التفاصيل البيبلوغرافية
| العنوان: |
Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells |
| المؤلفون: |
Valente, Sergio1, Lepore, Ilaria2, Dell'Aversana, Carmela2,3, Tardugno, Maria1,4, Castellano, Sabrina4, Sbardella, Gianluca4, Tomassi, Stefano5, Di Maro, Salvatore5, Novellino, Ettore5, Di Santo, Roberto1, Costi, Roberta1, Altucci, Lucia2,3, Mai, Antonello1 antonello.mai@uniroma1.it |
| المصدر: |
Biochimie. Nov2012, Vol. 94 Issue 11, p2308-2313. 6p. |
| مصطلحات موضوعية: |
*LEUKEMIA, *CELL death, *ENZYME inhibitors, *GENETICS, *BIOCHEMISTRY, *CELL differentiation |
| مستخلص: |
Abstract: Chemical manipulations undertaken on some bis(bromo- and dibromo-phenol) compounds previously reported by us as wide-spectrum epigenetic inhibitors let us to identify bis (bromo- and dibromo-methoxyphenyl) derivatives highly selective for PR-SET7 and EZH2 (compounds 4, 5, 9, and 10). Western blot analyses were carried out in U937 cells to determine the effects of such compounds on the methyl marks related to the tested enzymes (H3K4me1, H3K9me2, H4H20me1, and H3K27me3). The 1,5-bis(3-bromo-4-methoxyphenyl)penta-1,4-dien-3-one 4 (EC50 vs EZH2 = 74.9 μM), tested in U937 cells at 50 μM, induced massive cell death and 28% of granulocytic differentiation, highlighting the potential use of EZH2 inhibitors in cancer. [Copyright &y& Elsevier] |
| قاعدة البيانات: |
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