Development of HIV protease inhibitor

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Development of HIV protease inhibitor

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Development of HIV protease inhibitor

The first HIV protease inhibitor, saquinavir, is a peptidomimetic hydroxyethylamine and was marketed in 1995. It is a transition state analogue of a native substrate of the protease. The observation that HIV-1 protease cleaves the sequences containing the dipeptides Tyr-Pro or Phe-Pro was the basic design criterion. Addition of the decahydroisoquinoline (DIQ) group was one of the most significant modifications that led to the discovery of saquinavir.

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