Navigation Links
PI-103 Effective against Brain Cancer

According to the researchers at the University of California, San Francisco (UCSF) they have identified a class of compounds that prevents the growth of brain cancer. // The compound called the PI-103 acts as a potent drug candidate against lethal brain tumor. In animal studies (mice) with human glioma grafts the drug is found to be potent against proliferating cancer cells. The unique effectiveness of PI-103 stems from its ability to attack two separate steps in the series of signals that trigger the spread of cancer. The dual blockade proved to be a safe and effective inhibitor of cancer cell proliferation in mice with the human tumors, the scientists found.

The glioma research is being published online May 15 by the journal Cancer Cell. A description of the strategy used to identify the molecular level action of the inhibitors was published online by the journal Cell on April 27. Food and Drug Administration approval five years ago of the cancer drug Gleevec marked a promising new strategy against cancer. Gleevec was the first drug on the market designed to block ubiquitous signaling molecules called protein kinases – enzymes known to trigger normal cell proliferation, and in the case of cancer, the growth of tumors.

Another group of kinases, called lipid kinases are now emerging as important new targets, especially PI3 alpha kinase, an enzyme often found to be overactive in brain, breast, colon and stomach cancers. But the sheer number of related kinases – 15 in the PI3 kinase family alone – and uncertainty about how each acts in the body – has stalled progress. Broad spectrum drugs that inhibit many related kinases inevitably cause toxicity and are poor drug candidates. To overcome this hurdle, Kevan Shokat, PhD, a Howard Hughes Medical Institute investigator at UCSF, and Zachary Knight, a postdoctoral fellow in his lab, developed a strategy to systematically inhibit many different but related kinases to identify which ones might be prime t argets to treat brain tumors.

In the Cell paper they described their success synthesizing a panel of different PI3 kinase inhibitors, showing for the first time the structural basis of the inhibitors' abilities to block different PI3 kinases. They used the new compounds to dissect the role of PI3 kinases in insulin signaling and in cancer. Drawing on this new tool, William Weiss, MD, associate professor of neurology at UCSF and an investigator in UCSF's Comprehensive Cancer Center, developed the strategy to treat gliomas. These cancers are the most common solid tumor of childhood, and about half of the people diagnosed with gliomas die within a year of diagnosis. Weiss and his colleagues report in the Cancer Cell paper that one PI3 kinase inhibitor in particular – PI-103 -- is unusually effective against gliomas in mice.

They believe the inhibitor is a promising drug candidate, and a UCSF neuro-oncologist is developing plans to launch a clinical trial within a year, Weiss says. The Weiss team discovered that the inhibitor's effectiveness lies in its dual impact. It inhibits both PI3 kinase and a protein kinase known as mTOR which acts downstream of PI3 kinase and is part of the cell's nutrient-sensing system. Clinical trials using inhibitors of mTOR alone have had disappointing results, Weiss says. One reason appears to be that the two kinases are part of a feedback loop. His group showed that mTOR inhibitors in clinical trials actually activate PI3-kinase while they inhibit mTOR. In effect, the drugs are blocking and encouraging cancer growth at the same time.

The new inhibitor offers a mechanism through which to block both the PI3 and the mTOR kinase pathways, a strategy that appears to be particularly effective at slowing growth of gliomas. Lead author on the Cancer Cell paper is Qi-Wen Fan, MD, PhD, assistant adjunct professor of neurology, in the Weiss lab. Co-authors along with Weiss, Shokat and Knight, all at UCSF, are David Gol denberg, staff research associate in neurology; Wei Yu, PhD, assistant research anatomist; and David Stokoe, PhD, assistant professor in the Cancer Research Institute. Shokat, UCSF professor of cellular and molecular pharmacology, is also a faculty affiliate in QB3, the Institute for Quantitative Biomedical Research.

Source: Eureklert
'"/>




Related medicine news :

1. New Way to "See" Genes, Evaluate Effectiveness of Gene Therapies Discovered
2. Inhaled Steroids Safe & Effective for Children with Asthma
3. ZD1839 Proves Effective - A Breakthrough in fighting Lung Cancer
4. Fluoride Found Effective in Osteoporosis
5. Aspirin and Warfarin Are Equally Effective for Stroke Prevention
6. Implantable Contact Lens Found Safe and Effective
7. Effective And Economical Agent For Anthrax
8. Stem Cell Transplants May Be Effective For MS Patients
9. Effective therapy for Huntingtons disease
10. Chemotherapy Effective for Bladder Cancer
11. Drug Effective for Vascular Dementia
Post Your Comments:
*Name:
*Comment:
*Email:


(Date:6/25/2016)... Canada (PRWEB) , ... June 25, 2016 , ... Conventional ... pursuit of success. In terms of the latter, setting the bar too high can ... risk more than just slow progress toward their goal. , Research from ...
(Date:6/24/2016)... Marne, Michigan (PRWEB) , ... June 24, 2016 , ... ... awareness about the dangers associated with chronic pain and the benefits of holistic treatments, ... for individuals who are suffering with Sickle Cell Disease. , Sickle Cell Disease (SCD) ...
(Date:6/24/2016)... MIAMI, Fla. (PRWEB) , ... June 24, 2016 , ... ... Florida Trend magazine’s 2016 Legal Elite. The attorneys chosen by their peers for this ... of Florida. , Seven Greenberg Traurig Shareholders received special honors as members of this ...
(Date:6/24/2016)... ... , ... Topical BioMedics, Inc, makers of Topricin and MyPainAway Pain Relief Products, join The ‘Business ... to $12 an hour by 2020 and then adjusting it yearly to increase at the ... minimum wage, assure the wage floor does not erode again, and make future increases more ...
(Date:6/24/2016)... (PRWEB) , ... June 24, 2016 , ... ... Living, is proud to recognize Dr. Barry M. Weintraub as a prominent plastic ... most beautiful women in the world, and the most handsome men, look naturally ...
Breaking Medicine News(10 mins):
(Date:6/24/2016)... --  Pulmatrix, Inc ., (NASDAQ: PULM ), ... today that it was added to the Russell Microcap ... set of U.S. and global equity indexes on June ... for Pulmatrix," said Chief Executive Officer Robert Clarke ... in developing drugs for crucial unmet medical needs, and ...
(Date:6/23/2016)... June 23, 2016  MedSource announced today that ... e-clinical software solution of choice.  This latest decision ... value to their clients by offering a state-of-the-art ... relationship establishes nowEDC as the EDC platform of ... full-service clients.  "nowEDC has long been a preferred ...
(Date:6/23/2016)... Research and Markets has announced the addition ... Chemical (Sugar, Petrochemical, Glycerin), Inorganic Chemical), Functionality (Filler, Binder, ... Forecast to 2021" report to their offering. ... excipients market is projected to reach USD 8.1 Billion ... forecast period 2016 to 2021. The ...
Breaking Medicine Technology: