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Substrate Envelope-Based Design of New Dipeptide Isostere Cores for the Development of Protease Inhibitors against Drug-Resistant HIV-1

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Drug resistance is one of the major causes for HIV-infected patients to lose lives. An innovative HIV-1 protease inhibitor scaffold needs to be developed to resolve drug resistance issues. During this investigation, HIV-1 protease inhibitors based on a novel keto-hydroxyethylene core were designed and synthesized based on the substrate envelope theory. This core targets to overcome drug resistance to Amprenavir and Darunavir caused by I50V mutation in the protease. The results of florescence resonance energy transfer (FRET) assays indicate that the new inhibitor has moderate enzymatic inhibitory activities against HIV-1 protease. In the future, a variety of drug analogues will be developed based on this new core structure and might provide better therapies against drug-resistant HIV-1.

  • This report represents the work of one or more WPI undergraduate students submitted to the faculty as evidence of completion of a degree requirement. WPI routinely publishes these reports on its website without editorial or peer review.
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  • E-project-011411-142612
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  • 2011
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Date created
  • 2011-01-14
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