Allosteric regulation of G protein-coupled receptors

Funding Activity

Website
http://purl.org/au-research/grants/nhmrc/400134

Funding Status
Closed

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Funded Activity Summary

The normal function of all living cells depends on how they respond to the multitude of physical and chemical stimuli to which they are constantly exposed. The majority of these stimuli acting on cells do so not by directly entering the cells, but rather by acting on specific types of receiver proteins on the cell's surface that are called receptors. The most important family of cell-surface receptors transmit their message to the inside of the cell by coupling to yet another type of protein known as a G protein, and are therefore commonly referred to as G protein-coupled receptors (or GPCRs). Aberrations in the normal function of these GPCRs have been implicated in a wide variety of disorders, including neuropsychiatric conditions, endocrine disorders, cardiovascular disease and many cancers. To date, the majority of drugs acting at GPCRs do so by binding to specific regions on these receptors. Although many breakthroughs in disease treatment have been achieved using this approach, there remain a number of acknowledged limitations, including lack of drug selectivity, toxicity and reduced responsiveness with prolonged therapy. Our current proposal focuses on targeting drugs to alternative regions of GPCRs that may overcome many of the limitations associated with current drug therapies. An understanding of the properties of these alternative drug binding sites, which will be investigated in our current grant, can lead to more effective treatments for a variety of diseases.

Funded Activity Details

Start Date: 01-01-2006

End Date: 01-01-2008

Funding Scheme: NHMRC Project Grants

Funding Amount: $509,017.00

Funder: National Health and Medical Research Council

Research Topics

ANZSRC Field of Research (FoR)

Pharmacology and Pharmaceutical Sciences

ANZSRC Socio-Economic Objective (SEO)

There are no SEO codes available for this funding activity

Other Keywords

Dementia | G protein-coupled receptors | Molecular pharmacology | Muscarinic receptors | Neuromodulation | Pain | Parkinson's Disease | Schizophrenia | Signal transduction

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