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:6/23/2017)... , ... June 23, 2017 , ... ... Act (BCRA), their proposed healthcare bill to repeal and replace the Affordable Care ... Senate bill would make significant cuts to Medicaid, a public health insurance program ...
(Date:6/23/2017)... ... June 23, 2017 , ... Everybody has their own ... others prefer to read it, and some people don't like it at all. FindaTopDoc ... what they found: , Erotic literature can give readers a taste of their deepest, ...
(Date:6/23/2017)... ... June 23, 2017 , ... 21 Middle East and South Asia Leaders ... leaders from government, business and civil society in 11 countries across the Middle East ... engaging in a transformative exchange of knowledge and ideas with the leading minds in ...
(Date:6/23/2017)... (PRWEB) , ... June 23, 2017 , ... Ulster University, ... June, 2017 from 9 am to 3 pm to present to graduate students exciting ... is an original curriculum project led by The Health Improvement Service of the ...
(Date:6/23/2017)... ... June 23, 2017 , ... Moore Insurance, an eastern ... access to asset protection and financial planning services, is teaming up with the ... lives of children with cancer and other chronic diseases. , The For A ...
Breaking Medicine News(10 mins):
(Date:6/16/2017)... WAYNE, N.J. , June 16, 2017 Datascope Corp. ... sold by Datascope Corp. for a potential electrical test failure code.     ... PRODUCT PART NUMBER ... CS100 IABP CS300 IABP ... ...
(Date:6/13/2017)... June 13, 2017 Zimmer Biomet Holdings, Inc. (NYSE ... announced that the U.S. Food and Drug Administration (FDA) has ... 2015 relating to its Zhejiang, China ... "The successful clearance of the Warning Letter related ... facility is a measure of the progress we have made ...
(Date:6/9/2017)... , June 9, 2017 More than 400 ... effort to help spread lessons learned from clinical research ... Diabetes Federation (IDF) and Eli Lilly and Company (NYSE: ... second phase of the Bringing Research in Diabetes to ... commitment to helping people with diabetes effectively manage their ...
Breaking Medicine Technology: