Navigation Links
Small molecules block cancer gene
Date:3/10/2009

HOUSTON (March 10, 2009) 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, said a Baylor College of Medicine researcher in a report that appears in the current online issue of the journal PLoS One (Public Library of Science ONE).

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 Dan L. Duncan Cancer Center.

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.

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 affect 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.


'/>"/>

Contact: Glenna Picton
picton@bcm.edu
713-798-4710
Baylor College of Medicine
Source:Eurekalert

Related biology news :

1. Social parasites of the smaller kind
2. Small animal imaging facility is big boon to research
3. Handbook of small grain insects available now
4. New molecular clock from LLNL and CDC indicates smallpox evolved earlier than believed
5. 2007 ozone hole smaller than usual
6. Cilia: small organelles, big decisions
7. Research shows loggerhead sea turtles threatened by small-scale fishing operations
8. Small-scale fishing in Mexico rivals industrial fisheries in accidental turtle deaths
9. Sweet potato shines as new promise for small enterprise and hunger relief in developing countries
10. Identification of a novel class of (not-so) small RNAs
11. Small RNA plays parallel roles in bacterial metabolism
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:2/14/2017)... Feb. 14, 2017  Wake Forest Baptist Medical Center ... new chief executive officer (CEO). Freischlag joins the medical ... D. McConnell , M.D., who last year announced that ... Medical Center, after leading it since 2008.   ... of Wake Forest Baptist,s academic health system, which includes ...
(Date:2/13/2017)... WASHINGTON , Feb. 13, 2017 Former ... U.S. Senate Judiciary Committee, Janice Kephart of ... regarding President Donald Trump,s "Executive Order: Protecting ... States" (Jan. 27, 2017):  "As President Trump,s ... 9th Circuit has now essentially banned the travel ban, ...
(Date:2/9/2017)... LONDON , Feb. 9, 2017 The ... in-depth analysis of the biomass boiler market globally in ... sales of biomass boilers. The market for biomass boilers ... product type, end-user, application, and country/region. The market based ... agriculture & forest residues, biogas & energy crops, urban ...
Breaking Biology News(10 mins):
(Date:3/29/2017)... Germany , March 29, 2017 QIAGEN ... STANDARD: QIA) today announced the U.S. launch of its ipsogen ... cleared by the U.S. Food and Drug Administration as a qualitative in vitro ... extracted from EDTA whole blood.* ... ipsogen JAK2 assay is processed on QIAGEN,s Rotor-Gene ® Q MDx ...
(Date:3/29/2017)... TIKVAH, Israel , March ... (NASDAQ: BCLI), a leading developer of adult ... financial results for the year ended December ... highly successful and pivotal year for Brainstorm, with a ... made on clinical, regulatory and operational fronts," said ...
(Date:3/29/2017)... , March 29, 2017  Halozyme Therapeutics, Inc. ... and drug-delivery therapies, today announced that an Oncologic ... Drug Administration voted 11 to 0 that the ... injection was favorable for patients in the proposed ... and chronic lymphocytic leukemia. The FDA action date ...
(Date:3/29/2017)... ... March 29, 2017 , ... Bactana Animal Health, a ... the world’s food supply through enhancement of the gut microbiota, today announced the closing ... Connecticut Innovations , New York-based Sustainable Income Capital Management, LLC and a number of ...
Breaking Biology Technology: