BI-2 destabilizes HIV-1 cores during infection and Prevents Binding of CPSF6 to the HIV-1 Capsid

Retrovirology. 2014 Dec 11;11:120. doi: 10.1186/s12977-014-0120-x.

Abstract

Background: The recently discovered small-molecule BI-2 potently blocks HIV-1 infection. BI-2 binds to the N-terminal domain of HIV-1 capsid. BI-2 utilizes the same capsid pocket used by the small molecule PF74. Although both drugs bind to the same pocket, it has been proposed that BI-2 uses a different mechanism to block HIV-1 infection when compared to PF74.

Findings: This work demonstrates that BI-2 destabilizes the HIV-1 core during infection, and prevents the binding of the cellular factor CPSF6 to the HIV-1 core.

Conclusions: Overall this short-form paper suggests that BI-2 is using a similar mechanism to the one used by PF74 to block HIV-1 infection.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-HIV Agents / pharmacology*
  • Capsid / metabolism*
  • HIV-1 / drug effects*
  • HIV-1 / physiology*
  • Host-Pathogen Interactions / drug effects*
  • Protein Binding
  • Virus Replication / drug effects*
  • mRNA Cleavage and Polyadenylation Factors / antagonists & inhibitors*
  • mRNA Cleavage and Polyadenylation Factors / metabolism

Substances

  • Anti-HIV Agents
  • cleavage factor Im, human
  • mRNA Cleavage and Polyadenylation Factors