Pilot screening programme for small molecule activators of p53

TY - JOUR

T1 - Pilot screening programme for small molecule activators of p53

AU - Berkson, Rachel G.

AU - Hollick, Jonathan J.

AU - Westwood, Nicholas J.

AU - Woods, Julie A.

AU - Lane, David P.

AU - Lain, Sonia

N1 - dc.publisher: Wiley-Blackwell

PY - 2005

Y1 - 2005

N2 - 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.

AB - 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.

KW - Transcription

KW - Screening

KW - Cancer-therapeutics

U2 - 10.1002/ijc.20968

DO - 10.1002/ijc.20968

M3 - Article

SN - 0020-7136

VL - 115

SP - 701

EP - 710

JO - International Journal of Cancer

JF - International Journal of Cancer

IS - 5

ER -