What is the mechanism of action of integrase strand-transfer 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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Answer

Answer

HIV integrase is responsible for the transport and attachment of proviral DNA to host-cell chromosomes, allowing transcription of viral proteins and subsequent assembly of virus particles. [72] Proviral integration involves 2 catalytic reactions, as follows:

  • 3'-processing in the host-cell cytoplasm to prepare proviral strands for attachment

  • Strand transfer whereby proviral DNA is covalently linked to cellular DNA

These agents competitively inhibit the strand transfer reaction by binding metallic ions in the active site. [73, 74]


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