What is the mechanism of action of fusion inhibitors (FIs) 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

Fusion inhibitors act extracellularly to prevent the fusion of HIV to the CD4 or other target cell. Enfuvirtide blocks the second step in the fusion pathway by binding to the HR1 region of glycoprotein 41 (gp41). This mechanism does not allow HR1 and HR2 to fold properly, thereby preventing the conformational change of gp41 required to complete the final step in the fusion process. [91, 92]


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