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:7/25/2014)... The North America Artificial lift market report defines ... analysis and forecast of revenue. The artificial lift market in ... in 2013 to around $7 billion by 2018, at a ... through the TOC of North America artificial lift market report, ... provides a glimpse of the segmentation in North America Artificial ...
(Date:7/25/2014)... July 25, 2014 Agoura Hills dentist ... on Zoom Whitening. Zoom Whitening is one of the most ... through a dental professional. This light-assisted treatment uses a prescription-strength ... of the tooth to break up stains that are in ... coffee, tea, wine, soft drink and tobacco stains. , ...
(Date:7/25/2014)... The rising pharmaceutical sale across the US ... of the US PBM industry. A slow but steady increase ... sales in the US over the past few years. The ... in the prescription volume over the past few years. , ... 2013 Edition” the demand for the pharmacy benefit managers in ...
(Date:7/25/2014)... July 25, 2014 Ross A. Clevens, ... been invited to join the exclusive Obagi Clinical Advisory ... facial plastic surgeons, plastic surgeons and dermatologists. , ... exclusive Advisory Board of thought leaders held its first ... meeting was to give Obagi the opportunity to meet ...
(Date:7/25/2014)... 25, 2014 (HealthDay News) -- Dietary changes can dramatically ... a daily basis, according to a new study. ... might help detect and ease flare-ups for people with ... colitis and Crohn,s disease), the researchers said. Trillions ... effect on human health isn,t well understood, the Massachusetts ...
Breaking Medicine News(10 mins):Health News:North America Artificial Lift Services Market is Expected to Reach $7 Billion in 2018 - New Report by MicroMarket Monitor 2Health News:North America Artificial Lift Services Market is Expected to Reach $7 Billion in 2018 - New Report by MicroMarket Monitor 3Health News:North America Artificial Lift Services Market is Expected to Reach $7 Billion in 2018 - New Report by MicroMarket Monitor 4Health News:Agoura Hills Dentist, Dr. Amir Choroomi, is Now Offering a Promotion on Zoom Whitening 2Health News:US Pharmacy Benefit Management (PBM) Market Trends and Developments Now Available at MarketReportsOnline.com 2Health News:US Pharmacy Benefit Management (PBM) Market Trends and Developments Now Available at MarketReportsOnline.com 3Health News:Renowned Melbourne Plastic Surgeon to Join Private Medical Advisory Board 2Health News:Diet Changes Can Alter Gut Bacteria, Study Says 2
... MONDAY, March 7 (HealthDay News) -- Genetics may predispose some ... and stress are a fact of daily life -- to ... warns. The culprit is a specific abnormality of the ... gene is known to play a key role in the ...
... March 7, 2011 Embargoed by the journal ... time Working as part of a public program to ... useful molecules, scientists from The Scripps Research Institute and ... potent class of potential anti-cancer and anti-neurodegenerative disorder compounds. ...
... it won,t be obvious to UCSF Medical Center patients, behind ... processes their medications. With a new automated hospital pharmacy, believed ... technology and electronics to prepare and track medications with the ... error has occurred in the 350,000 doses of medication prepared ...
... of recognizing tumor growth, and naturally mounts an anti-cancer ... (antigens) and present them to T cells, and those ... kill tumor cells. In recent years, researchers have attempted ... new therapies- namely, by generating a pool of tumor ...
... Transplanting stem cells derived from umbilical ... offer future therapeutic benefit for those suffering from ... says a team of neuroscience researchers from the ... Brain Repair and collaborators from three private-sector research ...
... Reinberg HealthDay Reporter , SUNDAY, March 6 (HealthDay ... a safe way to detect Down syndrome during pregnancy, researchers ... identified a gene mutation associated with Down syndrome with 100 ... is a common birth defect, with one Down syndrome birth ...
