LEDGF/p75-independent HIV-1 replication demonstrates a role for HRP-2 and remains sensitive to inhibition by LEDGINs

PLoS Pathog. 2012;8(3):e1002558. doi: 10.1371/journal.ppat.1002558. Epub 2012 Mar 1.

Abstract

Lens epithelium-derived growth factor (LEDGF/p75) is a cellular cofactor of HIV-1 integrase (IN) that interacts with IN through its IN binding domain (IBD) and tethers the viral pre-integration complex to the host cell chromatin. Here we report the generation of a human somatic LEDGF/p75 knockout cell line that allows the study of spreading HIV-1 infection in the absence of LEDGF/p75. By homologous recombination the exons encoding the LEDGF/p75 IBD (exons 11 to 14) were knocked out. In the absence of LEDGF/p75 replication of laboratory HIV-1 strains was severely delayed while clinical HIV-1 isolates were replication-defective. The residual replication was predominantly mediated by the Hepatoma-derived growth factor related protein 2 (HRP-2), the only cellular protein besides LEDGF/p75 that contains an IBD. Importantly, the recently described IN-LEDGF/p75 inhibitors (LEDGINs) remained active even in the absence of LEDGF/p75 by blocking the interaction with the IBD of HRP-2. These results further support the potential of LEDGINs as allosteric integrase inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing / genetics
  • Adaptor Proteins, Signal Transducing / metabolism*
  • Catalytic Domain
  • Gene Knockdown Techniques
  • Gene Silencing
  • HIV Integrase / metabolism*
  • HIV Integrase Inhibitors / pharmacology
  • HIV-1 / drug effects
  • HIV-1 / physiology*
  • Host-Pathogen Interactions
  • Humans
  • Intercellular Signaling Peptides and Proteins / metabolism*
  • Pentanoic Acids / pharmacology
  • Thiophenes / pharmacology
  • Transcription Factors / genetics
  • Transcription Factors / metabolism*
  • Virus Replication / drug effects
  • Virus Replication / genetics

Substances

  • Adaptor Proteins, Signal Transducing
  • HIV Integrase Inhibitors
  • Intercellular Signaling Peptides and Proteins
  • PSIP1 protein, human
  • Pentanoic Acids
  • Thiophenes
  • Transcription Factors
  • hepatoma-derived growth factor
  • ledgin 7
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1