Rutgers researchers discover new drugs with potent anti-HIV action
December 16 2004 1:00 AM ET
Researchers at Rutgers University have developed a trio of drugs they believe can destroy HIV, according to a published report. The drugs, called diarylpyrimidines (DAPYs), mimic the virus by changing shape, which enables them to interfere with the way HIV attacks the immune system. Tests conducted in conjunction with Johnson and Johnson have shown the drugs to be easily absorbed with minimal side effects. They also can be taken in one pill, in contrast to the multidrug cocktails currently taken by many HIV patients.
A research team led by Rutgers chemist Eddy Arnold prepublished details of the most promising of the three drugs, known as R278474, last month in the electronic edition of the Journal of Medicinal Chemistry. Full details will be published in the journal in early 2005. Arnold, 47, has worked at dismantling HIV over the last 20 years. He uses X-ray crystallography, a technique to determine the structure of molecules, the smallest particles that can retain all the characteristics of an element or compound.
The research has targeted reverse transcriptase, a submiscroscopic protein composed of two coiled chains of amino acids. It is considered HIV's key protein. "Reverse transcriptase is very important in the biology of AIDS," said Stephen Smith, head of the department of infectious diseases at Saint Michael's Medical Center in Newark, N.J. "If you can really inhibit reverse transcriptase, you can stop AIDS."
The optimism about R278474 stems from its potential to interfere with an enzyme that the virus needs to copy and insert itself into a human cell. "We're onto something very, very special," Arnold said.
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