A competitive inhibitor assay for SV40 T/pRB complex formation employing extracts of SV40-transformed human lung cells

In Vitro Cell Dev Biol Anim. 1993 Dec;29A(12):952-5. doi: 10.1007/BF02634234.

Abstract

Simian virus 40 (SV40) large T antigen (T), a potent dominant oncogene product, forms a specific complex with the human retinoblastoma protein (pRb), a cellular growth suppressor. We have used a recombinant pRb fusion protein (GST-Rb) in combination with extracts from a line of SV40-transformed human lung cells (WI-26 VA4) to develop a simple, non-radioactive assay to rapidly screen for competitive inhibitors of T/pRb binding. We illustrate the use of the assay by demonstrating that several short peptides containing the signature sequence, Leu-X-Cys-X-Glu, can inhibit T/pRb complex formation. In contrast, peptides containing the related motif, Leu-X-Glu-X-Glu, including two peptides derived from the transcription factor E2F, are inactive in this assay. These results show that Glu cannot substitute for Cys in the Leu-X-Cys-X-Glu motif. This assay will facilitate the identification of agents that are inhibitors of T/pRb complex formation and that might exert effects on cellular growth regulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antigens, Polyomavirus Transforming / analysis
  • Antigens, Polyomavirus Transforming / metabolism*
  • Binding, Competitive
  • Biological Assay
  • Blotting, Western
  • Cell Extracts / pharmacology*
  • Cell Line, Transformed
  • Chromatography, Affinity
  • Humans
  • Lung / cytology
  • Molecular Sequence Data
  • Oligopeptides / chemical synthesis
  • Oligopeptides / metabolism
  • Oligopeptides / pharmacology*
  • Protein Binding
  • Recombinant Fusion Proteins / metabolism
  • Retinoblastoma Protein / analysis
  • Retinoblastoma Protein / metabolism*

Substances

  • Antigens, Polyomavirus Transforming
  • Cell Extracts
  • Oligopeptides
  • Recombinant Fusion Proteins
  • Retinoblastoma Protein