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Drug Resistance

Structure-based phenotyping predicts HIV-1 protease inhibitor resistance

Published in Medical Letter on the CDC and FDA, September 21st, 2003

Structure-based phenotyping can predict HIV-1 protease inhibitor resistance.

"Mutations in HIV-1 drug targets lead to resistance and consequent therapeutic failure of antiretroviral drugs. Phenotypic resistance assays are time-consuming and costly, and genotypic rules-based interpretations may fail to predict the effects of multiple mutations. We have developed a computational procedure that rapidly evaluates changes in the binding energy of inhibitors to mutant HIV-1 PR variants," scientists in the United States report.

"Models of WT complexes were produced from crystal structures," said Mark D. Shenderovich and collaborators at Cengent Therapeutics...

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