Cached Medicine News:Health News:Mix of Genetics and Stress Can Impair Mental Abilities 2Health News:Scripps Research and MIT scientists discover class of potent anti-cancer compounds 2Health News:Scripps Research and MIT scientists discover class of potent anti-cancer compounds 3Health News:Scripps Research and MIT scientists discover class of potent anti-cancer compounds 4Health News:New UCSF robotic pharmacy aims to improve patient safety 2Health News:New UCSF robotic pharmacy aims to improve patient safety 3Health News:Transplanting umbilical cord and menstrual blood-derived stem cells offer hope for disorders 2Health News:Transplanting umbilical cord and menstrual blood-derived stem cells offer hope for disorders 3Health News:Transplanting umbilical cord and menstrual blood-derived stem cells offer hope for disorders 4Health News:Noninvasive Test May Identify Down Syndrome Early On 2
(Date:7/24/2014)... HILDEN , Deutschland, und ... , ... ermöglicht QIAGEN die Entwicklung von ... Genpanels, für Blutkrebs  Neuer Test ... Patienten mit Knochenmarkserkrankungen (myelodysplastischen Syndromen) einen günstigen ...
(Date:7/24/2014)... July 24, 2014  Uroplasty, Inc. (NASDAQ: ... manufactures and markets innovative proprietary products to treat ... fiscal 2015 first quarter ended June 30, 2014.  ...  PC Neuromodulation System grew 19% to $4.1 million, ... quarter of the prior year.  Total revenue for ...
(Date:7/24/2014)... July 24, 2014  Mettler-Toledo International Inc. (NYSE: ... 2014.  Provided below are the highlights: , ... quarter compared with the prior year. Reported sales increased ... , Net earnings per diluted share as reported (EPS) ... of 2013. Adjusted EPS was $2.57, an increase of ...
Breaking Medicine Technology:QIAGEN erweitert Pipeline für die personalisierte Medizin um vielversprechende genomische Biomarker zur Prognosebestimmung bei Blutkrebsbehandlungen 2QIAGEN erweitert Pipeline für die personalisierte Medizin um vielversprechende genomische Biomarker zur Prognosebestimmung bei Blutkrebsbehandlungen 3QIAGEN erweitert Pipeline für die personalisierte Medizin um vielversprechende genomische Biomarker zur Prognosebestimmung bei Blutkrebsbehandlungen 4QIAGEN erweitert Pipeline für die personalisierte Medizin um vielversprechende genomische Biomarker zur Prognosebestimmung bei Blutkrebsbehandlungen 5Uroplasty Reports Fiscal First Quarter Results 2Uroplasty Reports Fiscal First Quarter Results 3Uroplasty Reports Fiscal First Quarter Results 4Uroplasty Reports Fiscal First Quarter Results 5Uroplasty Reports Fiscal First Quarter Results 6Uroplasty Reports Fiscal First Quarter Results 7Uroplasty Reports Fiscal First Quarter Results 8Uroplasty Reports Fiscal First Quarter Results 9Uroplasty Reports Fiscal First Quarter Results 10Uroplasty Reports Fiscal First Quarter Results 11Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 2Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 3Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 4Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 5Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 6Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 7Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 8Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 9Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 10Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 11Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 12Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 13Mettler-Toledo International Inc. Reports Second Quarter 2014 Results 14
... , SAN DIEGO , Feb. 3 ... BDX ), today announced the launch of the ... prevention of influenza. Recognizing that schools and hospitals are important centers ... is designed to communicate that everyone can help prevent the spread ...
... , ATLANTA , Feb. 3 ... of Vytex® Natural Rubber Latex (NRL), a patented, all-natural ... natural rubber latex, has engaged The Investor Relations Group ... New York City , to serve as its ...
Cached Medicine Technology:BD Launches 'Be a Flu Fighter' Campaign to Promote Influenza Awareness and Prevention in Schools, Hospitals and Laboratories 2Vystar Corporation Engages The Investor Relations Group 2Vystar Corporation Engages The Investor Relations Group 3
... RayShield X-Drape combines full 0.25 ... Soft Fiber sterile drape material that ... sterile field between the clinician and ... when the clinician must be in ...
... The first mobile clinical assistant that ... convergence of technologies in the C5 ... normally do during your,shift such as ... take pictures using one single device.,With ...
Patent Pending lateral flow assay platform that contributes to increased sensitivty...
Colloidal Gold Conjugated, Rabbit anti-goat IgG (H&L) - 50 OD...
Medicine Products: