Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells.

Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells.
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苯并氮杂恶黄素作为沉默调节蛋白抑制剂,在癌症干细胞中具有抗增殖特性

DOI:
10.1021/jm301115r
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发表时间:
2012
影响因子:
7.3
通讯作者:
A. Mai
A. Mai
中科院分区:
医学1区
文献类型:
--
作者:
D. Rotili;D. Tarantino;V. Carafa;C. Paolini;J. Schemies;M. Jung;G. Botta;S. Di Maro;E. Novellino;C. Steinkuhler;R. De Maria;P. Gallinari;L. Altucci;A. Mai

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最近,抑制sirtuins被认为是一种很有前途的抗癌策略。一些新的苯并去氮恶黄素(2a、2b和2d)被报道为SIRT1/2抑制剂,在人类U937白血病细胞中被赋予促凋亡特性,最重要的是,与原型MC2141(1)一起在来自结直肠癌和多形性胶质母细胞瘤患者的癌症干细胞中显示出抗增殖作用,这些患者已知具有高致瘤性,对传统癌症化疗耐药,至少部分导致癌症复发或复发。
Inhibition of sirtuins has recently been proposed as a promising anticancer strategy. Some of the new benzodeazaoxaflavins (2a,2b, and2d) here reported as SIRT1/2 inhibitors were endowed with pro-apoptotic properties in human U937 leukemia cells and, most importantly, together with the prototype MC2141 (1) displayed antiproliferative effects in cancer stem cells from patients with colorectal carcinoma and glioblastoma multiforme, known to be highly tumorigenic, resistant to conventional cancer chemotherapy, and responsible, at least in part, for cancer relapse or recurrence.
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