Navigation Links
CSHL structural biologists reveal novel drug binding site in NMDA receptor subunit
Date:6/16/2011

Structural biologists at Cold Spring Harbor Laboratory (CSHL) have obtained a precise molecular map of the binding site for an allosteric inhibitor in a subtype of the NMDA (N-methyl-D-aspartate) receptor, which is commonly expressed in brain cells.

The newly discovered binding site -- a docking port within the receptor -- is important because it is a potential target for drugs that can modulate NMDA receptors, dysfunctions of which have been implicated in depression, schizophrenia, Parkinson's and Alzheimer's diseases as well as stroke-related brain injuries.

Allosteric sites in neurotransmitters are distinguished from their "primary" or "active" binding sites. Importantly, the newly obtained molecular map will enable scientists to design highly specific compounds that home in on the allosteric site, thereby minimizing "off-target effects," which give rise to a drug's unwanted side effects.

In a study led by CSHL Associate Professor Hiro Furukawa and published June 15 in the journal Nature, the allosteric site of interest is shown to be in the region of NMDA receptors called the amino terminal domain. A class of allosteric inhibitors for NMDA receptors, called phenylethanolamines, has previously been identified. One such compound, ifenprodil, is known to bind specifically to the GluN1/GluN2B subtype of the NMDA receptor, but not to other subtypes. The neuroprotective properties of phenylethanolamines have inspired scientists to employ them for treatment of neurological diseases and disorders. Some are now being tested in clinical trials for depression, pain, Parkinson's disease, and Alzheimer's disease.

The detailed blueprint of the allosteric site where phenylethanolamines bind to the receptor will facilitate rational design of improved compounds. In the work published on June 15th, Furukawa's group identifies the precise binding site of phenylethanolamine within the amino terminal domain of GluN1/GluN2B NMDA
'/>"/>

Contact: Peter Tarr
tarr@cshl.edu
516-367-5055
Cold Spring Harbor Laboratory
Source:Eurekalert

Page: 1 2

Related medicine news :

