Development Of Peptide-based Scaffolds For Intracellular Cancer Targets
Funder
National Health and Medical Research Council
Funding Amount
$1,479,836.00
Summary
The overall aim of this project is to develop peptide-based drugs that are able to cross cell membranes and inhibit specific targets inside cells leading to more effective, safer and cost effective drugs for cancer. One potential outcome of the project will be new drug leads to treat melanoma and leukemia that are likely to be less toxic, more potent and less likely to develop resistance than current treatments.
The Molecular Basis Of Cytochrome P450 Ligand Binding: Towards Predicting Enzyme Substrate Selectivity And Drug-drug Interaction Potential
Funder
National Health and Medical Research Council
Funding Amount
$558,447.00
Summary
Cytochrome P450 (CYP) enzymes play a pivotal role in the metabolism (i.e. chemical breakdown) of drugs, a process that is essential for their detoxification and elimination from the body. This project will combine advanced computational and experimental approaches to elucidate the molecular basis for the binding of drugs to CYP enzymes, which is crucial for the design of drugs with favourable metabolic properties and decreased propensity for harmful interactions with co-administered drugs.
We aim to develop a new class of cholesterol-lowering drugs by blocking the interaction between a protein in the blood called PCSK9 and its receptor, which is implicated in cholesterol absorption. We will do this by designing small stable peptides (mini proteins) that mimic part of the receptor and have the potential to interfere with the normal PCSK9 binding process. These drugs should be less expensive and potentially less immunogenic than competing therapies based on antibodies.
Structure-based Design Of Inhibitors Of PimA - A New Target For Tuberculosis Therapy
Funder
National Health and Medical Research Council
Funding Amount
$666,246.00
Summary
Tuberculosis (TB) is a devastating disease that kills 2 million people worldwide each year and affects one-third of the entire human population. Bacterial resistance to existing antibiotics is an ever increasing problem, highlighting the need to develop new anti-TB drugs. The aim of this project is to develop specific inhibitors to target a protein that is essential for the survival of the tuberculosis bacterium.
Targeting Nucleic Acid Synthesis And Cell Division In Gram-negative Bacterial Pathogens
Funder
National Health and Medical Research Council
Funding Amount
$966,800.00
Summary
Some bacteria like Acinetobacter species cause infections in hospitals that are difficult to treat because they have acquired resistance to most antibiotics. This project will combine the complementary expertise of five research groups to develop knowledge of, and how to block, three essential processes in these worrying pathogenic species: copying of DNA, RNA synthesis, and cell division. This promises to lead to development of new antibacterial therapies.
A number of Leukemias, lymphomas and other blood malignancies are caused by mutations in a protein called JAK (Janus Kinase). To combat this human cells produce a protein that inhibits JAK (called SOCS). We aim to study how this process works and to mimic SOCS with a drug in order to treat leukemia.
Targeting The Plasmodium Falciparum Metalloaminopeptidases For Development Of New Antimalarial Agents
Funder
National Health and Medical Research Council
Funding Amount
$565,507.00
Summary
Each year 1-2 million people will die from malaria. The prevention and treatment of malaria is becoming increasingly difficult due to the spread of drug-resistance. There is an urgent need for next generation of antimalarials with new modes of action. This project will develop new antimalarial agents against the malarial aminopeptidase drug targets.
New Positive Allosteric Modulators Of Nicotinic Acetylcholine Receptors For Treatment Of Cognitive Impairment In ADHD
Funder
National Health and Medical Research Council
Funding Amount
$612,851.00
Summary
The effects of Attention Deficit Hyperactivity Disorder (ADHD) can extend well beyond childhood. This project will target the nicotinic acetylcholine receptor family for developing new therapeutics to manage this disease.
Antibiotic resistance is a looming public health crisis. New antibiotics with new mechanisms of action are desperately needed. The long-term goal of this research is to develop new drugs that disarm bacteria to overcome the problem of antibiotic resistance.
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.