57148-23-9Relevant articles and documents
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
, p. 8700 - 8703 (2015)
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.
CTB-PI POLYAMIDE CONJUGATE FOR ACTIVATING EXPRESSION OF SPECIFIC GENE
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Paragraph 0110; 0111, (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
Novel urea protein tyrosine phosphatase 1B inhibitor, and preparation method, pharmaceutical composition and application thereof
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, (2017/01/09)
The invention relates to novel urea compounds with a structure as shown in a general formula I in the specification or pharmaceutically acceptable salts thereof, wherein the urea compounds and the pharmaceutically acceptable salts thereof can be used as a novel inhibitor of protein tyrosine phosphatase (PTP) 1B. The invention also relates to a pharmaceutical composition containing the compounds as shown in the general formula I or the pharmaceutically acceptable salts of the compounds. The compounds as shown in the general formula I or the pharmaceutically acceptable salts thereof have the effect of inhibiting the activity of the protein tyrosine phosphatase 1B (PTP1B), and can be applied in preparation of drugs capable of preventing and/or treating symptoms or diseases like hyperglycemia and type 2 diabetes.