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 A Map of the Cell’s Power Station
18.08.2017 | Albert-Ludwigs-Universität Freiburg im Breisgau

nachricht On the way to developing a new active ingredient against chronic infections
18.08.2017 | Deutsches Zentrum für Infektionsforschung

All articles from Life Sciences >>>

The most recent press releases about innovation >>>

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

Im Focus: Fizzy soda water could be key to clean manufacture of flat wonder material: Graphene

Whether you call it effervescent, fizzy, or sparkling, carbonated water is making a comeback as a beverage. Aside from quenching thirst, researchers at the University of Illinois at Urbana-Champaign have discovered a new use for these "bubbly" concoctions that will have major impact on the manufacturer of the world's thinnest, flattest, and one most useful materials -- graphene.

As graphene's popularity grows as an advanced "wonder" material, the speed and quality at which it can be manufactured will be paramount. With that in mind,...

Im Focus: Exotic quantum states made from light: Physicists create optical “wells” for a super-photon

Physicists at the University of Bonn have managed to create optical hollows and more complex patterns into which the light of a Bose-Einstein condensate flows. The creation of such highly low-loss structures for light is a prerequisite for complex light circuits, such as for quantum information processing for a new generation of computers. The researchers are now presenting their results in the journal Nature Photonics.

Light particles (photons) occur as tiny, indivisible portions. Many thousands of these light portions can be merged to form a single super-photon if they are...

Im Focus: Circular RNA linked to brain function

For the first time, scientists have shown that circular RNA is linked to brain function. When a RNA molecule called Cdr1as was deleted from the genome of mice, the animals had problems filtering out unnecessary information – like patients suffering from neuropsychiatric disorders.

While hundreds of circular RNAs (circRNAs) are abundant in mammalian brains, one big question has remained unanswered: What are they actually good for? In the...

Im Focus: RAVAN CubeSat measures Earth's outgoing energy

An experimental small satellite has successfully collected and delivered data on a key measurement for predicting changes in Earth's climate.

The Radiometer Assessment using Vertically Aligned Nanotubes (RAVAN) CubeSat was launched into low-Earth orbit on Nov. 11, 2016, in order to test new...

Im Focus: Scientists shine new light on the “other high temperature superconductor”

A study led by scientists of the Max Planck Institute for the Structure and Dynamics of Matter (MPSD) at the Center for Free-Electron Laser Science in Hamburg presents evidence of the coexistence of superconductivity and “charge-density-waves” in compounds of the poorly-studied family of bismuthates. This observation opens up new perspectives for a deeper understanding of the phenomenon of high-temperature superconductivity, a topic which is at the core of condensed matter research since more than 30 years. The paper by Nicoletti et al has been published in the PNAS.

Since the beginning of the 20th century, superconductivity had been observed in some metals at temperatures only a few degrees above the absolute zero (minus...

All Focus news of the innovation-report >>>

Anzeige

Anzeige

Event News

Call for Papers – ICNFT 2018, 5th International Conference on New Forming Technology

16.08.2017 | Event News

Sustainability is the business model of tomorrow

04.08.2017 | Event News

Clash of Realities 2017: Registration now open. International Conference at TH Köln

26.07.2017 | Event News

 
Latest News

A Map of the Cell’s Power Station

18.08.2017 | Life Sciences

Engineering team images tiny quasicrystals as they form

18.08.2017 | Physics and Astronomy

Researchers printed graphene-like materials with inkjet

18.08.2017 | Materials Sciences

VideoLinks
B2B-VideoLinks
More VideoLinks >>>