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Báo cáo khoa hoc:" CP-31398, a putative p53-stabilizing molecule tested in mammalian cells and in yeast for its effects on p53 transcriptional activity"

Tuyển tập báo cáo các nghiên cứu khoa học quốc tế ngành y học dành cho các bạn tham khảo đề tài: CP-31398, a putative p53-stabilizing molecule tested in mammalian cells and in yeast for its effects on p53 transcriptional activity | Journal of Negative Results in BioMedicine BioMed Central Research Open Access CP-31398 a putative p53-stabilizing molecule tested in mammalian cells and in yeast for its effects on p53 transcriptional activity Stefan Tanner and Alcide Barberis Address ESBATech AG Wagistrasse 21 CH-8952 Zurich-Schlieren Switzerland Email Stefan Tanner - tanner@esbatech.com Alcide Barberis - barberis@esbatech.com Corresponding author Published 17 November 2004 Received 08 March 2004 Accepted 17 November 2004 Journal of Negative Results in BioMedicine 2004 3 5 doi 10.1186 1477-5751-3-5 r This article is available from http www.jnrbm.com content 3 1 5 2004 Tanner and Barberis licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License http creativecommons.org licenses by 2.0 which permits unrestricted use distribution and reproduction in any medium provided the original work is properly cited. Abstract Background CP-31398 is a small molecule that has been reported to stabilize the DNA-binding core domain of the human tumor suppressor protein p53 in vitro. The compound was also reported to function as a potential anti-cancer drug by rescuing the DNA-binding activity and consequently the transcription activation function of mutant p53 protein in mammalian tissue culture cells and in mice. Results We performed a series of gene expression experiments to test the activity of CP-31398 in yeast and in human cell cultures. With these cell-based assays we were unable to detect any specific stimulation of mutant p53 activity by this compound. Concentrations of CP-31398 that were reported to be active in the published work were highly toxic to the human H1299 lung carcinoma and Saos-2 cell lines in our experiments. Conclusion In our experiments the small molecule CP-31398 was unable to reactivate mutant p53 protein. The results of our in vivo experiments are in agreement with the recently published biochemical analysis of .