卡洛芬类似物作为 SIRTUIN 抑制剂：酶和细胞研究。
Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies.
机构信息
Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, P.le A. Moro 5, 00185 Roma (Italy).
出版信息
ChemMedChem. 2012 Nov;7(11):1905-8. doi: 10.1002/cmdc.201200318.
PMID:24155041
Abstract
The best of both: SIRT1/2 inhibitors were developed by combining chemical features of selisistat (SIRT1-selective inhibitor; blue) and carprofen (anti-inflammatory drug; red). The most potent compound (shown) increased acetyl-p53 and acetyl-α-tubulin levels, and induced slight apoptosis at 50 μM in U937 cells, differently from selisistat and carprofen.
摘要
两者兼得
SIRT1/2 抑制剂是通过结合塞利昔他汀（SIRT1 选择性抑制剂；蓝色）和卡洛芬（抗炎药；红色）的化学特征开发的。最有效的化合物（如图所示）在 50μM 时增加了乙酰化 p53 和乙酰化 α-微管蛋白的水平，并在 U937 细胞中诱导轻微凋亡，与塞利昔他汀和卡洛芬不同。
Zotero 插件