Navigation Links
Disrupting a destructive duo: U of T Mississauga researchers inhibit cancer proteins
Date:8/20/2009

A research team led by U of T Mississauga scientists has developed a new way to split up a dangerous pair of cancer proteins, a finding that could ultimately lead to chemotherapy that is more effective and has fewer side effects.

Working with scientists at the University of Central Florida and the Princess Margaret Hospital, Professor Patrick Gunning of the Department of Chemical and Physical Sciences has created several molecules that inhibit Stat3, a protein that--in cancer cells--pairs with another copy of itself and goes haywire. The findings appear in the September issue of the journal ChemBioChem: A European Journal of Chemical Biology.

"The molecules we have created are particularly nice because they're showing selectivity against cancer cells but not against healthy cells," says senior author Gunning. "This molecule could be used in conjunction with typical chemotherapeutics, and it could mean that drugs will have less resistanceso you could use lower dosages and cause fewer side effects."

The Stat3 protein is involved in almost all cancers, and is known to contribute to the resistance of cancer cells to current drug therapies. "Most currently available therapeutics aim to induce cell death," says Gunning. "We wanted to make small molecules that could try and stop this protein."

In cancerous cells, Stat3 proteins bind together to work as a lethal pair, and inhibitors work to prevent this. This type of protein-protein interaction is notoriously difficult to counter. Gunning's team targeted binding "hotspots" on a known Stat3 inhibitor called S3I-201. They chemically altered the inhibitor to produce several new variants, which they then tested on Stat3.

In in vitro studies, some variants proved to be even more powerful than S3I-201, and showed activity against prostate, breast and acute myeloid leukemia cancer cell lines. "These are some of the most potent inhibitors in the literature so far for this particular protein," says Gunning. "In some cases, they were more than twice as effective as the existing inhibitor."

When the team used more complex cancer cell models, they found the inhibitors survived the passage across the cell membrane and still targeted the Stat3 cancer proteins inside. Gunning and his colleagues are working to make the new inhibitors even more effective, as well as more metabolically stable, meaning that they can survive the chemical defense mechanisms within the cell.


'/>"/>

Contact: Nicolle Wahl
nicolle.wahl@utoronto.ca
905-569-4656
University of Toronto
Source:Eurekalert

Related biology news :

1. Disrupting common parasites ability to talk to each other reduces infection
2. New genus of self-destructive palm found in Madagascar
3. Researchers boost production of biofuel that could replace gasoline
4. Researchers find genetic link between physical pain and social rejection
5. UTSA biology researchers demystify elusive war zone bacterium
6. UGA researchers propose model for disorders caused by improper transmission of chromosomes
7. Researchers develop new, more-sensitive assay for detecting DNA methylation in colon cancer
8. NIH-funded researchers sequence exomes of 12 people
9. USC researchers identify regulatory genetic sequences that may predict risk for prostate cancer
10. K-State lab gives researchers the tools to study porcine circovirus associated diseases
11. Hebrew U. researchers shed light on the brain mechanism responsible for processing of speech
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/19/2017)... 19, 2017 The global military ... is marked by the presence of several large global ... by five major players - 3M Cogent, NEC Corporation, ... for nearly 61% of the global military biometric market ... the global military biometrics market boast global presence, which ...
(Date:4/13/2017)... According to a new market research report "Consumer IAM Market by ... Service, Authentication Type, Deployment Mode, Vertical, and Region - Global Forecast to ... USD 14.30 Billion in 2017 to USD 31.75 Billion by 2022, at ... ... MarketsandMarkets Logo ...
(Date:4/11/2017)... NXT-ID, Inc. (NASDAQ:   NXTD ) ("NXT-ID" or ... independent Directors Mr. Robin D. Richards and Mr. ... the company,s corporate governance and expertise. ... Gino Pereira , Chief Executive Officer said," ... and benefiting from their considerable expertise as we move forward ...
Breaking Biology News(10 mins):
(Date:10/10/2017)... ... 2017 , ... San Diego-based team building and cooking events company, Lajollacooks4u, has ... The bold new look is part of a transformation to increase awareness, appeal to ... period. , It will also expand its service offering from its signature gourmet cooking ...
(Date:10/10/2017)... ... ... Dr. Bob Harman, founder and CEO of VetStem Biopharma, Inc. ... event entitled “Stem Cells and Their Regenerative Powers,” was held on August 31st, ... was joined by two human doctors: Peter B. Hanson, M.D., Chief of Orthopedic Surgery, ...
(Date:10/10/2017)... BARBARA, CALIFORNIA (PRWEB) , ... October 10, 2017 ... ... management, technological innovation and business process optimization firm for the life sciences and ... BoxWorks conference in San Francisco. , The presentation, “Automating GxP Validation ...
(Date:10/9/2017)... ... ... The award-winning American Farmer television series will feature 3 Bar Biologics in an ... on RFD-TV. , With global population estimates nearing ten billion people by 2050, ... a growing nation. At the same time, many of our valuable resources are becoming ...
Breaking Biology Technology: