Navigation Links
Researchers trick Alzheimer's Enzyme

According to researchers in Scripps Research Institute, chemists have tricked an enzyme essential in Alzheimer's disease into blocking its own debilitating action.// A team led by Nobel laureate K. Barry Sharpless developed the chemical trick, called "click chemistry," to make a molecule that blocks neurotransmitter destruction caused by the brain enzyme acetylcholinesterase.

The destructive enzyme catalyzes the so-called "click reaction" that creates its own worst enemy -- its most potent inhibitor. "Think of this as a Trojan Horse approach for battling disease, but this horse goes the Greeks one better," Sharpless, W.M. Keck professor of chemistry at Scripps, said in a prepared statement.

Once the disease-causing enzyme assembles the horse, Sharpless explained, out march the inhibitors, chemical soldiers who stop the enzyme cold. By assembling its own inhibitor, the enzyme actually designs the drug that will best halts its progress.

James Olds, neuroscientist, director of the Krasnow Institute for Neurobiology at George Mason University in Fairfax, is indeed a revolutionary method in rational drug design."It may have great applicability to improving the specificity of drugs, particularly those currently used in the treatment of neurological and psychiatric diseases."

Molecular drug designers make inhibitor molecules that fit snuggly into the active sites of target enzymes, blocking their action on other molecules. Many diseases -- cancer, AIDS, Alzheimer's, arthritis and anthrax, for instance -- induce unnatural functions in enzymes. Inhibiting enzyme action can treat these diseases.

Enzyme active sites are also highly specific, so drugs react only with the sites and nowhere else. A major problem of current drugs is that they are 'dirty', that is, they have side effects -- often untoward -- because they interact with proteins or enzymes other than the ones planned for.

According to him, in additio n, Sharpless' method may have great import in designing drugs to interact with proteins for which we presently have no good compounds. The enzyme selected for the click chemistry test, acetylchonlinesterase, was one of the first brain enzymes identified. It breaks down acetylcholine, the neurotransmitter that propagates nerve signals. Inhibitors of acetylcholinesterase treat the dementia associated with Alzheimer's disease by increasing the amount of acetylcholine in the brain.

Sharpless and his team synthesized molecular building blocks that, when pieced together, create a single larger molecule with no by-products -- an acetylcholinesterase inhibitor. With the blocks in place, the essential ingredient -- the enemy enzyme itself -- goes to work. The trick active spots on the acetylcholinesterase surface act like hands that grab and orient the click components of the inhibitor, snapping them together.

Furthermore, the reaction occurs only when the pieces are held by the target enzyme -- acetylcholinesterase -- next to each other, not when they happen to bump into each other in solution.In other words, the disease-causing enzyme welds the bars of its own prison.


'"/>




Related medicine news :

1. Researchers urge caution in using ear tube surgery
2. Researchers Scale to assess the Severity of Epilepsy in Kids
3. Researchers find new HIV hiding place
4. New Hair in 15 Days Could Now Be A Possibility Say Researchers
5. Researchers developed world’s smallest toothbrus
6. Researchers discover receptor cells that can cause epilepsy
7. 15 Anti-SARS Drugs Identified By China-Europe Team of Researchers
8. Researchers reversed the process of memory loss
9. Researchers Identify Key Gene That May Help Brain Treatment
10. Researchers Discover Protein That Causes Malaria
11. Commercialization of Biotech Discoveries, An Encouragement For Researchers
Post Your Comments:
*Name:
*Comment:
*Email:


(Date:12/5/2016)... ... December 05, 2016 , ... Sabah Shah MD, MBA has joined the Retina ... of New York was founded by James M. Maisel, MD and has been providing tertiary ... has always followed a legacy of surpassing expectations amongst her peers. Growing up in ...
(Date:12/5/2016)... ... December 05, 2016 , ... ... Surgical Facial Rejuvenation" at the 2016 Anti-Aging & Beauty Awards at The ... The Aesthetic & Anti-aging Medicine European Congress (AMEC) brings together the industry’s ...
(Date:12/4/2016)... ... December 03, 2016 , ... The Lymphoma Research Foundation (LRF) ... and serving the lymphoma community through a comprehensive series of education programs, outreach ... in New York City, with long-time partners The Paul Foundation, on November 10, ...
(Date:12/4/2016)... ... 03, 2016 , ... Penrose Senior Care Auditors® was announced ... evening at the 26th Annual SMU Cox Dallas 100™ Awards Ceremony and Banquet ... for Entrepreneurship. Dallas 100™, co-founded by the Caruth Institute, honors the ingenuity, commitment ...
(Date:12/4/2016)... ... December 04, 2016 , ... Responsible dental care hinges on regular brushing of ... optimal results. This important necessity inspired an inventor from Las Vegas, Nev., to design ... that people break or avoid bad techniques of brushing the teeth in order to ...
Breaking Medicine News(10 mins):
(Date:12/5/2016)... Israel , December 5, 2016 ... identifying, in-licensing and developing promising therapeutic candidates, presents positive Phase ... BL-8040, the Company,s leading oncology platform at the ongoing 58th ... San Diego, California . ... , , ...
(Date:12/5/2016)... Taiwan , Dec. 5, 2016 ... non-inferiority to hydroxyurea (HU) in Complete Hematologic Response (CHR) ... profile of ropeginterferon alfa-2b versus HU AOP ... follow-up trial CONTINUATION-PV to obtain European marketing authorization in the ... data to the FDA as it seeks approval for commercialization ...
(Date:12/4/2016)... --  Pairnomix, LLC, a genetic research company and member ... White House, today announced that findings from its first case ... therapies for a patient with epileptic encephalopathy caused by a ... the 70 th Annual Meeting of the American ... December 2-6, 2016.  Pairnomix, unique process involves creating ...
Breaking Medicine Technology: