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p53 Inhibitors
No.161(April 2014)
p53 (Also known as Trp53 in mice, TP53 in humans) is a tumor suppressor protein that is frequently inactivated in tumors.1) It has been revealed that inhibition of p53 can improve the reprogramming efficiency of human and mouse somatic cells.2-7) The protein has been focused on in the research field.8)
Pifithrins are inhibitors of p53. Pifithrin-α is a transcriptional inhibitor of p53 and rapidly converts to the condensation form, cyclic-pifithrin-α (1, also called pifithrin-β).9). Pifithrin-μ (2) was initially identified as a small-molecule inhibitor of the binding of p53 to mitochondria by reducing its affinity to antiapoptic proteins Bcl-xL and Bcl-2.10).
References
- 1)Assessing TP53 status in human tumours to evaluate clinical outcome
- 2)Two supporting factors greatly improve the efficiency of human iPSC generation
- 3)Suppression of Induced pluripotent stem cell generation by the p53-p21 pathway
- 4)The Ink4/Arf locus is a barrier for iPS reprogramming
- 5)Linking the p53 tumour suppressor pathway to somatic cell reprogramming
- 6)Immortalization eliminates a roadblock during cellular reprogramming into iPS cells
- 7)A p53-mediated DNA damage response limits reprogramming to ensure iPS cell genomic integrity
- 8)p53, Stem cells, and reprogramming: tumor suppression beyond guarding the genome
- 9)A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy
- 10)Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation
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