Navigation Links
Researchers create drug to keep tumor growth switched off
Date:2/11/2010

A novel and rapid anti-cancer drug development strategy has resulted in a new drug that stops kidney and pancreatic tumors from growing in mice. Researchers at the Moores Cancer Center at the University of California, San Diego, have found a drug that binds to a molecular "switch" found in cancer cells and cancer-associated blood vessels to keep it in the "off" position.

"We locked the kinase switch in the off position in cancer and in tumor-associated blood vessels," which differs from the way current inhibitors attempt to block active kinases, said David Cheresh, PhD, professor and vice chair of pathology at the UCSD School of Medicine and the Moores UCSD Cancer Center, who led the work.

The new approach employs scaffold-based chemistry combined with supercomputer technology, allowing for rapid screening and development of drugs that are more selective for the tumor. The development and screening processes were used to identify potential drug candidates able to halt a growth signaling enzyme, or kinase, which can foster tumor blood vessel and tumor growth. According to the researchers, the novel approach may become a useful strategy in cancer drug development. The study appears online the week of February 8, 2010, in the Proceedings of the National Academy of Sciences.

In this "rational design approach," Cheresh and his co-workers used the supercomputer at the San Diego Supercomputer Center to custom-design molecules that stabilized the inactive forms of two similar kinases, PDGFRβ and B-RAF both of which are found to be activated in tumors and in blood vessels that feed tumors. Since PDGFRβ and B-RAF work cooperatively, keeping both turned off causes synergistic effects in tumors, according to Cheresh.

"We custom design a drug for a target that we know either plays a role in blood vessel angiogenesis or tumor invasion," said Cheresh. "By doing this on the computer screen and effectively locking the target in the off position, we can generate selective drugs that are expected to produce minimal side effects. Working with a series of chemical scaffolds, we are able to design specific interactions to fit certain targets in cancer cells."

They tested candidates for their effects on embryonic zebrafish blood vessels, which behave similarly to human cancer blood vessels. Molecules that blocked blood vessel growth in the fish were found to do the same in mice, and Cheresh hopes they will soon be tested in cancer patients.

The drug screen system has several advantages, Cheresh explained. Most standard screens test 400,000 candidates in test tubes to identify a single drug candidate. His group's screening method requires fewer than 100 compounds to be screened because they are rationally designed, look for specific types of targets, and use a zebrafish model, testing molecules in cells, tissues and organs for "physiological relevance." The zebrafish is a popular drug research model because it is transparent and the effects of drugs are easily monitored.

In addition, he said, the rational design approach provides drugs that are more selective, hitting desired targets and yielding fewer side effects.


'/>"/>

Contact: Steve Benowitz
sbenowitz@ucsd.edu
619-543-6163
University of California - San Diego
Source:Eurekalert

Related medicine news :

1. Researchers Who Discovered First Genes for Stuttering will Present Findings to the National Stuttering Association
2. Researchers discover new way to kill pediatric brain tumors
3. UH Case Medical Center researchers publish promising findings for advanced cervical cancer
4. Researchers map all the fragile sites of the yeast Saccharomyces cerevisiaes genome
5. UCSF Researchers Identify Regulator of Human Sperm Cells
6. Researchers find broad spectrum antiviral that fights multitude of viruses
7. Caregivers of ICU patients are collateral damage of critical illness, say Pitt researchers
8. Researchers fight world hunger by mapping the soybean genome
9. HIV researchers solve key puzzle after 20 years of trying
10. UC Davis researchers identify brain protein for synapse development
11. UCLA cancer researchers perform complete genomic sequencing of brain cancer cell line
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:10/13/2017)... , ... October 13, 2017 , ... Ellevate Network, the ... business to advocate for action towards gender equality at their inaugural Summit in New ... the globe, and reached a social audience of over 3 million. To watch the ...
(Date:10/13/2017)... ... 2017 , ... Talented host, actor Rob Lowe, is introducing ... new episode of "Success Files," which is an award-winning educational program broadcasted on ... subject in-depth with passion and integrity. , Sciatica occurs when the sciatic nerve ...
(Date:10/13/2017)... ... ... On The Brink”: the Christian history of the United States and the loss of ... William Nowers. Captain Nowers and his wife, Millie, have six children, ten grandchildren, ... Navy. Following his career as a naval aviator and carrier pilot, he spent ...
(Date:10/12/2017)... ... October 12, 2017 , ... Planet Fitness, one of the ... today its plans to open a flagship location in Covington, LA at 401 N. ... To Go store next to Office Depot in the Holiday Square shopping center. Its ...
(Date:10/12/2017)... ... October 12, 2017 , ... The American College of Medical ... Friedman, PhD, FACMI, during the Opening Session of AMIA’s Annual Symposium in Washington, D.C. ... honor of Morris F. Collen, a pioneer in the field of medical informatics, this ...
Breaking Medicine News(10 mins):
(Date:9/25/2017)... , Sept. 25, 2017  EpiVax, Inc., a ... design, and immune-engineering today announced the launch of ... development of personalized therapeutic cancer vaccines. EpiVax has ... exclusive access to enabling technologies to the new ... will lead EpiVax Oncology as Chief Executive Officer. ...
(Date:9/19/2017)... --  ZirMed Inc ., a recognized leader in cloud-based revenue ... been ranked #1 by its users for the seventh consecutive ... Survey. ZirMed was recognized as the top-ranked end-to-end revenue cycle ... over 200 beds and holds one of the longest #1 ... ...
(Date:9/12/2017)... , Sept. 12, 2017  Consumer reviews on the independent review ... as the number one company for hearing aids, ranking it higher ... other brands. ... Named #1 by Consumers For Hearing Aids ... Embrace Hearing is an online store that provides high performance, state-of-the-art, ...
Breaking Medicine Technology: