A structure-based approach for targeting the HIV-1 genomic RNA dimerization initiation site

Biochimie. 2007 Oct;89(10):1195-203. doi: 10.1016/j.biochi.2007.03.003. Epub 2007 Mar 12.

Abstract

Dimerization of the genomic RNA is an important step of the HIV-1 replication cycle. The Dimerization Initiation Site (DIS) promotes dimerization of the viral genome by forming a loop-loop complex between two DIS hairpins. Crystal structures of the DIS loop-loop complex revealed an unexpected and strong similitude with the bacterial 16S ribosomal aminoacyl-tRNA site (A site), which is the target of aminoglycoside antibiotics. As a consequence of these structural and sequence similarities, the HIV-1 DIS also binds some aminoglycosides, not only in vitro, but also ex vivo, in lymphoid cells and in viral particles. Crystal structures of the DIS loop-loop in complex with several aminoglycoside antibiotics provide a detailed-view of the DIS/drug interaction and reveal some hints about possible modifications to increase the drug affinity and/or specificity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Aminoglycosides / metabolism
  • Base Sequence
  • Binding Sites
  • Dimerization
  • Genome, Viral*
  • HIV-1 / genetics*
  • HIV-1 / metabolism
  • Humans
  • Models, Biological
  • Nucleic Acid Conformation
  • RNA, Viral / chemistry
  • RNA, Viral / genetics*
  • RNA, Viral / metabolism

Substances

  • Aminoglycosides
  • RNA, Viral