Pilot screening programme for small molecule activators of p53

R G Berkson, J J Hollick, N J Westwood, J A Woods, D P Lane, S Lain

Research output: Contribution to journalArticlepeer-review

38 Citations (Scopus)

Abstract

Activation of the p53 tumour suppressor is predicted to have therapeutically beneficial effects. Many current anti-cancer therapies activate the p53 response via DNA damage. Non-genotoxic activation of the p53 pathway would open the way to long-term and possibly prophylactic treatments. We have established a simple protocol to screen small compound libraries for activators of p53-dependent transcription, and to select and characterise the most interesting hits, which include non-genotoxic activators. These compounds or their derivatives are of potential clinical interest. This approach may also lead to the identification of novel p53-activating compound families and possibly to the description of novel molecular pathways regulating p53 activity. © 2005 Wiley-Liss, Inc.

Original languageEnglish
Pages (from-to)701-710
Number of pages10
JournalInternational Journal of Cancer
Volume115
DOIs
Publication statusPublished - 10 Jul 2005

Keywords

  • p53
  • transcription
  • screening
  • cancer-therapeutics
  • DNA-DAMAGE
  • IN-VIVO
  • TRANSCRIPTIONAL ACTIVITY
  • NEUROBLASTOMA-CELLS
  • ANTITUMOR AGENTS
  • APOPTOSIS
  • FIBROBLASTS
  • INHIBITOR
  • PROTEIN
  • CANCER

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