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Inhibition of Hypoxia‐Induced Gene Transcription by Substituted Pyrazolyl Oxadiazoles: Initial Lead Generation and Structure–Activity Relationships 下载免费PDF全文
Dr. Michael Härter Dr. Karl‐Heinz Thierauch Dr. Stephen Boyer Dr. Ajay Bhargava Dr. Peter Ellinghaus Dr. Hartmut Beck Dr. Kerstin Unterschemmann 《ChemMedChem》2014,9(1):61-66
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Dr. Jeffrey W. Johannes Christopher R. Denz Nancy Su Allan Wu Anna C. Impastato Dr. Scott Mlynarski Jeffrey G. Varnes D. Bryan Prince Dr. Justin Cidado Ning Gao Dr. Malcolm Haddrick Natalie H. Jones Shaobin Li Xiuwei Li Yang Liu Dr. Toan B. Nguyen Dr. Nichole O'Connell Dr. Emma Rivers Dr. Daniel W. Robbins Ronald Tomlinson Dr. Tieguang Yao Xiahui Zhu Dr. Andrew D. Ferguson Dr. Michelle L. Lamb Dr. John I. Manchester Dr. Sylvie Guichard 《ChemMedChem》2018,13(3):231-235
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Chemical Modification of a Synthetic Small Molecule Boosts Its Biological Efficacy against Pluripotency Genes in Mouse Fibroblasts 下载免费PDF全文
Abhijit Saha Dr. Ganesh N. Pandian Shinsuke Sato Junichi Taniguchi Yusuke Kawamoto Kaori Hashiya Dr. Toshikazu Bando Prof. Dr. Hiroshi Sugiyama 《ChemMedChem》2014,9(10):2374-2380
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传统的微生物代谢工程主要是通过过表达或敲除关键基因来实现产物产量最大化,但会造成代谢流失衡,生产效能降低。而对微生物代谢途径进行动态调控可维持细胞生长,平衡代谢流,提高生产效率。本文根据信号分子的来源不同,将微生物在转录水平的动态调控分为两种:一种是在光、温度、化学诱导剂的外源信号刺激下,利用响应该信号的启动子等元件调控下游代谢途径的人工诱导动态调控;另一种为在胞内代谢物水平或细胞密度改变的内源信号感应下,利用启动子、转录因子、核糖核酸开关调节关键基因的细胞自主诱导动态调控。本文同时介绍了转录水平动态调控策略在微生物代谢工程中的应用实例,以期对代谢途径的多个基因实现连续动态表达以及适配表达,有效提高目标产物的产量。 相似文献
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3‐(2‐Oxoethylidene)indolin‐2‐one Derivatives Activate Nrf2 and Inhibit NF‐κB: Potential Candidates for Chemoprevention 下载免费PDF全文
Dr. Amrita A. Nagle Dr. Shridhivya A. Reddy Dr. Helene Bertrand Dr. Hisashi Tajima Dr. Truong‐Minh Dang Dr. Siew‐Cheng Wong Prof. John D. Hayes Dr. Geoffrey Wells Dr. Eng‐Hui Chew 《ChemMedChem》2014,9(8):1763-1774
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Dr. Patricia García‐Domínguez Mélanie Weiss Ilaria Lepore Prof. Dr. Rosana Álvarez Prof. Dr. Lucia Altucci Prof. Dr. Hinrich Gronemeyer Prof. Dr. Ángel R. de Lera 《ChemMedChem》2012,7(12):2101-2112
A novel epigenetic modulator that displays a DNMT1 inhibition and DNMT3A activation profile was characterized (compound 8 ). This compound is a derivative of palmitic acid that incorporates the putative reactive functional group (diynone) of the peyssonenyne natural products. Other analogues containing the diynone or an acetoxyenediyne did not show the same biological profile. In U937 human leukemia cells, diynone 8 induced cell differentiation and apoptosis, which correlated with the expression of Fas protein. Very surprisingly, diynone 8 was toxic to normal human fibroblasts (BJ) and mouse embryo fibroblasts (MEF), but not to immortalized human fibroblasts (BJEL); this unique effect was not observed with the classical DNMT inhibitor 5‐azacytidine. Therefore, compound 8 interferes in a very specific manner with signaling pathways, the activities of which differ between normal and immortalized cell types. This toxicity is reminiscent of the effects of Dnmt1 ablation on mouse fibroblasts. In fact, some of the genes deregulated by the loss of Dnmt1 are similarly deregulated by 8 , but not by the DNMT inhibitor SGI‐1027. 相似文献