Amount
$552,572.00
Summary
We are developing a new antibiotic, called friulimicin, to combat the ïsuperbugsÍ that cause serious infections in hospitals and the community. We will optimize the drug to target MRSA (methicillin resistant Staphylococcus aureus) VRE (vancomycin resistant enterococci) and DRSP (drug resistant Streptococcus pneumoniae). We will also investigate how the drug can be used for treatment of lung infections such as pneumonia, where the antibiotic can work much better than existing drugs against resist ....We are developing a new antibiotic, called friulimicin, to combat the ïsuperbugsÍ that cause serious infections in hospitals and the community. We will optimize the drug to target MRSA (methicillin resistant Staphylococcus aureus) VRE (vancomycin resistant enterococci) and DRSP (drug resistant Streptococcus pneumoniae). We will also investigate how the drug can be used for treatment of lung infections such as pneumonia, where the antibiotic can work much better than existing drugs against resistant bacteria.Read moreRead less
Isoform Selective PI3 Kinase Inhibitors For Cancer, Thrombosis And Inflammatory Disease
Funder
National Health and Medical Research Council
Funding Amount
$474,473.00
Summary
Inhibitors of the PI3 kinase family of enzymes have potential as therapeutics in diseases such as cancer, thrombosis and inflammatory disease. In this project the investigators will develop a new class of PI3 kinase inhibitors they have discovered, optimizing their pharmaceutical properties and evaluating them in models of disease. The aim is to develop a candidate for human clinical studies.
MEDICINAL CHEMISTRY LED DISCOVERY OF NEW TREATMENTS FOR HUMAN AFRICAN TRYPANOSOMIASIS AND BETA-THALASSEMIA
Funder
National Health and Medical Research Council
Funding Amount
$636,524.00
Summary
I am a medicinal chemist interested in finding new treatments for sleeping sickness, a parasitic disease, and the blood diseases sickle cell anaemia and beta-thalassemia. After testing more than 80,000 compounds, we have discovered some promising starting points for drug discovery. These so-called “screening hits” are too weak to be useful but I hope to use my medicinal chemistry expertise to make these more potent, more selective, and hence therapeutically useful.
Chronic pain is a significant global health, economic and social problem, with the annual economic burden estimated at approximately $40 billion in Australia. My research will focus on the discovery and structure-function of venom peptides (trivially called toxins) from cone snails and spiders plus other Australian venomous creatures that modulate sodium and calcium channels in peripheral pain and associated pathways and optimise these for clinical development.
Lipopeptide Antibiotics For XDR Gram-negative Infections
Funder
National Health and Medical Research Council
Funding Amount
$994,897.00
Summary
The polymyxins are a drug class considered to be a last-resort treatment option for multidrug-resistant (MDR) and extremely drug resistant (XDR) Gram-negative infections. Unfortunately resistance is rapidly developing against these antibiotics, leaving no effective therapies and resulting in patient death. This project aims to develop an antibiotic with superior spectra of action and improved safety profiles compared to the polymyxins, with activity against polymyxin-resistant bacteria.
Unique And Selective Small Molecules To Dissect Histone Acetyltransferase Biology
Funder
National Health and Medical Research Council
Funding Amount
$694,255.00
Summary
A class of enzymes called histone acetyltransferases appear to be important in a variety of diseases, from inflammation to cancer. We are developing potent and selective compounds that will be able to tell us which of these enzymes may be targets for cancer, and which for inflammatory disorders. This will be invaluable for better treatment of debilitating human diseases with unmet needs.