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Novel anti-malarial drug candidate found by UT Southwestern researchers
Date:5/25/2010

DALLAS May 25, 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.

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 c
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Contact: Aline McKenzie
aline.mckenzie@utsouthwestern.edu
214-648-3404
UT Southwestern Medical Center
Source:Eurekalert

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