Forum for Science, Industry and Business

Sponsored by:     3M 
Search our Site:

 

Researchers develop synthetic compound that may lead to drugs to fight pancreatic, lung cancer

10.03.2011
Researchers at UT Southwestern Medical Center have identified a chemical compound that may eventually lead to a drug that fights cancers that are dependent on a particular anti-viral enzyme for growth.

The researchers are testing the compound's effectiveness at fighting tumors in mice. If it is successful, they will then work to develop a drug based on the compound to combat pancreatic and non-small cell lung cancer, two cancer types in which this particular enzyme, TBK-1, often is required for cancer cell survival.

"Our prediction is that TBK-1 is a good pharmacological intervention target for a subset of lung and pancreas cancers that are addicted to the activity of this enzyme. We believe there is a large population of cancer patients that could respond to inhibition of this activity," said Dr. Michael White, professor of cell biology and senior author of the study in the Feb. 18 issue of Molecular Cell.

The investigation, which lasted three and a half years, revealed how activation of the natural virus-fighting protein TBK-1 is hijacked in cancer cells to support growth and survival.

More than 250,000 compounds were screened to find one that would inhibit the enzyme's cancer-protection mechanism. The most effective, a compound called 6-aminopyrazolopyrimidine developed in collaboration with pharmaceutical company Amgen, blocked TBK-1's effects in 40 percent to 50 percent of the non-small cell lung cancer and pancreatic cancer tissue cultures tested, reducing cancer growth. TBK-1 is activated by the Ras family of oncogenes, which are mutated in 40 percent of lung cancers and 90 percent of pancreatic cancers.

"We found a biological activity that some cancer cells need to be able to survive, and we found a way to turn it off," said Dr. White.

The next step, he said, would be ascertaining in rodents whether 6-aminopyrazolopyrimidine can permeate tumors, "hit the target and be effective." If the compound continues to demonstrate efficacy, researchers would begin work to develop a drug with the compound's properties for further testing.

The compound appears to migrate into all tissues of studied mice, but the UT Southwestern researchers don't know yet if it will penetrate solid tumors in the animal, "which is an incredibly important step in evaluating chemicals as drug leads," Dr. White said.

"We've illuminated the dark matter of regulation of an incredibly important oncogenic survival pathway. We've found a new regulatory arm of this pathway, and we've discovered you can inhibit it pharmacologically. That's target validation. The next step is to translate that target validation into development of a medicine," he said.

Other UT Southwestern researchers involved in the study were lead author Yi-Hung Ou, graduate student in cancer biology; Michael Torres and Rosalyn Ram, student research assistants in cancer biology; Dr. Tzuling Cheng, postdoctoral researcher in pediatrics; Dr. Christina Roland, surgery resident; and Dr. Rolf Brekken, associate professor of surgery and pharmacology. Researchers from Hybrigenics of Paris and Amgen Inc. of Thousand Oaks, Calif., also participated.

The work was supported by the National Institutes of Health and the Welch Foundation.

Visit www.utsouthwestern.org/cancer to learn more about UT Southwestern's clinical services in cancer.

This news release is available on our World Wide Web home page at http://www.utsouthwestern.edu/home/news/index.html

To automatically receive news releases from UT Southwestern via e-mail, subscribe at www.utsouthwestern.edu/receivenews

Debbie Bolles | EurekAlert!
Further information:
http://www.utsouthwestern.edu

More articles from Life Sciences:

nachricht Stiffness matters
22.02.2018 | Albert-Ludwigs-Universität Freiburg im Breisgau

nachricht Separate brain systems cooperate during learning, study finds
22.02.2018 | Brown University

All articles from Life Sciences >>>

The most recent press releases about innovation >>>

Die letzten 5 Focus-News des innovations-reports im Überblick:

Im Focus: Developing reliable quantum computers

International research team makes important step on the path to solving certification problems

Quantum computers may one day solve algorithmic problems which even the biggest supercomputers today can’t manage. But how do you test a quantum computer to...

Im Focus: In best circles: First integrated circuit from self-assembled polymer

For the first time, a team of researchers at the Max-Planck Institute (MPI) for Polymer Research in Mainz, Germany, has succeeded in making an integrated circuit (IC) from just a monolayer of a semiconducting polymer via a bottom-up, self-assembly approach.

In the self-assembly process, the semiconducting polymer arranges itself into an ordered monolayer in a transistor. The transistors are binary switches used...

Im Focus: Demonstration of a single molecule piezoelectric effect

Breakthrough provides a new concept of the design of molecular motors, sensors and electricity generators at nanoscale

Researchers from the Institute of Organic Chemistry and Biochemistry of the CAS (IOCB Prague), Institute of Physics of the CAS (IP CAS) and Palacký University...

Im Focus: Hybrid optics bring color imaging using ultrathin metalenses into focus

For photographers and scientists, lenses are lifesavers. They reflect and refract light, making possible the imaging systems that drive discovery through the microscope and preserve history through cameras.

But today's glass-based lenses are bulky and resist miniaturization. Next-generation technologies, such as ultrathin cameras or tiny microscopes, require...

Im Focus: Stem cell divisions in the adult brain seen for the first time

Scientists from the University of Zurich have succeeded for the first time in tracking individual stem cells and their neuronal progeny over months within the intact adult brain. This study sheds light on how new neurons are produced throughout life.

The generation of new nerve cells was once thought to taper off at the end of embryonic development. However, recent research has shown that the adult brain...

All Focus news of the innovation-report >>>

Anzeige

Anzeige

VideoLinks
Industry & Economy
Event News

2nd International Conference on High Temperature Shape Memory Alloys (HTSMAs)

15.02.2018 | Event News

Aachen DC Grid Summit 2018

13.02.2018 | Event News

How Global Climate Policy Can Learn from the Energy Transition

12.02.2018 | Event News

 
Latest News

Stiffness matters

22.02.2018 | Life Sciences

Magnetic field traces gas and dust swirling around supermassive black hole

22.02.2018 | Physics and Astronomy

First evidence of surprising ocean warming around Galápagos corals

22.02.2018 | Earth Sciences

VideoLinks
Science & Research
Overview of more VideoLinks >>>