Navigation Links
Scripps Research and MIT scientists discover class of potent anti-cancer compounds
Date:3/7/2011

velop a PME-1 inhibitor, mainly because standard substrate assays for the enzyme were difficult to adapt for high-throughput screening," said Cravatt. "But we believed that we could use our new 'substrate-free' screening technology for PME-1; and we knew that we needed to try a large, high-throughput screen, because our small-scale efforts to find PME-1 inhibitors had come up empty."

Scripps Research runs an NIH Molecular Libraries Program screening center at its Jupiter, Florida campus. There, the institute's researchers set up an automated version of Bachovchin's new screening technique and used it to search for strong PME-1 inhibitors among the 300,000-plus small-molecule compounds in the NIH library.

Super Potent, Super Selective

Like many molecules, ABLs can exist in two mirror-image versions, known as enantiomers, and they usually are synthesized as an equal mixture of both compounds. But Fu and his group had used new chemistry techniques to produce the ABLs in an "enantiomerically selective" way, in case one enantiomer of a compound had more activity than its mirror-image twin. And, in fact, one of these enantiomeric molecules, ABL127, turned out to fit so precisely into a nook on PME-1 that it completely blocked PME-1 activity in cell cultures and in the brains of mice. Aside from being extremely potent, it also was highly selective for PME-1, so that even at higher doses, it had negligible effects on other enzymes in the PME-1 family, known as serine hydrolases. In mice, ABL127's inhibition of PME-1 activity caused a more than one-third drop in the measured level of demethylated ("inactive") PP2A.

The Cravatt and Fu labs are now working together to synthesize more ABLs and explore their chemistry, looking for the best possible PME-1 inhibitor. The near-term goal is to use ABL127 as a scientific probe to study PME-1 functions in animals. A longer-term goal is to develop ABL127, or related compounds, as potential oncolo
'/>"/>

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

Page: 1 2 3 4

Related medicine news :

1. Scripps Health Begins Pioneering Study of Human Tumor Sequencing in Cancer Patients
2. Top Scientists Explore the Origin of Life in Annual Lasker Lecture at Scripps Research Institute Florida Campus
3. Scripps Blood & Marrow Transplant Program Celebrates 30th Anniversary of Providing Life-Saving Care
4. Scripps Memorial Hospital La Jolla First in San Diego to Achieve Magnet Nursing Re-designation
5. Scripps Announces Plans for Region's First Proton Therapy Center; $185 Million Facility to Offer Advanced Care to Cancer Patients
6. Scripps Research scientists share $2 million in Florida state research grants
7. Scripps Center for Executive Health Now Offers Genetic Testing
8. Scripps Research scientists uncover previously unknown natural mechanism that controls cocaine use
9. NIH awards Scripps Florida scientists $2.3 Million to develop drug addiction treatments
10. Scripps Research scientists solve long-standing mystery of protein quality control mechanism
11. Scripps and Trius team up to develop new antibiotics with US Department of Defense grant
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:7/3/2015)... ... July 03, 2015 , ... On June ... a new SEO training system called "Page One Engine" . The program, ... has received glowing reviews from several well-known marketers. HonestyFirstReviews.com's Tiffany Hendricks has joined ...
(Date:7/3/2015)... ... July 03, 2015 , ... B. ... has been retained to lead a national president recruitment for Regional ... the healthcare industry, B. E. Smith has recently placed more than 1,000 healthcare ...
(Date:7/3/2015)... ... 2015 , ... Talcum powder attorneys representing clients in national lawsuits announce the ... Center website. Just as the previous version did, the new website will serve as ... and ovarian cancer warning information. The site is routinely updated with news articles on ...
(Date:7/3/2015)... , ... July 03, 2015 , ... Yisrayl Hawkins, Pastor ... article this week that he says will reveal biblical truth and expose popular lies ... Does Your Bible Say Don’t Have Sex”, immediately goes into the core of the ...
(Date:7/2/2015)... ... ... sweetFrog Enterprises, LLC. is pleased to announce the opening of its newest location in Dallas, ... The premium frozen yogurt chain was listed as #22 on the Inc. 500 list of ... at Bachman Lake, is located at:, 3701 W. Northwest Highway, STE 430, Dallas, TX 75220 ...
Breaking Medicine News(10 mins):Health News:Page One Engine - Review Of Dori Friend's SEO Training Course Released 2Health News:Regional Care, Inc. Retains B. E. Smith to Recruit New President 2Health News:Regional Care, Inc. Retains B. E. Smith to Recruit New President 3Health News:Talcum Powder Lawsuit News: Cancer Attorneys Launch Updated Mobile Site 2Health News:Talcum Powder Lawsuit News: Cancer Attorneys Launch Updated Mobile Site 3Health News:Yisrayl Hawkins Explains What the Bible Really Says about Sex in New Publication This Week 2Health News:sweetFrog Opens 18th Location in the Lone Star State 2
... may prevent damage to the liver caused by excessive ... Alabama at Birmingham. The findings, published online April 21, ... the way to treatments to reverse steatosis, or fatty ... and cancer. The research team, led by Victor ...
... , MONDAY, May 2 (HealthDay News) -- American workers forced ... a new study suggests. A team of U.S. researchers ... per month are at higher risk for cardiovascular disease than "light" ... month. The team at Columbia University,s Mailman School of Public ...
... hands with contaminated soap from bulk-soap-refillable dispensers can increase ... may play a role in transmission of bacteria in ... issue of the journal Applied and Environmental Microbiology ... a universally accepted practice for reducing the transmission of ...
... , MONDAY, May 2 (HealthDay News) -- Eating meals with ... study finds. Researchers pooled data from 17 earlier ... regularly for meals were 24 percent more likely to eat ... They were also less likely to suffer from eating disorders. ...
... DENVER, CO, MAY 2, 2011 Two scientists who ... been chosen to receive the 2011 March of Dimes ... OBE, DSc, FRS, professor of Human Genetics, Southampton University ... Laboratory, Salisbury, England and David C. Page, MD, director, ...
... MONDAY, May 2 (HealthDay News) -- Exercising while learning might ... researchers looked at students in grades 1 through 6 at ... in a program that incorporated physical activity and classroom lessons ... the study, the students had 40 minutes of physical education ...
Cached Medicine News:Health News:Antioxidant may prevent alcohol-induced liver disease 2Health News:Frequent Business Travel Tough on the Heart, Study Finds 2Health News:Washing with contaminated soap increases bacteria on hands 2Health News: Family Meals Keep Kids Slimmer, Healthier, Study Finds 2Health News: Family Meals Keep Kids Slimmer, Healthier, Study Finds 3Health News:Exercising While Learning Boosts Test Scores, Study Finds 2
(Date:7/2/2015)... 2, 2015 Pharma Major Lupin Limited ... "Biocom" in Russia subject to certain ... pharmaceutical market which recorded RUB 765 billion in sales, placing ... the world in 2014 (IMS Health). For over a decade, ... continue with this trend, projecting Russia ...
(Date:7/2/2015)... DURHAM, N.C. , July 2, 2015 /PRNewswire/ ... acquisition of assets related to the ion channel biology ... had previously been obtained as part of Pfizer,s 2011 ... of Pfizer,s rights to the "Icagen" name and trademark. ... provide comprehensive services for ion channel and transporter drug ...
(Date:7/2/2015)... Research and ... of the "2015 New Frontiers in ... Technologies, Competitive Landscape" report to their ... Clinical Chemistry and Immunodiagnostics: Global Challenges, Emerging ... strategic analysis of major business opportunities emerging ...
Breaking Medicine Technology:Lupin Acquires Biocom in Russia 2Lupin Acquires Biocom in Russia 3Icagen Re-launched through XRpro Sciences Acquisition of Pfizer Team and Technology for Ion Channel and Transporter Drug R&D 2Icagen Re-launched through XRpro Sciences Acquisition of Pfizer Team and Technology for Ion Channel and Transporter Drug R&D 3Icagen Re-launched through XRpro Sciences Acquisition of Pfizer Team and Technology for Ion Channel and Transporter Drug R&D 4New Frontiers in 2015 Global Clinical Chemistry and Immunodiagnostics Market: Challenges, Emerging Technologies, Competitive Landscape 2
... Therapeutics, Inc. (OTC Bulletin Board: ECTE ), ... a non-invasive, wireless, transdermal continuous glucose monitoring (tCGM) system ... today announced results for the year ended December 31, ... through Echo,s website at www.echotx.com . ...
... March 21, 2011 CardioFocus , a venture ... disorders, has secured $5M in debt financing from ... life science companies of all sizes worldwide. CardioFocus will ... in the United States and to expand the commercialization ...
Cached Medicine Technology:Echo Therapeutics Announces 2010 Financial Results 2Echo Therapeutics Announces 2010 Financial Results 3Echo Therapeutics Announces 2010 Financial Results 4CardioFocus Secures $5M Credit Facility with Silicon Valley Bank 2
... The Primus 96 Thermal Cyclers provide comprehensive ... They are ideal instruments for the optimization ... as for low to medium throughput PCR ... the 96 well block allows a choice ...
... TC-512 has a graphical touch screen display ... at the "touch of a screen." ... gradient, Touch Screen, Graphical Display, Memory Cards, ... Block Format, Intuitive Programmin, Free Instrument Software ...
... The Tetrad 2 thermal cycler incorporates a ... Tetrad chassis. As before, the chassis controls ... supply is internal, while a large, color LCD ... updated automatic lids -- Moto Alphas -- give ...
Dual-bay Dyad thermal cycler chassis, does not include the Alpha units (requires 2)...
Medicine Products: