Forum for Science, Industry and Business

Sponsored by:     3M 
Search our Site:

 

Novel anti-malarial drug candidate found by UT Southwestern researchers in multicenter study

26.05.2010
As part of a multicenter study, UT Southwestern Medical Center researchers have identified a series of chemical compounds that might serve as starting points for the identification of new classes of anti-malarial drugs.
“Malaria remains one of the most globally significant infectious diseases that we face,” said Dr. Margaret Phillips, professor of pharmacology at UT Southwestern and one of the senior authors of the study, which appears in the May 20 issue of Nature. Malaria affects about 40 percent of the world’s population and kills about a million people a year, she said. The parasite that causes the disease is spread by mosquito bites.

Researchers, including Dr. Margaret Phillips (right) and Farah El Mazouni, have collaborated to identify a series of chemical compounds that might serve as starting points for new classes of anti-malarial drugs. Drugs are the mainstay of malaria treatment, yet the parasite is notorious for developing drug resistance, which compromises current therapy.

Drugs are the mainstay of malaria treatment, yet the malaria parasite is notorious for developing drug resistance, which compromises current chemotherapy.

“Novel chemical compounds with anti-malarial activity represent a potent tool in the process of developing new drugs to treat this disease,” Dr. Phillips said.

The study, done in collaboration with Dr. Kiplin Guy of St. Jude Children’s Research Hospital in Memphis and other researchers, started with a “library” of 309,474 chemical compounds.

The researchers used a technique called high throughput screening, which allowed them to test thousands of compounds quickly to identify those with anti-malarial action.

“In addition, publishing the full set of identified compounds will maximize the chances for the most-promising candidates to move into large-scale drug development programs,” Dr. Phillips said.

The screen identified 1,152 compounds that killed the parasite. The researchers then followed up with further tests to determine the mechanism of action of the identified compounds, where possible.

Dr. Phillips and her group tested whether any of the identified compounds killed malaria parasites by inhibiting an enzyme necessary to make pyrimidine, an intermediate molecule for creating DNA. She discovered that three of the library’s compounds with anti-malarial activity blocked this enzyme. Two of those had similar chemical structures to a class of known compounds that she and her colleagues have been studying for possible drug development. The third compound previously was not known to target the enzyme.

“It looked very different from anything we knew about before,” she said.

Having a variety of anti-malarial drugs with different chemical structures and modes of action is important because different types of drugs are given together to slow the parasite from developing resistance, Dr. Phillips said.

In all, the researchers from the various centers found 172 compounds that are “reasonable starting points” for development of new types of drugs.

“We call the identified candidates ‘hits,’ but if any of them are going to become drugs, they’re going to have to undergo chemical modification,” Dr. Phillips said. “For instance, they may need to be altered chemically to enter the cell more easily, or to improve their pharmacology so they will be more effective in people.”

Farah El Mazouni, senior research associate in pharmacology at UT Southwestern, also participated in this study. In addition, the researchers used the UT Southwestern High Throughput System resource in the Department of Biochemistry.

Other participating researchers were from St. Jude Children’s Research Hospital; Griffith University in Australia; the University of Washington, Seattle; the University of Pennsylvania; GlaxoSmithKline; the University of California, San Francisco; Johns Hopkins Bloomberg School of Public Health; the University of Pittsburgh; Medicines for Malaria Venture, Switzerland; the Portland VA Medical Center; and Rutgers, The State University of New Jersey.

The study was funded by the National Institutes of Health, the Welch Foundation, the Medicines for Malaria Venture and other organizations.

Media Contact: Aline McKenzie
214-648-3404
aline.mckenzie@utsouthwestern.edu

Aline McKenzie | EurekAlert!
Further information:
http://www.utsouthwestern.edu

More articles from Life Sciences:

nachricht Bolstering fat cells offers potential new leukemia treatment
17.10.2017 | McMaster University

nachricht Ocean atmosphere rife with microbes
17.10.2017 | King Abdullah University of Science & Technology (KAUST)

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

Ocean atmosphere rife with microbes

17.10.2017 | Life Sciences

Neutrons observe vitamin B6-dependent enzyme activity useful for drug development

17.10.2017 | Life Sciences

NASA finds newly formed tropical storm lan over open waters

17.10.2017 | Earth Sciences

VideoLinks
B2B-VideoLinks
More VideoLinks >>>