Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors

Bioorg Med Chem. 2003 Jul 3;11(13):2663-76. doi: 10.1016/s0968-0896(03)00161-5.


This review addresses key pharmacology and virology issues relevant in discovery and development of CCR5 antagonists as anti-HIV drugs, such as target validation, receptor internalization, allosterism, viral resistance and tropism. Recent progress in the discovery and development of CCR5 antagonists, SAR and clinical status are reviewed. Finally, modeling-based structure of CCR5 is discussed in the context of a small-molecule antagonism of the CCR5 receptor.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / pharmacology
  • Binding, Competitive
  • CCR5 Receptor Antagonists*
  • Humans
  • Ligands
  • Models, Molecular
  • Receptors, CCR5 / physiology
  • Structure-Activity Relationship


  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Ligands
  • Receptors, CCR5