Analyses of anti-HIV type 1 activity of a small CCR5 peptide antagonist

AIDS Res Hum Retroviruses. 2011 Oct;27(10):1111-5. doi: 10.1089/AID.2010.0303. Epub 2011 Mar 31.


We have identified a small peptide (AFDWTFVPSLIL) that specifically binds to CC chemokine receptor 5 (CCR5) expressed on the Chinese hamster ovary (CHO) cell surface. Here, we further investigate its interaction with CCR5 on activated peripheral blood mononuclear cells (PBMCs), and determine whether the peptide inhibits HIV-1 infection mediated by CCR5 in PBMCs. The peptide antagonized the binding of CCR5 ligands, the second extracellular loop-specific monoclonal antibody (mAb) (2D7), regulated on activation of normal expressed and secreted T cells (RANTES), to PBMCs and blocked CCR5-mediated Ca(2+) signaling elicited by RANTES at a concentration of 10 μg/ml. Moreover, the peptide displayed selective inhibition of R5 HIV-1 replication. We conclude that the peptide is a CCR5 antagonist with anti-HIV-1 activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-HIV Agents / pharmacology*
  • CCR5 Receptor Antagonists*
  • CHO Cells
  • Calcium / metabolism
  • Chemokine CCL5 / pharmacology
  • Cricetinae
  • HIV-1 / drug effects*
  • HIV-1 / metabolism
  • HIV-1 / physiology
  • Humans
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • Leukocytes, Mononuclear / virology*
  • Microbial Sensitivity Tests
  • Peptides / chemical synthesis
  • Peptides / pharmacology*
  • Signal Transduction
  • Viral Load
  • Virus Attachment
  • Virus Replication


  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Chemokine CCL5
  • Peptides
  • Calcium