Factors Regulating The Temporal And Spatial Assembly Of G-protein Coupled Receptor-mediated Arrestin Complexes
Funder
National Health and Medical Research Council
Funding Amount
$472,770.00
Summary
G-protein coupled receptors are proteins that are present at the surface of most cells in the human body. They recognise and bind to specific molecules, such as hormones, the act of which results in a specific signal being transmitted into the cell. This signal alters the function of the cell and so it is critical that it is appropriate, both in type and duration. G-protein coupled receptors and the molecules that activate them provide an essential function within the human body for communicatin ....G-protein coupled receptors are proteins that are present at the surface of most cells in the human body. They recognise and bind to specific molecules, such as hormones, the act of which results in a specific signal being transmitted into the cell. This signal alters the function of the cell and so it is critical that it is appropriate, both in type and duration. G-protein coupled receptors and the molecules that activate them provide an essential function within the human body for communicating between cells, and consequently between organs. They are a major mechanism by which nerve signals are transmitted and hormones regulate bodily functions. They are therefore an important target for pharmaceuticals, with up to 50% of ethical drugs and many drugs of abuse acting upon them. It is critical to understand how these receptors alter cellular function once they receive an appropriate signal, but it is also essential to know how such responses are switched off. Arrestins are proteins within cells that interact with G-protein coupled receptors to 'arrest' their signalling. They desensitise the cell to continuous stimulation, but also act to resensitise the cell to respond to future, separate signals. Recently, they have also been shown to provide alternative mechanisms of altering cellular activity by interacting with other cellular proteins. These interactions greatly increase the potential ways in which a cell can respond once a G-protein coupled receptor is activated. Understanding the resulting complexity is essential if we are to fully exploit the vast therapeutic potential of this important receptor family.Read moreRead less
Novel Approaches To The Targeting Of GPCRs Towards Improved Treatment Of Schizophrenia
Funder
National Health and Medical Research Council
Funding Amount
$415,218.00
Summary
The focus of these studies are two important types of brain proteins that have been implicated in various symptoms associated with schizophrenia. The aim is to exploit two emerging paradigms of drug action at these brain proteins that will allow us to target them in a more selective manner. In particular, these studies will provide a starting point for safer, more effective treatments for schizophrenia.
A Breakdown Of Cortical Homeostasis In Depression: A Focus On The Anterior Cingulate
Funder
National Health and Medical Research Council
Funding Amount
$625,629.00
Summary
Major depressive disorders affect 20% of the Australian population. Some symptoms of major depressive disorders arise because of a dysfunction of the human brain, particularly the cortex. Our studies show there are biochemical changes in the anterior cingulate cortex in people with mood disorders. We will now extend our studies to show there is a breakdown in the balance between neurotransmitter and neuroinflammation pathways in the anterior cingulate cortex in major depressive disorders.
Rational Co-targeting Of G Protein-coupled Receptors As A Novel Approach Towards Treating Neuropsychiatric Disorders
Funder
National Health and Medical Research Council
Funding Amount
$620,399.00
Summary
Schizophrenia is a common mental disorder with multiple symptoms. Current therapeutics only treat some of these symptoms. This project will focus on two important brain proteins implicated in schizophrenia. With the hypothesis that the rational targeting of these two proteins will lead to the design of more effective medicines for treatment of schizophrenia we will develop novel methods to selectively and simultaneously and target these two proteins.