80074-90-4Relevant academic research and scientific papers
CTB-PI POLYAMIDE CONJUGATE FOR ACTIVATING EXPRESSION OF SPECIFIC GENE
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Paragraph 0108; 0109, (2018/01/13)
The present invention provides: a histone modification control agent for activating expression of a specific gene, i.e., a complex including a histone acetylation enzyme activator useful as an agent for activating a specific gene, and a polyamide for reco
A Synthetic DNA-Binding Domain Guides Distinct Chromatin-Modifying Small Molecules to Activate an Identical Gene Network
Han, Le,Pandian, Ganesh N.,Chandran, Anandhakumar,Sato, Shinsuke,Taniguchi, Junichi,Kashiwazaki, Gengo,Sawatani, Yoshito,Hashiya, Kaori,Bando, Toshikazu,Xu, Yufang,Qian, Xuhong,Sugiyama, Hiroshi
supporting information, p. 8700 - 8703 (2015/11/27)
Synthetic dual-function ligands targeting specific DNA sequences and histone-modifying enzymes were applied to achieve regulatory control over multi-gene networks in living cells. Unlike the broad array of targeting small molecules for histone deacetylases (HDACs), few modulators are known for histone acetyltransferases (HATs), which play a central role in transcriptional control. As a novel chemical approach to induce selective HAT-regulated genes, we conjugated a DNA-binding domain (DBD) "I" to N-(4-chloro-3-trifluoromethyl-phenyl)-2-ethoxy-benzamide (CTB), an artificial HAT activator. In vitro enzyme activity assays and microarray studies were used to demonstrate that distinct functional small molecules could be transformed to have identical bioactivity when conjugated with a targeting DBD. This proof-of-concept synthetic strategy validates the switchable functions of HDACs and HATs in gene regulation and provides a molecular basis for developing versatile bioactive ligands.
