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DYRK1A As A Novel Target For Glioblastoma Therapies
Funder
National Health and Medical Research Council
Funding Amount
$620,294.00
Summary
Glioblastoma is a form of brain cancer that is currently incurable. We have discovered that switching-off an enzyme called DYRK1A (using ‘DYRK1A inhibitors’) kills glioblastoma cells. This therapeutic advantage is even greater when combined with drugs approved for other cancers. This project will develop new DYRK1A inhibitors and examine a novel combination treatment for glioblastoma patients. This could initiate a novel therapy that could significantly extend patients’ lives.
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.
Chemical Biology Investigation Of Cell Death Processes: Development Of Molecular Probes Interfering With Necroptosis
Funder
National Health and Medical Research Council
Funding Amount
$630,736.00
Summary
Necroptotic programmed cell death has a key role in maintaining healthy tissue, and dysregulation of this process is associated with the pathology of infection and a range of chronic inflammation diseases for which there are few satisfactory treatments. In this project, we will discover small, drug like, molecules that interfere with the necroptosis pathway. These small molecules have the potential to become new therapeutics to treat these inflammatory diseases and will be invaluable probes to s ....Necroptotic programmed cell death has a key role in maintaining healthy tissue, and dysregulation of this process is associated with the pathology of infection and a range of chronic inflammation diseases for which there are few satisfactory treatments. In this project, we will discover small, drug like, molecules that interfere with the necroptosis pathway. These small molecules have the potential to become new therapeutics to treat these inflammatory diseases and will be invaluable probes to study this key biological pathway.Read moreRead less
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.
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.
Development Of Reversible Inhibitors Of Factor XIa
Funder
National Health and Medical Research Council
Funding Amount
$444,318.00
Summary
Blood usually clots in response to injury, but unwanted clots can cause thrombosis, as well as leading to stroke and heart disease. Existing drugs to treat thrombosis suffer from drawbacks such as invasive monitoring, interaction with diet and other medicines, and bleeding complications. New drugs are clearly needed. Our expert group of researchers will discover new anti-thrombotic compounds based upon our previous identification of natural products with anticoagulant properties.
Novel TB Drug Candidates Via The Inhibition Of Lipid I Biosynthesis
Funder
National Health and Medical Research Council
Funding Amount
$780,743.00
Summary
Tuberculosis (TB) is an enormous global health problem with a continuing impact in Australia. TB is now the leading killer of any infectious disease (1.8 million people per year) and the rapid emergence of drug resistant TB infections threatens to prevent efforts to control the disease. This project seeks to develop novel TB drug candidates that operate by preventing the construction of the cell wall by the bacterial agent that causes the disease.
Development Of A Novel And Highly Selective CDK4/6 Inhibitor For Treating Cancer
Funder
National Health and Medical Research Council
Funding Amount
$1,171,199.00
Summary
We have identified and patented novel drug molecules targeting enzymes namely CDKs 4 and 6, that are important for survival of cancer cells. The drugs are highly selective and potent against CDK4/6, well absorbed orally, and have attracted much interest from a pharmaceutical company. Further detailed work is needed to characterize fully their anti-cancer effects and toxicity, thereby securing a major investment from our commercial partner for drug development for treating cancers.
Development Of Antimalarial Histone Deacetylase Inhibitors
Funder
National Health and Medical Research Council
Funding Amount
$573,676.00
Summary
Human histone deacetylases (HDACs) are enzymes clinically validated as targets for cancer chemotherapy. Different HDAC enzymes are important for survival of infectious organisms, such as protozoan Plasmodium parasites that cause malaria. This project will develop promising drug leads that kill the parasites without damaging human cells through preclinical studies in mice towards a future clinical trial for the treatment of malaria in humans.
Capturing New Drugs That Selectively Modulate PAR2 Signaling Pathways
Funder
National Health and Medical Research Council
Funding Amount
$469,088.00
Summary
Infection and tissue damage provoke acute inflammatory responses that sometimes continue unchecked, leading to different kinds of debilitating inflammatory diseases and cancers. We have discovered a new class of drugs that bind to a new target on human cells and block undesirable prolonged inflammatory responses. This project tests a new strategy to produce 'cleaner' drugs that act more selectively with fewer side effects against a new target in the treatment of arthritis and other inflammatory ....Infection and tissue damage provoke acute inflammatory responses that sometimes continue unchecked, leading to different kinds of debilitating inflammatory diseases and cancers. We have discovered a new class of drugs that bind to a new target on human cells and block undesirable prolonged inflammatory responses. This project tests a new strategy to produce 'cleaner' drugs that act more selectively with fewer side effects against a new target in the treatment of arthritis and other inflammatory diseases, diet-induced obesity and cancers.Read moreRead less