What is the mechanism of action of protease inhibitors in antiretroviral therapy of HIV infection?

Updated: Apr 18, 2019
  • Author: R Chris Rathbun, PharmD, BCPS (AQ-ID), AAHIVP; Chief Editor: John Bartlett, MD  more...
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HIV protease is a 99-amino-acid, aspartic acid protein and is responsible for maturation of virus particles late in the viral life cycle. HIV protease systematically cleaves individual proteins from the gag and gag -pol polypeptide precursors into functional subunits for viral capsid formation during or shortly after viral budding from an infected cell.

HIV protease inhibitors function as competitive inhibitors that directly bind to HIV protease and prevent subsequent cleavage of polypeptides. [42] They exhibit activity against clinical isolates of both HIV-1 and HIV-2. [42]

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