1. Current opinion in structural biology and DNA repair
2. Learning causes structural changes in affected neurons
3. Study finds structural brain alterations in patients with irritable bowel syndrome
4. Mount Sinai researchers find structural basis for incidence of skin cancers in a genetic disorder
5. Childhood stress such as abuse or emotional neglect can result in structural brain changes
6. Tufts biologists find another clue to the origins of degenerative diseases
7. MIT biologists pinpoint a genetic change that helps tumors move to other parts of the body
8. Biologists discover control center for sperm production
9. National Academy of Sciences honors microbiologists for major scientific contributions
10. Biologists, educators recognize excellence in evolution education
11. Caltech biologists discover microRNAs that control function of blood stem cells
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/18/2015)... Carinsurancesavings.biz has released a new blog post ... during Spring. , Spring can be a great ... make sure they compare the newest policies before deciding ... more about Spring car insurance offers by reading the ... are becoming more and more popular. Many insurance brokerage ...
(Date:4/18/2015)... April 18, 2015 Review of Ophthalmology ... a ‘Strategies for Success’ program for cataract surgeons attending ... in San Diego, where eye surgeon Jeffrey L. Martin, ... invitation-only event. Dr. Martin is the Managing Partner of ... Ophthalmology chose Dr. Martin to lead this year’s discussion ...
(Date:4/18/2015)... Raleigh, NC (PRWEB) April 18, 2015 ... the risk of developing mesothelioma later in life, but ... ways from mesothelioma that is unrelated to radiation. Surviving ... study on its website. Click here to read ... and Australia compared the cases of 45 patients who ...
(Date:4/18/2015)... York, NY (PRWEB) April 18, 2015 On ... Internal Security Threat Report , which they say, “exposes a ... how many new malware variants were introduced in 2014 - ... took for Zero Day threats to be identified and patched ... it is abundantly clear that doing business in a digital ...
(Date:4/18/2015)... (PRWEB) April 18, 2015 French physician ... on food choices when he uttered, “Tell me what ... are.” Using food to cope with stress or sadness ... Queendom.com indicates otherwise. Data collected from their ... fall victim to emotional eating, but for different reasons. ...
Breaking Medicine News(10 mins):Health News:Auto Insurance Plans Are Cheaper During Spring! 2Health News:Dr. Jeffrey Martin Invited to Share Latest Breakthroughs in Cataract Care During Roundtable Discussion at National 2015 ASCRS Meeting In San Diego 2Health News:New Study Examines Relationship Between Radiation for Hematologic Cancers and Development of Mesothelioma, According to Surviving Mesothelioma 2Health News:Cyber Attackers Continue to Fine Tune Deception and Stealth Tactics According to New Report 2Health News:Cyber Attackers Continue to Fine Tune Deception and Stealth Tactics According to New Report 3Health News:Cyber Attackers Continue to Fine Tune Deception and Stealth Tactics According to New Report 4Health News:Cyber Attackers Continue to Fine Tune Deception and Stealth Tactics According to New Report 5Health News:It’s Not Just A Girl Thing: Queendom Study Reveals That Men Struggle With Emotional Eating Too 2Health News:It’s Not Just A Girl Thing: Queendom Study Reveals That Men Struggle With Emotional Eating Too 3Health News:It’s Not Just A Girl Thing: Queendom Study Reveals That Men Struggle With Emotional Eating Too 4Health News:It’s Not Just A Girl Thing: Queendom Study Reveals That Men Struggle With Emotional Eating Too 5Health News:It’s Not Just A Girl Thing: Queendom Study Reveals That Men Struggle With Emotional Eating Too 6
... began as research into how diabetics could possibly preserve ... the vision of children afflicted with retinoblastoma. Dolores ... was researching protein kinase C gamma in the lens ... fascinating turn when she discovered a correlation between the ...
... ... of the New Video Marketing Quiz. , ... (PRWEB) March 9, 2010 -- EyeView , the world’s leading video solution provider for performance ... March 10, 2010 at 10 am ET. The Video Marketing Quiz showcases some of ...
... ... tools for monitoring apoptosis in live mammals, an important biomarker in cancer studies. , ... Madison, WI (PRWEB) March 9, 2010 ... sensitive tools for monitoring apoptosis in live mammals, an important biomarker in cancer studies. Under ...
... ... ... ... ...
... , , ... ... ... ...
... soda when the price went up, study found , TUESDAY, ... increases, people consume less of it, a new study has found. ... young adults, aged 18 to 30, beginning in 1985 to 1986 ... 10 percent increase in price was associated with a 7 percent ...
Cached Medicine News:Health News:K-State professor finds link between low oxygen levels in body and cancer-aiding protein 2Health News:EyeView Launches Innovative Video Marketing Quiz 2Health News:EyeView Launches Innovative Video Marketing Quiz 3Health News:Promega - TOP srl Agreement Enables Live Animal Imaging for Cancer Studies 2Health News:Wanted: Indianapolis Customer Service Professionals 2Health News:Wanted: Indianapolis Customer Service Professionals 3Health News:Wanted: Indianapolis Customer Service Professionals 4Health News:Wanted: Indianapolis Customer Service Professionals 5Health News:World's First 3D Dance DVD Released! 2Health News:World's First 3D Dance DVD Released! 3Health News:Cost of Junk Food May Influence Consumption 2
(Date:4/17/2015)... HILL, N.C. , April 17, 2015 /PRNewswire/ ... the creation of many new forms of provider ... Accountable Care Organizations (ACOs). The rapid evolution of ... to adapt their access, pricing and service delivery ... networks. To help the pharma sector ...
(Date:4/17/2015)... , April 17, 2015 Inivata, ... company announced today that their presence at the 2015 American ... a presentation by co-founder Nitzan Rosenfeld and a ... attending April 18 th - 22 nd . ... plasma using ctDNA , forms part of a ...
(Date:4/17/2015)... 17, 2015 Research and Markets ( ... "ADME-Toxicology Testing - Global Strategic Business Report" report ... worldwide markets for ADME-Toxicology Testing in US$ Million by ... ADME Testing. The report provides separate comprehensive ... Japan , Europe ...
Breaking Medicine Technology:Pharmaceutical Industry Struggling to Better Serve Provider Networks Such as Accountable Care Organizations (ACOs) 2Inivata Co-founder Nitzan Rosenfeld to Present at AACR Annual Meeting 2ADME-Toxicology Testing (In-Vivo, & In-Vitro) Market - Global Strategic Business Report 2015: Pharma Industry Renews Focus on Cost Optimization 2
... with Teplizumab Manufactured at ... MacroGenics, ROCKVILLE, ... actively enrolling adults and children ages,8 to 35 with recent-onset type 1 ... of three teplizumab dosing,regimens administered at the start of the study and ...
... and Oncomine Concepts Map Integral in Expression and Association ... ... Building on an earlier study,that used Oncomine(TM) to identify ETS-fusion proteins in ... of,four additional classes of ETS rearrangements in prostate cancer, each of,which activates ...
Cached Medicine Technology:MacroGenics Begins Global Phase 2/3 Protege Study in Recent-onset Type 1 Diabetes Mellitus 2MacroGenics Begins Global Phase 2/3 Protege Study in Recent-onset Type 1 Diabetes Mellitus 3MacroGenics Begins Global Phase 2/3 Protege Study in Recent-onset Type 1 Diabetes Mellitus 4Gene Fusion Subtypes in Prostate Carcinoma Have Clinical Implications 2
... a national reference laboratory and a worldwide ... ARUP offers an extensive test menu of ... clinical and anatomic pathology. Owned by the ... more than half of the nation's university ...
... is a national reference laboratory and a ... development. ARUP offers an extensive test menu ... in clinical and anatomic pathology. Owned by ... include more than half of the nation's ...
... is a national reference laboratory and a ... development. ARUP offers an extensive test menu ... in clinical and anatomic pathology. Owned by ... include more than half of the nation's ...
... reference laboratory and a worldwide leader in ... an extensive test menu of highly complex ... anatomic pathology. Owned by the University of ... half of the nation's university teaching hospitals ...
Medicine Products: