Structural And Drug Discovery Studies Of Medically Important Protein Complexes
Funder
National Health and Medical Research Council
Funding Amount
$438,577.00
Summary
My research is focused on structural studies of medically important biological systems, where specific protein complex formation contributes to human illnesses. I use X-ray crystallography to visualize the whole complex at atomic resolution as well as to determine whether binding partners have undergone changes in shape upon complex formation. This structural information then helps me in drug design with goals to either disrupt or modulate the complex.
Exploitation Of Bacterial Transcription Initiation As A Target For New Antimicrobials
Funder
National Health and Medical Research Council
Funding Amount
$540,356.00
Summary
Antibiotic resistant infections from 'superbugs' are a major health problem. We will exploit information we have gathered on the machinery that copies genetic information into a message to discover chemical compounds that can be used for the development of new antibiotics with a novel mechanism of action.
Developing Drugs To Prevent Prostate Cancer Spread.
Funder
National Health and Medical Research Council
Funding Amount
$99,248.00
Summary
Current therapies for prostate cancer lose their efficacy as the cancer advances. Moreover, despite the spread of cancer being the major cause of prostate cancer mortality, there is no therapy available which selectively targets this process, thus new agents are needed. By using computer modelling to predict molecules that bind to the cell surface protein CD151 and testing these in biological assays, we aim to discover molecules that reduce cell migration of prostate cancer and that can be devel ....Current therapies for prostate cancer lose their efficacy as the cancer advances. Moreover, despite the spread of cancer being the major cause of prostate cancer mortality, there is no therapy available which selectively targets this process, thus new agents are needed. By using computer modelling to predict molecules that bind to the cell surface protein CD151 and testing these in biological assays, we aim to discover molecules that reduce cell migration of prostate cancer and that can be developed into anti-migration drugs.Read moreRead less
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.
Structural Studies Of The Jak And Abl Kinases: A Prerequisite For Drug Design
Funder
National Health and Medical Research Council
Funding Amount
$360,965.00
Summary
Protein tyrosine kinases (PTK) are a large, pivotal family of signalling molecules implicated in diseases such as cancer and immune related disorders. This fellowship aims to develop more potent kinase inhibitors of a number of PTKs using Cytopia’s drug discovery capability coupled with the X-ray crystallography expertise within Monash University. This innovative approach will permit a rational structure-based drug discovery platform to be established and will lead to the creation of a portfolio ....Protein tyrosine kinases (PTK) are a large, pivotal family of signalling molecules implicated in diseases such as cancer and immune related disorders. This fellowship aims to develop more potent kinase inhibitors of a number of PTKs using Cytopia’s drug discovery capability coupled with the X-ray crystallography expertise within Monash University. This innovative approach will permit a rational structure-based drug discovery platform to be established and will lead to the creation of a portfolio of phase I therapeutics, which will be of substantial benefit in the medical health area.Read moreRead less
Design And Delivery Of Peptide-based Anti-cancer Grb7 Inhibitors
Funder
National Health and Medical Research Council
Funding Amount
$603,126.00
Summary
The Grb7 protein is overproduced in many types of cancer cells and plays a role in cancer cell growth and spread. The current proposal builds upon the discovery of a peptide-based Grb7 inhibitor that has anti-cancer activity. This proposal is to prepare more potent inhibitor molecules that can efficiently reach the target cancer cells. Such molecules will be used for the study of Grb7 and for the development of a new Grb7-based anti-cancer drug therapy.
Dementia is the third leading cause of death in Australia and the single greatest cause of disability in the elderly. Current therapies for Alzheimer’s disease (AD), the most common form of dementia, are inadequate and fundamentally new treatment approaches are required. The aim of this proposal is to develop novel drug candidates for the treatment and prevention of AD and other neurodegenerative disorders by targeting a class of cell-surface receptors called G protein-coupled receptors (GPCRs).
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
Plasmodium Falciparum Neutral Aminopeptidases: Structure-function Analysis For The Discovery Of Anti-malarial Drugs.
Funder
National Health and Medical Research Council
Funding Amount
$634,027.00
Summary
Malaria is the world's most prevalent parasitic disease. Due to the spread of drug resistant parasites there is an urgent need to identify new anti-malaria targets and develop new drugs. We have shown that two enzymes, termed neutral aminopeptidases, are essential to the parasite's survival in the host. In this proposal we will obtain the structure of these enzymes and bring forth novel lead compounds that will form the basis of a new class of anti-malaria treatment.