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Pilot screening programme for small molecule activators of p53
Author(s) -
Berkson Rachel G.,
Hollick Jonathan J.,
Westwood Nicholas J.,
Woods Julie A.,
Lane David P.,
Lain Sonia
Publication year - 2005
Publication title -
international journal of cancer
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.475
H-Index - 234
eISSN - 1097-0215
pISSN - 0020-7136
DOI - 10.1002/ijc.20968
Subject(s) - suppressor , small molecule , transcription factor , dna damage , cancer research , computational biology , biology , chemistry , dna , bioinformatics , cancer , genetics , gene
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.