Epilepsy is one of the most common chronic neurological disorders; it affects 1% of the world’s population, yet about 1 in 3 patients fail to achieve seizure control with current drugs. We will improve the properties of small molecules (drugs) that specifically target the GTPase activity of the enzyme dynamin, to reduce seizure effect in the brain by a novel mechanism. We will optimize and pre-clinically test these future chemical entities as potential anti-epileptic drugs.
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.
Polymyxin-like Lipopeptide Antibiotics Of The Future
Funder
National Health and Medical Research Council
Funding Amount
$335,323.00
Summary
Polymyxins are now being clinically used as the ‘last-line’ therapy for infections caused by multidrug-resistant Gram-negative ‘superbugs’. For the first time our novel approach will interface chemistry and biology of the polymyxins with the purpose of creating a new generation of safer and more efficacious polymyxin antibiotics.
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.
Development Of Small Molecules For The Treament Of Colon Cancer
Funder
National Health and Medical Research Council
Funding Amount
$684,379.00
Summary
Colon cancer remains one of the leading causes of cancer related deaths in Australia and in the developed world. Despite improvements in prevention and therapies, there remains a considerable need for efficacious therapeutic options. We have identified a lead compound inhibiting the growth of cancer cells. We will progress this series further toward clinical trials and aim to provide patients with a new orally available molecule with potent activity against colon cancer.
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.
Development Of Small Molecule Antagonists Of HGF/SF And MET Signalling To Treat Metastatic Cancer
Funder
National Health and Medical Research Council
Funding Amount
$353,866.00
Summary
The spread of cancer throughout the body, metastasis, is the major cause of death from cancer. The MET receptor plays a crucial role in over 60% of all metastases and several approaches to block its activity are currently in clinical trials. This project will use a new approach to develop small molecule inhibitors that block the MET receptor from interacting with another protein, HGF/SF. Small molecules that block this interaction will be highly effective treatments against metastatic cancers.