Featured Research

from universities, journals, and other organizations

Small-molecule inhibitors effectively targeted active colon cancer enzyme

Date:
December 7, 2010
Source:
American Association for Cancer Research
Summary:
Researchers have identified two small-molecule inhibitors that effectively targeted the focal adhesion kinase (FAK), an enzyme present in certain cancers that helps tumors thrive and survive.

Researchers have identified two small-molecule inhibitors that effectively targeted the focal adhesion kinase (FAK), an enzyme present in certain cancers that helps tumors thrive and survive.

Related Articles


If the drugs are developed into oral therapeutic agents in the future, they could open up the potential for more effective and less toxic cancer therapies, according to research presented at The American Association for Cancer Research special conference on Colorectal Cancer: Biology to Therapy, held Oct. 27-30, 2010.

"It is well known that FAK is overexpressed in more than 89 percent of colon cancer tumors, helping these cancer cells survive and spread," said Vita M. Golubovskaya, Ph.D., associate professor in the department of surgical oncology at Roswell Park Cancer Institute, Buffalo, N.Y., and co-founder and senior scientist of CureFAKtor Pharmaceuticals. "We have found that targeting a specific site of FAK, called the autophosphorylation site, is an effective way to kill colon cancers cells, as it blocks FAK activation and its survival signaling."

Through prior research, Golubovskaya and colleagues identified a novel cancer therapy approach that targets the autophosphorylation site of FAK, known as Y397. Once it is "activated" the Y397 site acts as a controller that can "activate" additional cells of the FAK enzyme.

"Thus, our goal was to inhibit this Y397 site to block FAK activity," Golubovskaya said.

To do that, the researchers screened more than 140,000 small molecules from the National Cancer Institute database and identified several small molecules that could effectively target Y397. They then tested all of these molecules and found two that were the most potent at stopping colon cancer-cell growth: Y11 and Y30.

The effect of Y11 and Y30 were then tested on colon cancer cells. Compared with a commercially available inhibitor, Y11 and Y30 decreased the viability of all colon cancer cells in a time- and dose-dependent manner.

"Most companies target a site called the ATP binding site, which is very conservative, thus drugs developed to target this site are less specific and more toxic," Golubovskaya said. "Our inhibitors are very specific, inhibiting colon cancer survival and decreasing its viability and inhibiting tumor formation."

According to Golubovskaya, the next step is to test Y11 and Y30 in mice, eventually conducting pre-clinical studies with the goal in the future to use these drugs in patients after clinical trials.


Story Source:

The above story is based on materials provided by American Association for Cancer Research. Note: Materials may be edited for content and length.


Cite This Page:

American Association for Cancer Research. "Small-molecule inhibitors effectively targeted active colon cancer enzyme." ScienceDaily. ScienceDaily, 7 December 2010. <www.sciencedaily.com/releases/2010/10/101028132303.htm>.
American Association for Cancer Research. (2010, December 7). Small-molecule inhibitors effectively targeted active colon cancer enzyme. ScienceDaily. Retrieved October 25, 2014 from www.sciencedaily.com/releases/2010/10/101028132303.htm
American Association for Cancer Research. "Small-molecule inhibitors effectively targeted active colon cancer enzyme." ScienceDaily. www.sciencedaily.com/releases/2010/10/101028132303.htm (accessed October 25, 2014).

Share This



More Health & Medicine News

Saturday, October 25, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

IKEA Desk Converts From Standing to Sitting With One Button

IKEA Desk Converts From Standing to Sitting With One Button

Buzz60 (Oct. 24, 2014) IKEA is out with a new convertible desk that can convert from a sitting desk to a standing one with just the push of a button. Jen Markham explains. Video provided by Buzz60
Powered by NewsLook.com
Ebola Protective Suits Being Made in China

Ebola Protective Suits Being Made in China

AFP (Oct. 24, 2014) A factory in China is busy making Ebola protective suits for healthcare workers and others fighting the spread of the virus. Duration: 00:38 Video provided by AFP
Powered by NewsLook.com
WHO: Millions of Ebola Vaccine Doses by 2015

WHO: Millions of Ebola Vaccine Doses by 2015

AP (Oct. 24, 2014) The World Health Organization said on Friday that millions of doses of two experimental Ebola vaccines could be ready for use in 2015 and five more experimental vaccines would start being tested in March. (Oct. 24) Video provided by AP
Powered by NewsLook.com
Doctor in NYC Quarantined With Ebola

Doctor in NYC Quarantined With Ebola

AP (Oct. 24, 2014) An emergency room doctor who recently returned to the city after treating Ebola patients in West Africa has tested positive for the virus. He's quarantined in a hospital. (Oct. 24) Video provided by AP
Powered by NewsLook.com

Search ScienceDaily

Number of stories in archives: 140,361

Find with keyword(s):
Enter a keyword or phrase to search ScienceDaily for related topics and research stories.

Save/Print:
Share:

Breaking News:

Strange & Offbeat Stories


Health & Medicine

Mind & Brain

Living & Well

In Other News

... from NewsDaily.com

Science News

Health News

Environment News

Technology News



Save/Print:
Share:

Free Subscriptions


Get the latest science news with ScienceDaily's free email newsletters, updated daily and weekly. Or view hourly updated newsfeeds in your RSS reader:

Get Social & Mobile


Keep up to date with the latest news from ScienceDaily via social networks and mobile apps:

Have Feedback?


Tell us what you think of ScienceDaily -- we welcome both positive and negative comments. Have any problems using the site? Questions?
Mobile: iPhone Android Web
Follow: Facebook Twitter Google+
Subscribe: RSS Feeds Email Newsletters
Latest Headlines Health & Medicine Mind & Brain Space & Time Matter & Energy Computers & Math Plants & Animals Earth & Climate Fossils & Ruins