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Scripps Research scientists find two compounds that lay the foundation for a new class of AIDS drug
Date:2/3/2010

maller pieces.

Current HIV-protease drugs mimic the shape of certain regions of the HIV protein chain (i.e., the "cleavage sites") and bind to the active site in the hollow center of protease. Once this site is blocked by the drug, the protease is disabled, and HIV cannot make new infectious particles. Thus, protease drugs impede the spread of the HIV infection to other cells within a patient.

Perryman wanted to find out what was different about drug-resistant strains of the virusinformation that was not obvious from static pictures of the molecules. So, he conducted computer simulations of the movement of a particularly nasty multi-drug-resistant mutant strain of HIV (V82F/I84V).

The findings showed that the flaps of the drug-resistant protease molecule tended to be open more often than their standard counterparts, and they were also more flexible. While the anti-HIV drugs still fit into the active site binding pocket, more energy was needed to close the flaps than the drugs could muster. As a consequence, the drugs wouldn't stay in the binding site, and the pocket remained available for the HIV protein chain, which was still able to close the flaps and go on to create new infectious particles.

In their simulations, Perryman and his colleagues identified a potential solution to this problem. Like restraining the handle-end of a pair of scissors to keep the blades from opening too wide, a new type of drug might be able to bind to alternate sites on the sides of the protease, restraining the flaps from their ends and providing the current anti-HIV drugs enough help to close the flaps and disable the protease. Instead of blocking the protease's active site, these compounds would be "allosteric fragments," small molecule building blocks that shift the dynamics of the molecule so it prefers a different conformation (shape).

The plan sounded good in theory, but could it work in practice?

Putting Together the Pieces'/>"/>

Contact: Keith McKeown
kmckeown@scripps.edu
858-784-8134
Scripps Research Institute
Source:Eurekalert

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