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:12/10/2014)... California , December 9, 2014 ... with ITN,s BCARD Platform   ... cloud-based enterprise meeting scheduling solutions for business-to-business (B2B) ... the world leader in mobile near-field communication (NFC), ...      (Logo: http://photos.prnewswire.com/prnh/20140612/691055) , ...
(Date:12/4/2014)... PALM BEACH GARDENS, Fla. , Dec. 3, ... identity management solutions, today announced that its DigitalPersona ... 4500 fingerprint readers have been deployed throughout ... Carolina , South Carolina ... network headquartered in Southern Pines, North ...
(Date:11/21/2014)... According to a new market research report ... Control, Intrusion Detection, Parking Management, Under Vehicle Inspection), End ... - Global Forecasts to 2020", published by MarketsandMarkets, The ... $25 Billion in 2014 and is expected to reach ... 8.69%. Browse 116 market data Tables and ...
Breaking Biology News(10 mins):Jifflenow And ITN International Bring Cutting-Edge Badge Scanning Technology To B2B Events 2Jifflenow And ITN International Bring Cutting-Edge Badge Scanning Technology To B2B Events 3First Bank Partners with Crossmatch to Increase Log In Security 2First Bank Partners with Crossmatch to Increase Log In Security 3Industrial Security Systems Market Worth $38 Billion by 2020 2Industrial Security Systems Market Worth $38 Billion by 2020 3
... This news release is available in German . ... is made up of a highly concentrated protein solution that imparts ... content the ocular lens must remain clear and transparent. To this ... thrown overboard the complex machinery present in all other cells of ...
... study led by scientists at the University of Miami (UM) ... complex circulation from the Mississippi River plume played a substantial ... the 2010 Deepwater Horizon incident. These findings provide new information ... Gulf of Mexico. The research, published in the Oct. 2013 ...
... use in vaccines and cancer medicines, enzymes for the ... already be produced on a large scale using biotechnology. ... making use of living cells or organisms. This involves ... protein to bacteria, yeasts, or cultures of animal or ...
Cached Biology News:A protein safeguards against cataracts 2A protein safeguards against cataracts 3New research illustrates Mississippi River's role 2Biomolecules for the production line 2Biomolecules for the production line 3
(Date:12/19/2014)... , Dec. 18, 2014  Decision Resources Group ... dental biomaterial market will grow moderately through 2023 as ... and growing awareness of dental biomaterials all spur procedure ... such as China and ... bring dental procedures within reach for a larger proportion ...
(Date:12/19/2014)... YORK , Dec. 18, 2014 Relmada ... therapies for the treatment of chronic pain, announced the ... today. "This was a transformational year in ... promising future for our company," said Sergio Traversa ... year, we have executed on key financial, human resource ...
(Date:12/17/2014)... “Never say, ‘I cannot do ... Department of Physics, advises young women pursuing careers ... SPIE Women in Optics 18-month planner ... ask questions.” , In the annual planner, women ... ranging from university professor and laboratory researcher to ...
(Date:12/17/2014)... CA (PRWEB) December 17, 2014 Once ... to provide a larger packaged waste water treatment plant ... King Abdullah Economic City (KAEC). Two years ago Bioshaft ... Jeddah Gate Development, serving two residential towers with an ... is over a quarter million gallons per day and ...
Breaking Biology Technology:Asia Pacific Dental Biomaterial Market Will Grow Strongly Through 2023 2Asia Pacific Dental Biomaterial Market Will Grow Strongly Through 2023 3Relmada Therapeutics Announces Results of Annual Shareholders Meeting 2Network, Multitask, Persevere: SPIE Women in Optics Planner Subjects Share from Experience 2Network, Multitask, Persevere: SPIE Women in Optics Planner Subjects Share from Experience 3
... , ... that the European Investment Fund (EIF) has entered into ... be,managed by Karolinska Development and used to invest in ... EIF,has agreed to invest 26.7 M Euros in the ...
... ... a free webinar, “The Role of Process Analytical Technology (PAT) in Green Chemistry and ... ... of Process Analytical Technology (PAT) in Green Chemistry and Green Engineering Webinar on ...
... SEATTLE, Nov. 19 Omeros Corporation (Nasdaq: OMER ) today ... 2009. For the three months ended September 30, 2009, Omeros reported ... compared to a net loss of $7.4 million, or $2.54 per ... ended September 30, 2009, the Company reported a net loss of ...
Cached Biology Technology:Karolinska Development and EIF Start Landmark Co-Investment Fund for Life Science Innovation 2Karolinska Development and EIF Start Landmark Co-Investment Fund for Life Science Innovation 3Process Analytical Technology (PAT) in Green Chemistry and Green Engineering 2Omeros Corporation Reports Third Quarter 2009 Financial Results and Development Highlights 2Omeros Corporation Reports Third Quarter 2009 Financial Results and Development Highlights 3Omeros Corporation Reports Third Quarter 2009 Financial Results and Development Highlights 4Omeros Corporation Reports Third Quarter 2009 Financial Results and Development Highlights 5Omeros Corporation Reports Third Quarter 2009 Financial Results and Development Highlights 6Omeros Corporation Reports Third Quarter 2009 Financial Results and Development Highlights 7Omeros Corporation Reports Third Quarter 2009 Financial Results and Development Highlights 8
... a small and sensitive single quadrupole ... LC and IC. It features a newly ... (API) source for outstanding sensitivity and noise ... existing LC and IC methods, especially those ...
... The CHEMICON® CaspaTag™ Caspase-9 Pan-Caspase In Situ ... for detection of active caspases in cells ... use only. Not for use in diagnostic ... Caspase Detection Kits use a novel approach ...
... of Saccharomyces cerevisiae, as well as other ... many molecular biology laboratories. The ability to ... plasmid and linear DNAs using lithium based ... plasmid transformations and library screening easy and ...
... a fluorescein-conjugated jetSI-ENDO (excitation ... 520 nm), the powerful siRNA ... used to determine the transfection ... delivery and trafficking of siRNAs. ...
Biology Products: