Pricing updated 2019-03-21. Prices are subject to change without notice.
The protein p53, often called the ‘guardian of the genome,’ is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis.1,2 Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. MDM2, a key negative regulator of p53, which is over-expressed in many human tumors, functions by binding to and targeting p53 for proteasomal degradation. Nutlin-3 is a potent inhibitor of p53-MDM2 interaction.3 (−)-
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2. Lane, D.P., and Hupp, T.R. Drug discovery and p53 Drug Discovery Today 8(8), 347-355 (2003).
Vassilev, L.T., Vu, B.T., Graves, B., et al. In vivo activation of the p53 pathway by small-
Tovar, C., Rosinski, J., Filipovic, Z., et al. Small-
Jewett, K.A., Christian, C.A., Bacos, J.T., et al. Feedback modulation of neural network synchrony and seizure susceptibility by Mdm2-