What is the mechanism of action of chemokine receptor antagonists 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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The method by which HIV binds to CD4 cells and ultimately fuses with the host cell is a complex multistep process, which begins with binding of the gp120 HIV surface protein to the CD4 receptor. This binding induces a structural change that reveals the V3 loop of the protein. The V3 loop then binds with a chemokine coreceptor (principally either CCR5 or CXCR4), allowing gp41 to insert itself into the host cell and leading to fusion of the cell membranes.

Maraviroc is a small molecule that selectively and reversibly binds the CCR5 coreceptor, blocking the V3 loop interaction and inhibiting fusion of the cellular membranes. Maraviroc is active against HIV-1 CCR5 tropic viruses. It has no activity against CXCR4 tropic or dual/mixed tropic virus. [97]

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