Inhibition of HIV-1 infection by a CCR5-binding cyclophilin from Toxoplasma gondii

Blood. 2003 Nov 1;102(9):3280-6. doi: 10.1182/blood-2003-04-1096. Epub 2003 Jul 10.

Abstract

The activation of murine dendritic cells by Toxoplasma gondii has recently been shown to depend on a parasite protein that signals through the chemokine receptor CCR5. Here we demonstrate that this molecule, cyclophilin-18 (C-18), is an inhibitor of HIV-1 cell fusion and infection with cell-free virus. T gondii C-18 efficiently blocked syncytium formation between human T cells and effector cells expressing R5 but not X4 envelopes. Neither human nor Plasmodium falciparum cyclophilins possess such inhibitory activity. Importantly, C-18 protected peripheral blood leukocytes from infection with multiple HIV-1 R5 primary isolates from several clades. C-18 bound directly to human CCR5, and this interaction was partially competed by the beta-chemokine macrophage inflammatory protein 1 beta (MIP-1 beta) and by HIV-1 R5 gp120. In contrast to several other antagonists of HIV coreceptor function, C-18 mediated inhibition did not induce beta-chemokines or cause CCR5 downmodulation, suggesting direct blocking of envelope binding to the receptor. These data support the further development of C-18 derivatives as HIV-1 inhibitors for preventing HIV-1 transmission and for postexposure prophylaxis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-HIV Agents / metabolism
  • Anti-HIV Agents / pharmacology
  • Binding, Competitive
  • Cyclophilins / metabolism
  • Cyclophilins / pharmacology*
  • Giant Cells / drug effects
  • HIV Envelope Protein gp120 / metabolism
  • HIV Infections / prevention & control*
  • Humans
  • Macrophages / cytology
  • Macrophages / virology
  • Protein Binding / drug effects
  • Protozoan Proteins / metabolism
  • Protozoan Proteins / pharmacology
  • Receptors, CCR5 / metabolism*
  • T-Lymphocytes / cytology
  • T-Lymphocytes / virology
  • Toxoplasma / chemistry*

Substances

  • Anti-HIV Agents
  • HIV Envelope Protein gp120
  • Protozoan Proteins
  • Receptors, CCR5
  • Cyclophilins