Rational design of novel HIV-1 entry inhibitors by RANTES engineering

Luca Vangelista, Massimiliano Secchi, Paolo Lusso

Research output: Contribution to journalReview articlepeer-review

39 Citations (Scopus)


The discovery that the CC chemokines RANTES, MIP-1α and MIP-1β act as potent natural inhibitors of HIV-1, the causative agent of AIDS, and the subsequent identification of CCR5 as a major virus coreceptor have triggered a wealth of basic and applied research approaches aimed at developing safe and effective viral entry inhibitors. Some of these efforts have focused on RANTES engineering with the goal of enhancing the antiviral activity of the native molecule while reducing or abrogating its inflammatory properties. The wavefront generated a decade ago is still on its course, with a flow of promising leads constantly emerging and being evaluated in preclinical studies. Here, we present an overview of this rapidly evolving field, highlighting the most important features of RANTES molecular architecture and structure-function relationships.

Original languageEnglish
Pages (from-to)3008-3015
Number of pages8
Issue number24
Publication statusPublished - Jun 6 2008


  • CCR5
  • Chemokine receptors
  • Chemokines
  • HIV-1
  • Inhibitors
  • Rational design

ASJC Scopus subject areas

  • Molecular Medicine
  • Immunology and Microbiology(all)
  • veterinary(all)
  • Public Health, Environmental and Occupational Health
  • Infectious Diseases

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