Navigation Links
Moffitt Cancer Center researchers design small molecule to disrupt cancer-causing protein
Date:3/25/2013

Researchers at Moffitt Cancer Center and colleagues at the University of South Florida have developed a small molecule that inhibits STAT3, a protein that causes cancer. This development could impact the treatment of several tumor types, including breast, lung, prostate and others that depend on STAT3 for survival.

The study appeared in the Jan. 15 online issue of Cancer Research, a publication of the American Association for Cancer Research.

"STAT3 has been associated with poor prognosis and resistance to chemotherapy in patients with cancer," explained Said M. Sebti, Ph.D., chair of the Drug Discovery Department at Moffitt. "Two STAT3 molecules need to bind to each other, a process called dimerization, to cause malignancy. We developed a small molecule called S3I-1757 to prevent dimerization by disrupting STAT3-STAT3 binding. Once disrupted, STAT3's ability to help cancer cells survive, grow and invade is neutralized."

"Activated STAT3 contributes to cancer at several levels," said study co-author Nicholas J. Lawrence, Ph.D., senior member of Moffitt's Drug Discovery Department. "It triggers the uncontrolled proliferation, invasion and spread of cancer cells. That makes STAT3 an attractive target for drug discovery and therapy."

STAT3 was first found to be involved in malignant transformation in 1995, but researchers have been unable to develop an inhibitor for the protein. In part, the challenge stemmed from the fact that STAT3-STAT3 binding is a protein-protein interaction involving a large surface area, difficult to target with drug-like small molecules.

The researchers, who had been working on finding an inhibitor for STAT3-STAT3 dimerization for some time, recently overcame that challenge and demonstrated in laboratory studies that S31-1757 was effective in neutralizing STAT3's activity.

"We used several approaches to demonstrate that S31-1757 is able to inhibit malignant transformation by its ability to inhibit the STAT3 function," Sebti said. "These included targeting the ability of STAT3 to bind itself."

Their findings will be presented at the annual AACR meeting in April in Washington, D.C.


'/>"/>

Contact: Kim Polacek
kim.polacek@moffitt.org
813-745-7408
H. Lee Moffitt Cancer Center & Research Institute
Source:Eurekalert

Related medicine news :

1. Genetic risk strategies needed for young, black, female breast cancer patients, Moffitt study shows
2. Moffitt Cancer Center researchers study use of dasatinib for patients with high-risk MDS
3. Cancer doesnt change young girls desire to have children, Moffitt Cancer Center study shows
4. Surgery and radiation improve survival for metastatic gastric cancer patients, Moffitt study shows
5. Moffitt researchers say silencing of retinoblastoma gene regulates differentiation of myeloid cells
6. Moffitt researchers find potential new therapeutic target for treating non-small cell lung cancer
7. Moffitt Cancer Center researchers develop automated breast density test linked to cancer risk
8. Tumor cells engineer acidity to drive cell invasion, Moffitt Cancer Center researchers say
9. New drug improves survival in multiple myeloma relapse, Moffitt Cancer Center researchers say
10. Moffitt study shows smoking cessation more successful for cancer patients who quit before surgery
11. Hispanics leery of health care providers, often avoid cancer screenings, Moffitt study shows
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/21/2017)... , ... April 21, 2017 , ... ... announced an exciting new partnership with the highly regarded and well renowned Asian ... highly innovative, myTAP & myTAP PAP Nasal Pillow Mask, and will stabilize and ...
(Date:4/21/2017)... MD (PRWEB) , ... April ... ... accreditation organization promoting quality-based imaging practices, is seeking candidates to serve on ... for diagnostic imaging. , “RadSite’s ultimate mission is improving image quality ...
(Date:4/21/2017)... ... , ... Westside Dental Associates and its owner, Dr. Les Latner, ... Dr. Latner has become one of the Los Angeles area’s premier dentists. “It’s been ... all their dental needs,” said Dr. Latner, who was recently named Chairperson of the ...
(Date:4/21/2017)... ... April 21, 2017 , ... During April 21-23, Super-Sod will join ... This festival offers entertainment for everyone — from the avid gardener to the landscape ... very high quality event held in a grand venue, and we are certainly looking ...
(Date:4/21/2017)... ... April 21, 2017 , ... Indiana Fiber Network, LLC (IFN), ... service to Tele-Media Solutions. IFN is delivering Multi-Gigabit data rates as an ... Solution’s protect transport with 3GB Dual Access Internet access now available in their ...
Breaking Medicine News(10 mins):
(Date:4/20/2017)... April 20, 2017  CVS Pharmacy, the retail ... a new store design to enhance the retail ... food, health-focused products and expanded beauty selections paired ... customers discover new offerings. Together with its innovative ... of the customer experience at CVS Pharmacy.  ...
(Date:4/20/2017)... , April 20, 2017 NeuroVive Pharmaceutical ... today announced positive preclinical results demonstrating anti-fibrotic ... for non-alcoholic steatohepatitis (NASH), in an additional ... NV556 has previously shown similar anti-fibrotic ... Today, NeuroVive,s scientists present novel data demonstrating ...
(Date:4/19/2017)... VIEW, Calif. , April 19, 2017  IRIDEX ... it will release financial results for the first quarter ... 3, 2017.  The Company,s management team will host a ... 5:30 p.m. ET. Investors interested in listening ... (844) 707-0665 for domestic callers or (703) 326-3030 for ...
Breaking Medicine Technology: