Positive Allosteric Modulation Of Metabotropic Glutamate Receptor 5; A Novel Approach For The Treatment Of Schizophrenia And Cognitive Disorders
Funder
National Health and Medical Research Council
Funding Amount
$348,428.00
Summary
The metabotropic glutamate receptor subtype 5 (mGluR5) has emerged as an exciting new target for the treatment of schizophrenia and cognitive disorders. We will investigate novel drug-binding sites on these receptors with the aim to discover new therapeutics. These studies also aim to definitively characterize mGluR5 activity following treatment with novel compounds to improve our understanding of the normal function of these important receptors.
Biased Allosteric Modulators Of Metabotropic Glutamate Receptors: Novel Therapeutic Targets For CNS Disorders
Funder
National Health and Medical Research Council
Funding Amount
$611,534.00
Summary
Metabotropic glutamate receptor 5 (mGlu5) is a major therapeutic target for depression and schizophrenia. The proposed studies will improve our understanding of how drug-like chemicals interact with mGlu5 and therefore change the activity of these receptors and in turn the activity of brain cells leading to therapeutic effectiveness. The research undertaken in this program will allow us to be smarter in developing new mGlu5 drugs that are both effective and have minimal side effects.
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.
Translating Membrane Proteins Into Therapeutics; From Bedside To Bench
Funder
National Health and Medical Research Council
Funding Amount
$9,466,000.00
Summary
Membrane proteins are the principal gatekeepers for control of cellular response, with G protein-coupled receptors (GPCRs) the largest family of cell surface proteins. These proteins are critically important for pathophysiological control, and are a major target for drug discovery. Nonetheless drug attrition due to lack of clinical efficacy remains high. We are combining cell biology, clinical management and drug discovery science to enable more effective therapeutic translation.
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.
Understanding New Drug Paradigms At M1 Muscarinic Receptors.
Funder
National Health and Medical Research Council
Funding Amount
$334,053.00
Summary
The M1 muscarinic receptor is a brain protein that plays vital roles in memory, and has been implicated in Alzheimer�s and schizophrenia. However, this protein remains poorly targeted by current medications. The current proposal will investigate the mechanisms of action of a new class of more selective M1 receptor drugs. Our studies will generate valuable information that is directly relevant to the pharmaceutical industry and academic drug discovery.
Bitopic Ligands As A Novel Approach To G-protein-coupled Receptor Selectivity
Funder
National Health and Medical Research Council
Funding Amount
$540,356.00
Summary
This project will focus on two important types of brain proteins that have been implicated in various symptoms associated with schizophrenia. The aim is to exploit a new paradigm of drug action that we have discovered, whereby novel compounds can be utilized to simultaneously target multiples sites on these brain proteins, in an effort to discover new mechanisms that can promote more selective signalling and, ultimately, can be used to design safer and more effective medicines.