Navigation Links
UCI team finds new target for treating wide spectrum of cancers
Date:1/31/2013

Irvine, Calif., Jan. 30, 2013 UC Irvine biologists, chemists and computer scientists have identified an elusive pocket on the surface of the p53 protein that can be targeted by cancer-fighting drugs. The finding heralds a new treatment approach, as mutant forms of this protein are implicated in nearly 40 percent of diagnosed cases of cancer, which kills more than half a million Americans each year.

In a study published online this week in Nature Communications, the UC Irvine researchers describe how they employed a computational method to capture the various shapes of the p53 protein. In its regular form, p53 helps repair damaged DNA in cells or triggers cell death if the damage is too great; it has been called the "guardian of the genome."

Mutant p53, however, does not function properly, allowing the cancer cells it normally would target to slip through control mechanisms and proliferate. For this reason, the protein is a key target of research on cancer therapeutics.

Within cells, p53 proteins undulate constantly, much like a seaweed bed in the ocean, making binding sites for potential drug compounds difficult to locate. But through a computational method called molecular dynamics, the UC Irvine team created a computer simulation of these physical movements and identified an elusive binding pocket that's open only 5 percent of the time.

After using a computer to screen a library of 2,298 small molecules, the researchers selected the 45 most promising to undergo biological assays. Among these 45 compounds, they found one, called stictic acid, that fits into the protein pocket and triggers tumor-suppressing abilities in mutant p53s.

While stictic acid cannot be developed into a viable drug, noted study co-leader Peter Kaiser, professor of biological chemistry, the work suggests that a comprehensive screening of small molecules with similar traits may uncover a usable compound that binds to this specific p53 pocket.

"The discovery and pharmaceutical development of such a compound could have a profound impact on cancer treatments," Kaiser said. "Instead of focusing on a specific form of the disease, oncologists could treat a wide spectrum of cancers, including those of the lung and breast." He added that there is currently one group of experimental drugs called Nutlins that stop p53 degradation, but they don't target protein mutations as would a drug binding to the newly discovered pocket.

The results are the culmination of years of labor by researchers with UC Irvine's Institute for Genomics & Bioinformatics and the Chao Family Comprehensive Cancer Center.

"It's been a large and complex multidisciplinary effort," said Richard Lathrop, professor of computer science and co-leader of the study. "We're working on the leading edge of what's possible, and a variety of skills and expertise is required to make progress. Hopefully, our research eventually will lead to drugs that target many different forms of cancer."


'/>"/>
Contact: Tom Vasich
tmvasich@uci.edu
949-824-6455
University of California - Irvine
Source:Eurekalert

Related medicine news :

1. People Can Emit Flu Germs in Air Up to 6 Feet Away, Study Finds
2. Early menopause may occur in women with BRCA gene, new study finds
3. Poll Finds Broad Support for Tougher Gun Laws
4. Study finds eating deep-fried food is associated with an increased risk of prostate cancer
5. University of Tennessee researcher finds first time could predict sexual satisfaction
6. Economic analysis finds penicillin, not "the pill," may have launched the sexual revolution
7. Smoking Still Takes a Heavy Toll in U.S., CDC Finds
8. Quitting Smoking Before Cancer Surgery Best, Study Finds
9. MD Anderson study finds qigong improves quality of life for breast cancer patients
10. Folic Acid Supplements Dont Affect Cancer Risk, Review Finds
11. Andrew Hawley of Vintage Rock Posters Finds Jimi Hendrix 1970 Sicks Stadium Seattle Concert Poster
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:10/13/2017)... PITTSBURGH, Pa. (PRWEB) , ... October 13, 2017 , ... ... the dark poses a problem. Fortunately, an inventor from Austin, Texas, has identified a ... access to medication in darkness or restricted lighting. As such, it eliminates the need ...
(Date:10/13/2017)... , ... October 13, 2017 ... ... of Pharmacy (SOP) alumni Hannah Randall, PharmD ‘17, and Jennifer Huggins, PharmD ... on guideline updates for the primary prevention of cardiovascular diseases during the ...
(Date:10/13/2017)... ... October 13, 2017 , ... The Visiting Nurse Association (VNA) of Somerset ... of specialty vendors and unique items from across the nation, this holiday-themed event will ... services offered by the VNA. The boutique will be open Saturday, November 4 ...
(Date:10/13/2017)... ... October 13, 2017 , ... Talented host, ... lowdown on sciatica in a new episode of "Success Files," which is an ... and innovation and investigates each subject in-depth with passion and integrity. , Sciatica ...
(Date:10/12/2017)... ... 12, 2017 , ... First Healthcare Compliance (FHC), an industry ... a range of technology and learning solutions at the 68th Annual American Healthcare ... be held October 14–18, 2017 at the Mandalay Bay Resort in Las Vegas, ...
Breaking Medicine News(10 mins):
(Date:10/12/2017)... , Oct. 12, 2017 West ... in innovative solutions for injectable drug administration, today announced ... the market opens on Thursday, October 26, 2017, and ... results and business expectations at 9:00 a.m. Eastern Time. ... or 253-336-8738 (International). The conference ID is 94093362. ...
(Date:10/11/2017)... Holdings, Inc. ("Hill-Rom") (NYSE: HRC), today provided an update ... Puerto Rico , where the company manufactures ... Following a comprehensive onsite assessment, the ... temporary loss of power and minimal water damage due ... have resumed, and the company expects to return to ...
(Date:10/5/2017)... ROSEMONT, Ill. , Oct. 5, 2017 /PRNewswire-USNewswire/ ... American Association of Oral and Maxillofacial Surgeons (AAOMS) ... than opioids – to be used as a ... post-surgical pain. ... relationship, the AAOMS White Paper "Opioid Prescribing: Acute ...
Breaking Medicine Technology: