Navigation Links
Scientists find new class of compounds with great potential for research and drug development
Date:5/15/2011

s. This chemical tweaking would once have been a lengthy and burdensome task, but in this case it was done using simple "click chemistry" techniques developed at Scripps Research by Nobel laureate Professor K. Barry Sharpless and his colleague Associate Professor Valery Fokin.

"We can make these modifications in just two chemical steps, which is a great advantage," said Alexander Adibekian, a postdoctoral fellow in the Cravatt lab and first author of the new paper. "And despite this technical simplicity, we were able to generate compounds that were extremely potent and selective."

From the 20 compounds the scientists generated this way, they found three with powerful and highly specific inhibitory effects on individual serine hydrolases with many unknown characteristics.

Most of the study's enzyme-inhibition tests were conducted in mouse cell cultures, a more realistic biochemical environment than traditional "test-tube" biochemical preparations; but for one of the group's inhibitor compounds, AA74-1, the scientists extended their inhibition-measurement techniques to animal models, showing that the compound potently blocked the activity of its target serine hydrolase, acyl-peptide hydrolase, or APEH, without significantly affecting other enzymes.

Not much had been known about APEH, but with its inhibitor AA74-1, the team was able to illuminate the enzyme's normal role in the chemical modification of proteins, showing the levels of more than two dozen proteins dropped sharply when APEH was inhibited.

"This was unexpected and unusual," said Adibekian. "But it's what one wants to see with these compoundsstrong enzyme-inhibiting activity in different tissues, at a low dose. And it's the first time this kind of evaluation has been done in both cultured cells and animal tissues."

The Cravatt lab is now using the expanding number of inhibitors that team members have generated so far to study serine hydrolases with pr
'/>"/>

Contact: Mika Ono
mikaono@scripps.edu
858-784-2052
Scripps Research Institute
Source:Eurekalert

Page: 1 2 3

Related biology news :

1. Jefferson scientists deliver toxic genes to effectively kill pancreatic cancer cells
2. Scientists identify novel inhibitor of human microRNA
3. Argonne scientists peer into heart of compound that may detect chemical, biological weapons
4. MU scientists go green with gold, distribute environmentally friendly nanoparticles
5. Scientists identify gene that may contribute to improved rice yield
6. Scientists discover why a mothers high-fat diet contributes to obesity in her children
7. MU scientists see how HIV matures into an infection
8. Earth scientists keep an eye on Texas
9. Thinking it through: Scientists call for policy to guide biofuels industry toward sustainability
10. Scientists identify a molecule that coordinates the movement of cells
11. Scientists Find new migratory patterns for Mediterranean and Western Atlantic bluefin tuna
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/18/2014)... X-ray crystallography and nuclear magnetic resonance imaging (NMR) to ... but such efforts have long been hampered by the ... molecule and often in ordered and crystalized form to ... peer into the structure of most molecules. , Harvard ... thing of the past. , A team of ...
(Date:4/18/2014)... Asteroid and comet impacts can cause widespread ecological havoc, ... global scales. But new research from Brown University shows ... life at the time of an impact. , A ... found fragments of leaves and preserved organic compounds lodged ... Argentina. The material could provide a snapshot of environmental ...
(Date:4/17/2014)... for chili peppers. Information about archaeological remains of ancient ... the appearance of words for chili peppers in ancient ... and highlight the value of multi-proxy data analysis. Their ... nine papers presented in a special feature issue of ... on plant and animal domestication edited by Dolores ...
Breaking Biology News(10 mins):MRI, on a molecular scale 2MRI, on a molecular scale 3Impact glass stores biodata for millions of years 2Impact glass stores biodata for millions of years 3Chickens to chili peppers 2Chickens to chili peppers 3
... team of researchers at the University of Pittsburgh has ... HIV, that could be potential treatments for drug-resistant bacterial ... agents are quite small, making them inexpensive and easy ... 2013 issue of the journal Antimicrobial Agents and ...
... A new variety of canary seeds bred specifically for human ... for people with celiac disease (CD), scientists have confirmed in ... Food Chemistry . Joyce Irene Boye and colleagues ... United States alone have CD. They develop gastrointestinal and other ...
... Agency (EMA) approved the modified adeno-associated virus AAV-LPL S447X ... in the Western world. uniQure, a Dutch biotech company, ... rare inherited metabolic disease called lipoprotein lipase deficiency (LPLD) ... million people. The disease causes severe, life-threatening inflammations of ...
Cached Biology News:HIV-derived antibacterial shows promise against drug-resistant bacteria 2No danger of cancer through gene therapy virus 2
(Date:1/15/2014)... January 15, 2014 Two champions of ... their sponsorship of an annual competition for middle and ... access to, innovative STEM study. The competition presents students ... Tests of Engineering Aptitude, Mathematics, and Sciences is ...
(Date:1/15/2014)... 2014 AudioNotch is the internet's leading ... the treatment of tinnitus. Patients listen to sound therapy ... a period of weeks to months, their tinnitus volume decreases. ... forms: Notched Music and Notched White Noise. Now, AudioNotch is ...
(Date:1/14/2014)...  3D Communications, a leading provider of strategic communications services to corporations ... in the United States and ... , JD, is returning to the firm,s Washington, D.C. ... after more than two years of service as Associate Commissioner for ...
(Date:1/14/2014)... iLab Solutions, the leader in core facility management software, today ... In this role, Michelle will work with current and potential ... development of iLab products. Her main goal will be to ... scientific community by offering the most advanced, user-friendly, and high-impact ...
Breaking Biology Technology:Technology Student Association Partners with Leaders in STEM Education Advocacy for Annual Competition 2Technology Student Association Partners with Leaders in STEM Education Advocacy for Annual Competition 3Technology Student Association Partners with Leaders in STEM Education Advocacy for Annual Competition 4Technology Student Association Partners with Leaders in STEM Education Advocacy for Annual Competition 5Former FDA Associate Commissioner Returns To 3D Communications 2iLab Solutions Announces Michelle Detwiler as the New Director of Product Strategy 2
... faculty members will explore energy from the ocean, manufacturing ... to prestigious Faculty Early Career Development (CAREER) Awards from ... million over five years, went to assistant professors Yannis ... and Wheeler Ruml of the computer science department. ...
... Calif., Feb. 21, 2012  Life Technologies Corporation (NASDAQ: ... Barclays Capital Global Healthcare Conference on Wednesday, March 14 ... Vice President and Chief Financial Officer, will present on ... presentation, which will be available for three weeks following ...
... leaders from the medical community in Europe and the U.S. ... liver disease and sepsis, and in cardiac surgery, during ... "Albumin in Clinical Fluid Management ." (Logo: ... a frank and provocative exchange about the uses and effectiveness ...
Cached Biology Technology:NSF CAREER grants support ocean energy, microforming, computer planning 2Life Technologies to Present at Barclays Capital Global Healthcare Conference 2Medical Experts Who Participated in CSL Behring's Key Issues Dialogue Prefer Albumin for Fluid Management 2Medical Experts Who Participated in CSL Behring's Key Issues Dialogue Prefer Albumin for Fluid Management 3
Human endothelial progenitor cells, For immunohistochemistry (IHC) Cell Chip with Human Peripheral Blood Dendritic Cells and EPCs...
Yeast tRNA 50 l...
Human monocyte-derived dendritic cells, For immunohistochemistry (IHC) Cell Chip with Human Peripheral Blood Dendritic Cells and EPCs...
...
Biology Products: