Featured Research

from universities, journals, and other organizations

Small Molecules Block Cancer Gene

Date:
March 18, 2009
Source:
Baylor College of Medicine
Summary:
Finding molecules that block the activity of the oncogene Stat 3 (signal transducer and activator of transcription) required screening literally millions of compounds, using computers that compared the structure of the cancer-causing gene to those of the small molecules.

Finding molecules that block the activity of the oncogene Stat3 (signal transducer and activator of transcription) required screening literally millions of compounds, using computers that compared the structure of the cancer-causing gene to those of the small molecules, said a Baylor College of Medicine researcher in a report that appears in the current online issue of the journal PLoS One.

Related Articles


It was worth the effort, said Dr. David J. Tweardy, professor of medicine and molecular and cellular biology and chief of the division of infectious diseases at BCM, because it could point the way to better treatment of breast and other cancers, as well as chronic viral infections, asthma, and inflammatory bowel disease. He is also on the faculty of the NCI-designated Dan L. Duncan Cancer Center at BCM.

Virtual screening

The "virtual" high throughput screening looked at the possibility of "docking" 920,000 small drug-like compounds into a pocket of a specific domain of Stat3, said Tweardy. In other words, Tweardy and his colleagues identified an area on the Stat3 molecule that was important to its activity. Stat3 actually is critical in keeping malignant cells alive in the majority of cancers.

Once Tweardy and his colleagues had identified a critical "pocket" on Stat3, they used the computer to look for small molecules that would fit in that pocket and block the ability of Stat3 to maintain the cancer cell. That screen of nearly 1 million small molecules identified three likely compounds.

Assays of these compounds showed that they did halt the activity of Stat3 in the laboratory. With that information, Tweardy and his colleagues then screened another 2.47 million compounds for similarity to the original three.

They found another three. While five of the six had some activity in stopping Stat3, one – called 188 – was most effective. Three of the six worked to induce programmed cell death or apoptosis in breast cancer cell lines.

"It induced death in those breast cancer cells that depend for their survival on Stat3," said Tweardy.

Second-generation compounds

Tweardy and his colleagues are now looking at second generation compounds that promise to be even more effective against Stat3.

When he and his colleagues started looking at Stat3, they knew it was important in cancers of the head and neck. Further research showed that it also was important in breast, lung and prostate cancers as well as multiple myeloma (a cancer affecting blood-forming cells) and acute myelogenous leukemia.

Stat3 also plays a role in chronic virus infections, asthma, psoriasis and inflammatory bowel disease – all areas that Tweardy and his colleagues hope to pursue in the future.

Others who took part in this research include Xuejun Xu, Moses M. Kasembeli, Xueqing Jiang and Benjamin J. Tweardy, all of BCM.

Funding for this research comes from the National Cancer Institute.


Story Source:

The above story is based on materials provided by Baylor College of Medicine. Note: Materials may be edited for content and length.


Cite This Page:

Baylor College of Medicine. "Small Molecules Block Cancer Gene." ScienceDaily. ScienceDaily, 18 March 2009. <www.sciencedaily.com/releases/2009/03/090310152351.htm>.
Baylor College of Medicine. (2009, March 18). Small Molecules Block Cancer Gene. ScienceDaily. Retrieved November 28, 2014 from www.sciencedaily.com/releases/2009/03/090310152351.htm
Baylor College of Medicine. "Small Molecules Block Cancer Gene." ScienceDaily. www.sciencedaily.com/releases/2009/03/090310152351.htm (accessed November 28, 2014).

Share This


More From ScienceDaily



More Health & Medicine News

Friday, November 28, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Ebola Leaves Orphans Alone in Sierra Leone

Ebola Leaves Orphans Alone in Sierra Leone

AFP (Nov. 27, 2014) — The Ebola epidemic sweeping Sierra Leone is having a profound effect on the country's children, many of whom have been left without any family members to support them. Duration: 01:02 Video provided by AFP
Powered by NewsLook.com
Experimental Ebola Vaccine Shows Promise In Human Trial

Experimental Ebola Vaccine Shows Promise In Human Trial

Newsy (Nov. 27, 2014) — A recent test of a prototype Ebola vaccine generated an immune response to the disease in subjects. Video provided by Newsy
Powered by NewsLook.com
Pet Dogs to Be Used in Anti-Ageing Trial

Pet Dogs to Be Used in Anti-Ageing Trial

Reuters - Innovations Video Online (Nov. 26, 2014) — Researchers in the United States are preparing to discover whether a drug commonly used in human organ transplants can extend the lifespan and health quality of pet dogs. Video provided by Reuters
Powered by NewsLook.com
Today's Prostheses Are More Capable Than Ever

Today's Prostheses Are More Capable Than Ever

Newsy (Nov. 26, 2014) — Advances in prosthetics are making replacement body parts stronger and more lifelike than they’ve ever been. Video provided by Newsy
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