Integrated Approaches To Targeting G Protein-coupled Receptors: Translational Studies Of Novel Drug-receptor Paradigms
Funder
National Health and Medical Research Council
Funding Amount
$851,980.00
Summary
This Fellowship focuses on one of the largest family of proteins found in the human body, the so-called ‘G protein-coupled receptors ‘ (GPCRs). GPCRs control how each of our cells communicates with one another, and have been implicated in virtually all diseases. This proposal will study new mechanisms of targeting drugs to GPCRs that can overcome current drug discovery bottlenecks and lead to new ways of treating neuropsychiatric, cardiovascular, inflammatory and metabolic diseases.
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.
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.
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
Relaxin family peptides are small proteins that have numerous essential biological roles in the vascular system, brain and gut. The hormone relaxin is currently in Phase III clinical trials to treat heart failure and the other peptides show great potential as drugs to treat diseases including mental illnesses and obesity. My research focuses on developing drugs targeting the receptors for these important peptide systems and understanding how these drugs can be best used therapeutically
G Protein-Coupled Receptors (GPCRs) form the largest family of receptors and drug targets in living organisms. Currently, the major reason that new drugs fail to reach the clinic is lack of appropriate drug effect (approx. 30%). Thus, we need a better understanding of how GPCRs work and how this relates to disease. Work within my fellowship will address this knowledge gap, using GPCR models that are relevant to treatment of metabolic, inflammatory, cardiovascular and central nervous system disea ....G Protein-Coupled Receptors (GPCRs) form the largest family of receptors and drug targets in living organisms. Currently, the major reason that new drugs fail to reach the clinic is lack of appropriate drug effect (approx. 30%). Thus, we need a better understanding of how GPCRs work and how this relates to disease. Work within my fellowship will address this knowledge gap, using GPCR models that are relevant to treatment of metabolic, inflammatory, cardiovascular and central nervous system disease.Read moreRead less
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.
Mechanisms Of Gene Regulation - Structure, Function And Design
Funder
National Health and Medical Research Council
Funding Amount
$697,209.00
Summary
The human genome contains at least 20000 genes. The activity of these genes must be tightly controlled throughout an individual’s life and problems with the regulation of genes lie at the heart of many common and serious diseases, including most forms of cancer. My program of research is focused on understanding the mechanisms underlying gene regulation and on the design of new reagents that could be used to manipulate the activity of genes that behave aberrantly in disease states.
I am a biochemist focussed on understanding how the structures of proteins determine their functions. I intend to apply this understanding to medically relevant questions by working collaboratively and using a range of complementary structural, computational and cell biology techniques. In particular, I will focus on proteins involved in infection and immunity, to understand how they work, and contribute to the development of drugs and vaccines.
Sphingosine Kinase As A Target For Anti-cancer Therapy
Funder
National Health and Medical Research Council
Funding Amount
$590,785.00
Summary
Sphingosine kinase is a protein involved in the development and progression of numerous types of solid tumors and leukaemias. We have recently made a major break-through by identifing how the cancer-inducing activity of sphingosine kinase is controlled. In this study we will target these control mechanisms to develop potential new anti-cancer therapies.