Navigation Links
Fatty acid to enhance anticancer drug
Date:5/7/2010

Chemical changes in the genetic material, known as epigenetic modifications, regulate the activity of many genes. Thus, attachment of methyl groups to DNA often inactivates important cellular growth brakes. Therefore, this process called methylation is believed to be a major cause of uncontrolled division of cancer cells. Specific enzymes, the DNA methyltransferases, are responsible for methylation.

Unlike changes in the blueprint of the genetic material, epigenetic mutations are reversible and, thus, cancer cells can be restored to their "normal state". Substances causing this re-programming are already being used as anticancer drugs. Examples are azacytidine and decitabine, which are used in the treatment of a specific type of blood cancer called acute myeloid leukemia. Both substances are incorporated into the cell's genetic material, where they act as a trap for methyltransferases. They form permanent chemical bonds with the enzyme, thereby catching the methyltransferases one by one, so that no more genes are being silenced.

Scientists in Professor Frank Lyko's team at DKFZ were searching for azacytidine variants with enhanced efficacy, because the drug still remains ineffective in many cases even when it is has been established that tumor brakes have been put out of effect by methylation. Researchers believe that this therapy resistance is frequently caused by the fact that not enough of the agent gets into the interior of the cells, because cancer cells lack particular transport molecules in the cell membrane.

The Norwegian company Clavis Pharma produced the azacytidine variants with modified chemical properties. Among the substances studied was CP-4200, a coupled product of azacytidine and a fatty acid (elaidic acid). CP-4200 showed particularly good results. When cancer cells in the culture dish are treated with CP-4200, the amount of methyltransferase molecules in the interior of the cells is reduced. At the same time, the methyl groups bound to the DNA of cancer cells disappear and silenced tumor brakes are reactivated. The investigators assume that the elaidic acid makes it possible even for cells without special transport proteins to take up CP-4200; the substance might reach the cell interior directly through the membrane.

The effectiveness of azacytidine was previously proven only for acute myeloid leukemia. To find out whether CP-4200 shows an increased efficacy range, the investigators compared the two substances in mice suffering from another form of blood cancer, acute lymphatic leukemia. In all treatment tests investigated, the effectiveness of CP-4200 was superior to that of azacytidine. "Coupling to elaidic acid improves the bioavailability of the agent without impeding its epigenetic effect," explains project leader Frank Lyko."Therefore, we see chances of reversing methylation in far more cancer patients in the future and arresting tumor growth in this way."


'/>"/>

Contact: Dr.Sibylle Kohlstdt
s.kohlstaedt@dkfz.de
Helmholtz Association of German Research Centres
Source:Eurekalert

Related medicine news :

1. Researchers Identify 2 Genes Linked to Fatty Liver Disease
2. Studies Detail Possible Benefits of omega-3 Fatty Acids for Dogs With Arthritis
3. Shedding Light on Why Omega-3 Fatty Acids May Help the Heart
4. Horizon Display Demonstrates their Dedication to After-Sales Support with Enhanced Online Resources
5. Natural Wellness Announces New, All Natural Female and Male Sexual Enhancement Supplements
6. Orion Health Helps Northumbria Healthcare NHS Foundation Trust Deliver an Enhanced Electronic Patient Record
7. Summer Brings Increased Demand For Breast and Body Enhancement
8. Provalis Research Announces the Release of WordStat 6, Delivering Enhanced Analytical and Visualization Tools for Textual Data
9. Partnering to Enhance Consumer Safety with Residential Fire Sprinklers
10. PMSI and Ameritox Launch Program to Enhance Quality and Effectiveness of Opioid Therapy
11. CradlePoint Connectivity Enables HealthCare Professionals to Enhance In-Home Patient Care
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:10/13/2017)... (PRWEB) , ... October 13, 2017 , ... While it’s ... poses a problem. Fortunately, an inventor from Austin, Texas, has identified a solution. , ... medication in darkness or restricted lighting. As such, it eliminates the need to turn ...
(Date:10/13/2017)... , ... October 13, 2017 , ... PurhealthRX , ... Oil utilizing Purzorb™ technology. Applying the Purzorb™process to full spectrum CBD oil will revolutionize ... providing a CBD form that can be easily incorporated into liquid products, while reducing ...
(Date:10/13/2017)... Shelton, CT (PRWEB) , ... October 13, 2017 , ... ... and long-term care services, staged a mock evacuation of the facility as part of ... Department, Shelton Fire Department, Echo Hose EMS and Shelton City Emergency Manager, as well ...
(Date:10/13/2017)... NY (PRWEB) , ... October 13, 2017 , ... Ellevate ... people in business to advocate for action towards gender equality at their inaugural Summit ... from around the globe, and reached a social audience of over 3 million. To ...
(Date:10/13/2017)... , ... October 13, 2017 , ... ... be giving viewers the lowdown on sciatica in a new episode of "Success ... focuses on current events and innovation and investigates each subject in-depth with passion ...
Breaking Medicine News(10 mins):
(Date:9/23/2017)... 22, 2017 Janssen Biotech, Inc. (Janssen) announced ... from the U.S. Food and Drug Administration (FDA) for ... for the treatment of moderately to severely active rheumatoid ... data are needed to further evaluate the safety of ... RA. "We ...
(Date:9/19/2017)... 19, 2017   ZirMed Inc ., a recognized leader ... that it has been ranked #1 by its users for ... Rankings 2017 User Survey. ZirMed was recognized as the top-ranked ... and medical centers over 200 beds and holds one of ... user survey history. ...
(Date:9/12/2017)... PARIS and NEW YORK , Sept. 12, ... ethical performance ratings for global supply chains, has published the first annual ... the CSR performance of more than 20,400 companies evaluated by EcoVadis, based ... years 2015 and 2016. ... EcoVadis Global CSR Risk & Performance Index ...
Breaking Medicine Technology: