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Professor Michael Parker from St Vincent’s Institute in Melbourne is one of Australia’s leading structural biologists. He will use his Fellowship to help establish a Cancer Structural Biology Centre to provide early stage drug discovery tools which will aid many of Australia’s leading cancer researchers to translate their basic discoveries into drugs. This work will utilise key major infrastructure investments including the Australian Synchrotron.
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.
Research Fellowship: Understanding G Protein-coupled Receptors (GPCRs)
Funder
National Health and Medical Research Council
Funding Amount
$444,177.00
Summary
This project focuses on drug action at G protein-coupled receptors (GPCRs), the largest class of drug targets. It builds on key discoveries by the applicant that novel sites on GPCRs can be targeted by small molecules in a selective manner, thus minimizing side effects and maximizing therapeutic efficacy. Because this approach can work across most GPCR families, the relevance to the pharmaceutical industry and GPCR-related diseases, such as schizophrenia and diabetes, is very high.
G protein-coupled receptors are proteins that exist on every human cell, where they sense, and respond to environmental stimuli. Because of their importance they are targeted by drugs to treat many diseases. However little is known about how drugs activate these receptors and this has hindered new drug development. I use state-of-the-art technology to determine how drugs activate receptors and develop new methods for drug discovery. This work will have major impact on the Pharmaceutical industry
Structural Biology And Therapeutic Targeting Of Proteins Involved In Infection And Immunity
Funder
National Health and Medical Research Council
Funding Amount
$753,300.00
Summary
Structural biology plays an essential role in uncovering how proteins function at the molecular level, and further facilitates strategies to develop therapeutics targeting the diseases these proteins are involved in. In the proposed work, I will focus on bacterial virulence factors, to develop new antibiotics and vaccination strategies, and proteins involved in innate immunity pathways, to develop therapeutics against a number of associated disorders including chronic inflammatory diseases.
This research draws together my expertise in medicinal chemistry, biochemistry, pharmacology and virology to design and develop new compounds that we can use to interrogate and regulate human and viral proteins that cause disease. Protein, cell and animal studies relevant to major 21st century health burdens (such as inflammatory, infectious and metabolic diseases, cancer, pain and viral infections) will provide important new information on mechanisms of disease development and drug action.
Peptides (mini proteins) have outstanding potential as new drugs for cancer, pain and many other diseases, but their potential has not been realised so far because peptides tend to be unstable in the body. I have discovered a new class of peptides that are ultra-stable and have very favourable pharmaceutical properties. I will use these peptides to develop a new generation of drugs that are more potent and with fewer side effects than traditional drugs.
Modulating Protein-Protein Interactions In Disease
Funder
National Health and Medical Research Council
Funding Amount
$863,910.00
Summary
Most diseases are driven by protein-protein interactions often with few/no greasy pockets to fit small molecule drugs. Innovative approaches to new drugs are needed for these proteins. This project combines chemistry, biochemistry and pharmacology to create new drug leads, new knowledge on drug action and disease development at gene, protein, cell, animal levels, and aims to trial new drug leads in preclinical and eventually clinical tests in inflammatory and metabolic diseases, pain and cancer.
A common characteristic of cancer is the failure of cells to die when they normally would. One of the problems with many cancer therapies is that they rely on the integrity of signalling pathways to the normal ‘death machinery’ of the cell to do their job. By understanding how the molecular death machine operates we are fashioning new drugs that can target it directly, thus bypassing the very pathways that are so frequently disrupted in tumour cells.
Inhibitory Neurotransmitter Receptors As Therapeutic Targets For Chronic Pain And Anxiety Disorders
Funder
National Health and Medical Research Council
Funding Amount
$763,409.00
Summary
There are currently few effective long-term treatments for chronic pain and anxiety disorders. Here we propose to develop innovative therapies for both of these debilitating neurological disorders. In addition, we plan to improve our current understanding of how these disorders occur in the first place. This may identify novel potential therapeutic strategies for treating pain, anxiety and a host of other neurological disorders.