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:2/8/2016)... ... February 08, 2016 , ... Discover the Rocky Mountain ... 1,400 booths and 700 companies. Attendees also get to see the most incredible ... Garden & Home Show , at the Colorado Convention Center - 700 14th St. ...
(Date:2/8/2016)... ... February 08, 2016 , ... Joshua Rosenthal, PhD, Chief Scientific ... can use newly released government data on populations and physicians to better calculate ... capture the value they create to succeed in new economic models for value ...
(Date:2/7/2016)... Michigan (PRWEB) , ... February 07, 2016 , ... ... organ prolapse with the latest techniques and the most minimally invasive approaches. , ... organ prolapse, particularly after menopause. Other risk factors include surgery to the pelvic ...
(Date:2/6/2016)... ... February 06, 2016 , ... ... NURSES EXPECTED AT AORN SURGICAL CONFERENCE & EXPO , WHAT:     , This ... an estimated 5000 perioperative nurses in attendance to study the latest evidence-based ...
(Date:2/6/2016)... ... February 06, 2016 , ... Research has shown that building ... the frequency and level of relapse. , At the 2016 iaedp ... will explore the critical tasks of the recovery phase and beyond including relapse ...
Breaking Medicine News(10 mins):
(Date:2/8/2016)... 8, 2016   GS1 US will hold ... them through GS1 Standards implementation to address the requirements ... Device Identification (UDI) rule. Scott Brown ... Gibson , senior director industry development, medical devices, GS1 ... GS1 US --> Scott Brown ...
(Date:2/8/2016)... Pa. , Feb. 8, 2016   ... November Research Group (NRG),s pharmacovigilance technology services ... system-related consulting services and an Oracle Argus Specialized ... services to Life Sciences companies. ... and expands HighPoint,s life sciences capabilities and provides ...
(Date:2/8/2016)... , Switzerland and PALO ALTO, Calif. ... in biological and chemical manufacturing, and Kodiak Sciences Inc., ... the treatment of retinal disease, announced today agreements for ... agreement, Lonza will manufacture material at multiple sites, including ... --> --> Retinal diseases, ...
Breaking Medicine Technology: