HIV-1 entry and its inhibition

Curr Top Microbiol Immunol. 2003:281:1-27. doi: 10.1007/978-3-642-19012-4_1.


Entry of HIV-1 virions into cells is a complex and dynamic process carried out by envelope (Env) glycoproteins on the surface of the virion that promote the thermodynamically unfavorable fusion of highly stable viral and target cell membranes. Insight gained from studies of the mechanism of viral entry allowed insight into the design of novel inhibitors of HIV-1 entry, several of which are now in clinical trials. This review highlights the mechanism by which viral and cellular proteins mediate entry of HIV-1 into permissive cells, with an emphasis on targeting this process in the design of novel therapies that target distinct steps of the entry process, including antagonizing receptor binding events and blocking conformational changes intimately involved in membrane fusion.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents / pharmacology*
  • Anti-HIV Agents / therapeutic use
  • CD4 Antigens / metabolism*
  • HIV Envelope Protein gp120 / therapeutic use
  • HIV Envelope Protein gp41 / therapeutic use
  • HIV Infections / prevention & control*
  • HIV-1 / drug effects*
  • HIV-1 / physiology
  • Humans
  • Membrane Fusion / drug effects*
  • Models, Biological
  • Receptors, CCR5 / metabolism
  • Receptors, CCR5 / therapeutic use
  • Receptors, CXCR4 / metabolism
  • Receptors, CXCR4 / therapeutic use
  • Receptors, Chemokine / metabolism


  • Anti-HIV Agents
  • CD4 Antigens
  • HIV Envelope Protein gp120
  • HIV Envelope Protein gp41
  • Receptors, CCR5
  • Receptors, CXCR4
  • Receptors, Chemokine