Results 161 to 170 of about 141,545 (201)
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DNA methyltransferase inhibitor CDA-II inhibits myogenic differentiation
Biochemical and Biophysical Research Communications, 2012CDA-II (cell differentiation agent II), isolated from healthy human urine, is a DNA methyltransferase inhibitor. Previous studies indicated that CDA-II played important roles in the regulation of cell growth and certain differentiation processes. However, it has not been determined whether CDA-II affects skeletal myogenesis.
Zirong, Chen +9 more
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Interaction Between DNA/histone Methyltransferases and their Inhibitors
Current Medicinal Chemistry, 2014Epigenetic research has recently become one of the hotspots in the field of bioscience and drug design. DNA methylation and histone methylation serve a critical function in influencing gene expression and genome function. The inhibition of DNA and histone methyltransferases (DNMTs and HMTs) is a promising approach for the therapeutic treatment of ...
J, Hu +7 more
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[DNA methyltransferase inhibitors * histone deacetylase inhibitors].
Nihon rinsho. Japanese journal of clinical medicine, 2014Epigenetics is a cell intrinsic mechanism to maintain genomic integrity by modifying chromatin architecture independently of changes in heritable DNA sequences namely genetic code. Chromatin is composed of nucleosome cores, in which DNA(147bp) is wrapped around a core histone octamer(two each of histones H2A, H2B, H3 and H4), arranged in a "beads-on-a ...
Jiro, Kikuchi, Yusuke, Furukawa
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FLAVONES AND FLAVANONES DERIVATES AS DNA METHYLTRANSFERASES INHIBITORS
2011The present invention relates to a compound of formula (I) or its pharmaceutically acceptable salts, hydrates or hydrated salts or its polymorphic crystalline structures, racemates, diastereomers or enantiomers, for its use in the prevention and/or treatment of cancer, developmental diseases, neurodegenerative diseases or Trypanomiasis diseases by ...
Ceccaldi, A, +8 more
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DNA Methyltransferase Inhibitors in Myeloid Cancer
The Cancer Journal, 2017Abstract DNA methyltransferase inhibitors, so-called hypomethylating agents (HMAs), are the only drugs approved for the treatment of higher-risk myelodysplastic syndromes and are widely used in this context. However, it is still unclear why some patients respond to HMAs, whereas others do not.
Ørskov, Andreas Due, Grønbæk, Kirsten
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Molecular Modeling and Virtual Screening of DNA Methyltransferase Inhibitors
Current Pharmaceutical Design, 2013Inhibition of DNA methyltransferases (DNMTs) is a promising approach for the therapeutic treatment of cancer and other diseases. In this work, we review the recent progress on the molecular modeling and virtual screening toward the identification of key structural features associated with the enzyme inhibitory action of active compounds and to identify
José L, Medina-Franco, Jakyung, Yoo
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Advances in the computational development of DNA methyltransferase inhibitors
Drug Discovery Today, 2011DNA methylation is an epigenetic change that results in the addition of a methyl group at the carbon-5 position of cytosine residues. The process is mediated by DNA methyltransferases (DNMTs), a family of enzymes for which inhibition is a promising strategy for the treatment of cancer and other diseases.
José L, Medina-Franco +1 more
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Development of rationally designed DNA N6 adenine methyltransferase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2012A series of bisubstrate inhibitors for DNA N6 adenine methyltransferase (Dam) have been synthesized by linking an amine analogue of S-adenosylmethionine to an aryl moiety designed to probe the binding pocket of the DNA adenine base. An initial structure-activity relationship study has identified substituents that increase inhibitor potency to the ∼10 ...
Gerard, Hobley +5 more
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DNA methyltransferase inhibitors: an updated patent review (2012-2015)
Expert Opinion on Therapeutic Patents, 2016DNA methyltransferases (DNMTs), important enzymes involved in epigenetic regulation of gene expression, represent promising targets in cancer therapy. DNMT inhibitors (DNMTi), which can modulate the aberrant DNA methylation pattern in a reversible way via inhibiting DNMT activity, have attracted significant attention in recent years.This review ...
Pan, Xu +3 more
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DNA Methyltransferase-1 Inhibitors as Epigenetic Therapy for Cancer
Current Cancer Drug Targets, 2013DNA methylation is an epigenetic modification involved in gene expression regulation. In cancer, the DNA methylation pattern becomes aberrant, causing an array of tumor suppressor genes to undergo promoter hypermethylation and become transcriptionally silent.
Varinder, Singh +2 more
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