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UMass Medical School researchers receive $8.5M grant award to fight AIDS
Date:10/24/2007

that most of the currently used inhibitors protrude beyond the substrate envelope, and many mutations that cause drug resistance occur where the inhibitors protrude away from the substrates. Drug resistance occurs since mutations at these positions limit drug binding, but allow HIV-1 protease to continue to function by recognizing and cutting substrates, thereby permitting the virus to mature.

In 2006, expanding upon this work the investigators reported on a new strategy to reduce the probability of drug resistance, by designing and synthesizing novel inhibitors to fit within the substrate envelope. This strategy should greatly retard the occurrence of drug resistance as any mutation that would confer drug resistance would simultaneously impact substrate recognition, thereby preventing HIV protease from functioning. Thus inhibitors developed by this method should be more robust against resistance occurring. Confirming the validity of this strategy, the scientists have designed, synthesized and are evaluating a novel series of highly potent HIV protease inhibitors that appear promising against drug resistant variants of HIV protease.


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Contact: Kelly Bishop
kelly.bishop@umassmed.edu
508-856-2000
University of Massachusetts Medical School
Source:Eurekalert

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