Forum for Science, Industry and Business

Sponsored by:     3M 
Search our Site:

 

Map of substrate-kinase interactions may lead to more effective cancer drugs

28.03.2012
Later-stage cancers thrive by finding detours around roadblocks that cancer drugs put in their path, but a Purdue University biochemist is creating maps that will help drugmakers close more routes and develop better drugs.

Kinase enzymes deliver phosphates to cell proteins in a process called phosphorylation, switching a cellular function on or off. Irregularities in phosphorylation can lead to uncontrolled cell growth and are a hallmark of cancer.

Many successful cancer drugs are kinase inhibitors, which block the ability of a kinase to bind with a particular protein on the cell, stopping phosphorylation and the creation of cancer cells.

W. Andy Tao, a Purdue associate professor of biochemistry and member of the Purdue University Center for Cancer Research, said that in later stages of cancers, kinase-inhibiting drugs are ineffective because the kinases adapt, finding new protein targets and forming new cancer cells. He believes that creating maps of all the potential routes for cancer cell formation is a key to developing better cancer drugs.

"I would say that 99 percent of these drugs are effective for a few months in late-state cancers, and then the cancers develop resistance," said Tao, whose findings were published online early in the Proceedings of the National Academy of Sciences. "In the beginning, the cell cannot adjust and it dies. In later stages, the cells find a way. Cancer cells find a way to survive. You block one pathway, and they find another."

The kinase-protein maps Tao is creating identify kinases and the direct protein targets they phosphorylate. His method weeds out other proteins that are not direct targets, but are later phosphorylated as part of a cascade of reactions that begins when direct target proteins are phosphorylated.

Tao compared cells with and without kinases. The phosphoproteins present only when a kinase was present were considered possible targets. Further, the proteins were dephosphorylated, meaning the phosphate groups that had been added by kinases were removed.

The kinase was then re-introduced, and those proteins that accepted phosphate groups from the kinase were deemed direct targets of that kinase. With that information, drugmakers could tailor kinase-inhibiting drugs to ensure that the drug would stop kinases from reaching all potential targets, making the drugs more effective.

"If you understand the network, you can block all the pathways to cure the cancer," Tao said.
Tao's research findings focused on the SYK kinase, which is involved in leukemia and breast cancers. He plans to study other kinases, as well as mutated kinases, to understand whether they have different protein targets.

Tao collaborated with Robert Geahlen, a professor in medicinal chemistry and molecular pharmacology at Purdue. The National Institutes of Health funded the research.

Writer: Brian Wallheimer, 765-496-2050, bwallhei@purdue.edu
Source: Andy Tao, 765-494-9605, taow@purdue.edu
Ag Communications: (765) 494-2722;
Keith Robinson, robins89@purdue.edu
Agriculture News Page

Brian Wallheimer | EurekAlert!
Further information:
http://www.purdue.edu

More articles from Life Sciences:

nachricht The birth of a new protein
20.10.2017 | University of Arizona

nachricht Building New Moss Factories
20.10.2017 | Albert-Ludwigs-Universität Freiburg im Breisgau

All articles from Life Sciences >>>

The most recent press releases about innovation >>>

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

Im Focus: Neutron star merger directly observed for the first time

University of Maryland researchers contribute to historic detection of gravitational waves and light created by event

On August 17, 2017, at 12:41:04 UTC, scientists made the first direct observation of a merger between two neutron stars--the dense, collapsed cores that remain...

Im Focus: Breaking: the first light from two neutron stars merging

Seven new papers describe the first-ever detection of light from a gravitational wave source. The event, caused by two neutron stars colliding and merging together, was dubbed GW170817 because it sent ripples through space-time that reached Earth on 2017 August 17. Around the world, hundreds of excited astronomers mobilized quickly and were able to observe the event using numerous telescopes, providing a wealth of new data.

Previous detections of gravitational waves have all involved the merger of two black holes, a feat that won the 2017 Nobel Prize in Physics earlier this month....

Im Focus: Smart sensors for efficient processes

Material defects in end products can quickly result in failures in many areas of industry, and have a massive impact on the safe use of their products. This is why, in the field of quality assurance, intelligent, nondestructive sensor systems play a key role. They allow testing components and parts in a rapid and cost-efficient manner without destroying the actual product or changing its surface. Experts from the Fraunhofer IZFP in Saarbrücken will be presenting two exhibits at the Blechexpo in Stuttgart from 7–10 November 2017 that allow fast, reliable, and automated characterization of materials and detection of defects (Hall 5, Booth 5306).

When quality testing uses time-consuming destructive test methods, it can result in enormous costs due to damaging or destroying the products. And given that...

Im Focus: Cold molecules on collision course

Using a new cooling technique MPQ scientists succeed at observing collisions in a dense beam of cold and slow dipolar molecules.

How do chemical reactions proceed at extremely low temperatures? The answer requires the investigation of molecular samples that are cold, dense, and slow at...

Im Focus: Shrinking the proton again!

Scientists from the Max Planck Institute of Quantum Optics, using high precision laser spectroscopy of atomic hydrogen, confirm the surprisingly small value of the proton radius determined from muonic hydrogen.

It was one of the breakthroughs of the year 2010: Laser spectroscopy of muonic hydrogen resulted in a value for the proton charge radius that was significantly...

All Focus news of the innovation-report >>>

Anzeige

Anzeige

Event News

ASEAN Member States discuss the future role of renewable energy

17.10.2017 | Event News

World Health Summit 2017: International experts set the course for the future of Global Health

10.10.2017 | Event News

Climate Engineering Conference 2017 Opens in Berlin

10.10.2017 | Event News

 
Latest News

Terahertz spectroscopy goes nano

20.10.2017 | Information Technology

Strange but true: Turning a material upside down can sometimes make it softer

20.10.2017 | Materials Sciences

NRL clarifies valley polarization for electronic and optoelectronic technologies

20.10.2017 | Interdisciplinary Research

VideoLinks
B2B-VideoLinks
More VideoLinks >>>