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:4/26/2016)... Research and Markets has announced ... 2016-2020"  report to their offering.  , ,     (Logo: ... analysts forecast the global multimodal biometrics market to ... period 2016-2020.  Multimodal biometrics is being ... the healthcare, BFSI, transportation, automotive, and government for ...
(Date:4/14/2016)... Israel , April 14, 2016 ... Authentication and Malware Detection, today announced the appointment of ... assumed the new role. Goldwerger,s leadership appointment ... on the heels of the deployment of its platform ... BioCatch,s behavioral biometric technology, which discerns unique cognitive and ...
(Date:3/29/2016)... RATON, Florida , March 29, 2016 ... or the "Company") LegacyXChange "LEGX" and SelectaDNA/CSI Protect are ... DNA in ink used in a variety of writing ... theft. Buyers of originally created collectibles from athletes on ... through forensic analysis of the DNA. ...
Breaking Biology News(10 mins):
(Date:6/24/2016)... (PRWEB) , ... June 24, 2016 , ... While the ... such as the Cary 5000 and the 6000i models are higher end machines that ... the height of the spectrophotometer’s light beam from the bottom of the cuvette holder. ...
(Date:6/23/2016)... /PRNewswire/ - FACIT has announced the creation of ... company, Propellon Therapeutics Inc. ("Propellon" or "the Company"), ... portfolio of first-in-class WDR5 inhibitors for the treatment ... represent an exciting class of therapies, possessing the ... cancer patients. Substantial advances have been achieved with ...
(Date:6/23/2016)... -- The Biodesign Challenge (BDC), a university competition that asks ... systems and biotechnology, announced its winning teams at the ... York City . The teams, chosen ... MoMA,s Celeste Bartos Theater during the daylong summit. Keynote ... of architecture and design, and Suzanne Lee , ...
(Date:6/23/2016)... , June 23, 2016 Apellis Pharmaceuticals, ... 1 clinical trials of its complement C3 inhibitor, ... and multiple ascending dose studies designed to assess ... of subcutaneous injection in healthy adult volunteers. ... either as a single dose (ranging from 45 ...
Breaking Biology Technology: