Available treatments for Alzheimer’s disease offer relatively small symptomatic benefits and more effective treatments are much needed. β-Amyloid has been implicated in the pathogenesis of Alzheimer’s disease and much attention has focussed on inhibiting two enzymes responsible for production of this peptide, the β- and γ-secretases. 
Although potent inhibitors of both enzymes have been identified, achieving robust activity in animal models and progression to clinical studies has proved more challenging. Using a high-throughput functional genomics screen, scientists at VIB and Galapagos Pharmaceuticals have now identified a constitutively expressed orphan G protein-coupled receptor, GPR3, as another modulator of β-amyloid production. GPR3 is highly expressed in areas of the brain associated with Alzheimer’s disease and levels are elevated in brain tissue from people with sporadic Alzheimer’s disease. The researchers showed that blocking GPR3 prevented accumulation of β-amyloid, both in cell culture experiments and in a mouse model of Alzheimer’s disease.
Since G protein-coupled receptors have been relatively easy to exploit as drug targets, the scientists hope that GPR3 will prove to be a promising target for the treatment of Alzheimer’s disease.
The study is published in the February 13th issue of the journal Science.
Related posts:
- How Arthritis May Protect Against Alzheimer’s Disease Epidemiological studies have suggested that either rheumatoid arthritis itself – or the anti-inflammatory drugs used to control it – are...
- Prion Protein linked to Alzheimer’s Disease Mis-folded prion proteins have been linked to a number of neurological diseases including scrapie in sheep, bovine spongiform encephalopathy (BSE,...
- New Role for APP in Alzheimer’s Disease Cleavage of amyloid precursor protein (APP) by β- and γ-secretases into neurotoxic β-amyloid peptides is believed to play a leading...
- Complement-ary Treatment for Alzheimer’s Disease? The complement system is a complex cascade of reactions forming a central component of the innate immune system which assists...
- Insulin Growth Factor Signalling in Alzheimer’s Disease Although family history and lifestyle choices play a role, ageing is recognised to be the largest single risk factor for...
Related posts brought to you by Yet Another Related Posts Plugin.
This entry was posted on Tuesday, February 17th, 2009 at 8:30 am and is filed under News. You can follow any responses to this entry through the RSS 2.0 feed. You can leave a response, or trackback from your own site.
Entries (RSS)