📜环己酮置于碘体系中,用 苯 作为反应溶剂,化学反应 54.0H,反应生成 2-(2-亚氨基-4,5,6,7-四氢苯并噻唑-3-基)-1-P-苯甲基乙酮氢溴酸盐 参考文献: Pifithrin Analogues And Methods Of Treating Rett Syndrome[fr] Analogues De Pifithrine Et Méthodes De Traitement Du Syndrome De Rett 标题: Pifithrin Analogues And Methods Of Treating Rett Syndrome[fr] Analogues De Pifithrine Et Méthodes De Traitement Du Syndrome De Rett 摘要:本文披露了pifithrin化合物,治疗雷特综合征的方法,包括脑融合器官样体,其中包括大脑皮层(cx)器官样体和神经节突起(ge)器官样体之间的融合,其中一个器官样体包括,基本上由或完全由在甲基-Cpg结合蛋白2(mecp2)基因中具有功能丧失突变的神经细胞,并且使用脑融合器官样体来筛选治疗,减少或抑制由mecp2突变引起的异常神经活动的候选化合物的方法.
专利号:WO-2011045374-A1 优先权日:2009-10-15 标 题 :Model-guided random assembly pcr for the synthesis of eukaryotic promoters 发明人:REIS YARA; RICHTER DANIELA; REICHENZELLER MICHAELA; IWAMOTO NAO; ZHU CHENCHEN; UCKELMANN HANNAH; EILS ROLAND; KEIENBURG JENS; HUNDESHAGEN PHILIPP; BERNARDO MARTI; BAUER TOBIAS; KRANZ ANNA-LENA; KOENIG RAINER; HEINEMANN TIM; MUGAHID DOUAA; VELTEN LARS; HAAS SIMON; HILLER CORINNA; BARTOSCHEK MICHAEL; RADEMACHER ANNE; MEYER HANNAH; KRAEMER STEPHEN; ZHAO BINGGING 权利人:DEUTSCHES KREBSFORSCH; UNIV RUPRECHT KARLS HEIDELBERG; REIS YARA; RICHTER DANIELA; REICHENZELLER MICHAELA; IWAMOTO NAO; ZHU CHENCHEN; UCKELMANN HANNAH; EILS ROLAND; KEIENBURG JENS; HUNDESHAGEN PHILIPP; BERNARDO MARTI; BAUER TOBIAS; KRANZ ANNA-LENA; KOENIG RAINER; HEINEMANN TIM; MUGAHID DOUAA; VELTEN LARS; HAAS SIMON; HILLER CORINNA; BARTOSCHEK MICHAEL; RADEMACHER ANNE; MEYER HANNAH; KRAEMER STEPHEN; ZHAO BINGGING 摘要:The current invention is concerned with a method for the manufacture of a polynucleotide comprising a synthetic promoter specifically controlled by at least one selected transcription factor, comprising a) determining the distance between the transcriptional start point and the binding site for said at least one transcription factor in a given number of promoters comprising at least one binding site for said at least one transcription factor, b) selecting a distance range comprising the distances determined in a) to occur most frequently, c) determining the accompanying transcription factors in a given number of promoters, d) selecting a suitable number of accompanying transcription factors determined in c) to occur most frequently, e) synthesizing the synthetic promoter by randomly assembling i) at least one binding site for each of the at least one transcription factor, ii) at least one binding site for each of the selected accompanying transcription factor(s), and iii) a suitable number of stuffer fragments and by arranging said randomly assembled binding sites in the distance range from the transcriptional start point selected in b). The invention is further concerned with a polynucleotide comprising the synthetic promoter manufactured by the method of the current invention, a vector comprising the polynucleotide of the current invention, and a cell comprising the polynucleotide or the vector of the current invention. Furthermore, the invention relates to a device for the manufacture of oligonucleotides suitable for manufacturing a synthetic promoter of the current invention and a device for the manufacture of the synthetic promoter of the current invention.
1: Wu A, Zhao C. Astilbin Induces Apoptosis in Oral Squamous Cell Carcinoma through p53 Reactivation and Mdm-2 Inhibition. Dokl Biochem Biophys. 2024 Aug 28. doi: 10.1134/S1607672924600374. Epub ahead of print. 15(1):7154. doi: 10.1038/s41467-024-51328-3. 4: Xia Y, Wang D, Zhao H, Meng T, Jiang Q, Pan Z, Wang G, An T, Li B, Bi S, Wang H, Lu J, Liu H, Lin H, Lin C, Zheng Q, Li D. Silencing of tropomodulin 1 inhibits acute myeloid leukemia cell proliferation and tumor growth by elevating karyopherin alpha 2-mediated autophagy. Pharmacol Res. 2024 Sep;207:107327. doi: 10.1016/j.phrs.2024.107327. Epub 2024 Jul 28. 45(8):947-953. doi: 10.1097/MAO.0000000000004271. Epub 2024 Aug 6. 13(13):1086. doi: 10.3390/cells13131086. 9: Wu E, Wu C, Jia K, Zhou S, Sun L. HSPA8 inhibitors augment cancer chemotherapeutic effectiveness via potentiating necroptosis. Mol Biol Cell. 2024 Aug 1;35(8):ar108. doi: 10.1091/mbc.E24-04-0194. Epub 2024 Jul 3.
合成参考文献
参考文献:10.1016/j.expneurol.2004.01.030 摘要:Leker RR, Aharonowiz M, Greig NH, Ovadia H. The role of p53-induced apoptosis in cerebral ischemia: effects of the p53 inhibitor pifithrin alpha. Exp Neurol. 2004 Jun;187(2):478–86. doi: 10.1016/j.expneurol.2004.01.030. 参考文献:10.1074/jbc.m403539200 摘要:Murphy PJ, Galigniana MD, Morishima Y, Harrell JM, Kwok RP, Ljungman M, Pratt WB. Pifithrin-alpha inhibits p53 signaling after interaction of the tumor suppressor protein with hsp90 and its nuclear translocation. J Biol Chem. 2004 Jul 16;279(29):30195–201. doi: 10.1074/jbc.m403539200. 参考文献:10.1021/jm060318n 摘要:Pietrancosta N, Moumen A, Dono R, Lingor P, Planchamp V, Lamballe F, Bähr M, Kraus JL, Maina F. Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: discovery of a highly potent in vivo inhibitor and its action mechanism. J Med Chem. 2006 Jun 15;49(12):3645–52. doi: 10.1021/jm060318n. 参考文献:10.1093/carcin/bgl098 摘要:Tyagi A, Singh RP, Agarwal C, Agarwal R. Silibinin activates p53-caspase 2 pathway and causes caspase-mediated cleavage of Cip1/p21 in apoptosis induction in bladder transitional-cell papilloma RT4 cells: evidence for a regulatory loop between p53 and caspase 2. Carcinogenesis. 2006 Nov;27(11):2269–80. doi: 10.1093/carcin/bgl098. 参考文献:10.1097/00029330-200803010-00009 摘要:YAN J, YANG X, CHEN C, HU Q, ZHAO J, SHI X, LUAN L, YANG L, QIN L, ZHOU C. Pifithrin-α reduces cerebral vasospasm by attenuating apoptosis of endothelial cells in a subarachnoid haemorrhage model of rat. Chinese Medical Journal. 2008 Mar;121(5):414–9. doi: 10.1097/00029330-200803010-00009.