Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
By S. Kubicek, Roderick J. O’Sullivan, E. August, E. Hickey, Qiang Zhang, Miguel L. Teodoro, S. Rea, K. Mechtler, J. Kowalski, C. Homon and 2 more. Molecules and Cells, 2007
831 citations recorded by the source corpus.
Subfields: Molecular Biology
View Paper: https://www.semanticscholar.org/paper/c9badc2a8b4b7e4c4c74d70f28091f2adbed12a4
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In Molecular Biology
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Citations in the corpus
- Overexpression of the JmjC histone demethylase KDM5B in human carcinogenesis: involvement in the proliferation of cancer cells through the E2F/RB pathway (2010, background): “In addition, some histone methyltransferase and demethylase inhibitors have recently been reported [27-29].”
- Enhanced expression of EHMT2 is involved in the proliferation of cancer cells through negative regulation of SIAH1. (2011, background): “reduces H3K9me2 levels at the chromatin regions of several EHMT2 target genes [28,29].”
- Epigenetic Modifications as Therapeutic Targets (2010, background): “Thus far, the most efficient inhibitor is BIX-01294, a diazepine-quinazoline-amine derivative that transiently reduces global H3K9me2 levels in several cell line”
- Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. (2008, methodology): “The synthesis and full characterization of compound BIX-01294 was as previously described (Kubicek et al., 2007), and Bayk8644 was purchased from EMD/Calbiochem Biochemical (San Diego, CA).”
- A combined chemical and genetic approach for the generation of induced pluripotent stem cells. (2008, positive): “We also found that the small molecule BIX-01294 (BIX), an inhibitor of the G9a histone methyltransferase (Kubicek et al., 2007), can improve the reprogramming efficiency in NPCs transduced with Oct3/4-Klf4 to a level comparable to transduction with all four factors; we obtained 12 ± 1.41 iPS cell…”
- Single-cell dynamics of genome-nuclear lamina interactions. (2013, methodology): “A similar effect was observed after treatment with BIX01294, an inhibitor of the HKMT activity of both G9a and GLP1 (Kubicek et al., 2007; Quinn et al., 2010) (Figure 6B).”
- Overexpression of LSD1 contributes to human carcinogenesis through chromatin regulation in various cancers (2011, background): “In addition, development of histone methyltransferase and demethylase inhibitors has recently been reported.(41,42) Bisguanidine and biguanide, polyamine analogues, may be the potential inhibitors for LSD1-dependent demethylation.”