CpG dinucleotide methylation of the CYP19 I.3/II promoter modulates cAMP-stimulated aromatase activity

AbstractStably silenced genes that display a high level of CpG dinucleotide methylation are refractory to the current generation of dCas9-based activation systems. To counter this, we created an improved activation system by coupling the catalytic domain of DNA demethylating enzyme TET1 with transcriptional activators (TETact). TETact induces transcription of heavily suppressed non-coding RNA and surface protein, and the reactivation of embryonic haemoglobin genes in non-erythroid cells.

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Reduced expression and increased CpG dinucleotide methylation of the rat APOBEC-1 promoter in transgenic rabbits

Biochimica et Biophysica Acta (BBA) - Gene Structure and Expression ◽

10.1016/s0167-4781(02)00412-8 ◽

2002 ◽

Vol 1577 (3) ◽

pp. 384-394 ◽

Cited By ~ 4

Author(s):

Frank Apostel ◽

Reinhard Dammann ◽

Gerd P Pfeifer ◽

Jobst Greeve

Keyword(s):

Transgenic Rabbits ◽

Cpg Dinucleotide ◽

Cpg Dinucleotide Methylation

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Rapid and Reversible Inhibition of Brain Aromatase Activity

Journal of Neuroendocrinology ◽

10.1046/j.1365-2826.2001.00598.x ◽

2001 ◽

Vol 13 (1) ◽

pp. 63-73 ◽

Cited By ~ 104

Author(s):

J. Balthazart ◽

M. Baillien ◽

G. F. Ball

Keyword(s):

Aromatase Activity ◽

Reversible Inhibition ◽

Brain Aromatase

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Phosphorylation Processes Controlling Aromatase Activity in Br east Cancer: An Update

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557516666160321113041 ◽

2016 ◽

Vol 16 (9) ◽

pp. 691-698 ◽

Cited By ~ 3

Author(s):

Stefania Catalano ◽

Ines Barone ◽

Stefania Marsico ◽

Rosalinda Bruno ◽

Sebastiano Andò

Keyword(s):

Aromatase Activity

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Assessment of the Aromatase Inhibitory Activity of Ma-Huang-Tang (MHT) and Its Active Compounds

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2019/4809846 ◽

2019 ◽

Vol 2019 ◽

pp. 1-9

Author(s):

Dong Ho Jung ◽

Joo Tae Hwang ◽

Bo-Jeong Pyun ◽

Song Yi Yu ◽

Byoung Seob Ko

Keyword(s):

Herbal Medicines ◽

Inhibitory Effect ◽

Aromatase Activity ◽

Cytochrome P450 Enzyme ◽

Active Components ◽

Glycyrrhizae Radix ◽

Potent Inhibition ◽

P450 Enzyme ◽

Medicine Prescription ◽

Ma Huang

Aromatase, a cytochrome P450 enzyme that converts androgens into estrogens, is an important drug target for hormone-dependent diseases. The purpose of this study was to elucidate the aromatase inhibitory effects of Ma-Huang-Tang (MHT), a traditional Korean herbal medicine prescription, and to identify its active ingredients. In this study, the inhibitory effect of MHT on aromatase activity was observed using dibenzylfluorescein (DBF) and KGN cells, and the dose-dependent effect of MHT was verified (IC50 values of 251 μg/mL and 246 μg/mL as determined by the two methods, respectively). Furthermore, among the six herbal medicines that constitute MHT, Ephedrae Herba, Cinnamomi Ramulus, and Glycyrrhizae Radix et Rhizoma showed the most potent inhibition of aromatase activity. Furthermore, upon identification of the active MHT compounds, three markers from Glycyrrhizae Radix et Rhizoma, liquiritin (5), liquiritin apioside (6), and liquiritigenin (7), were verified (IC50 values of 530 μM, 508 μM, and 1.611 mM and 499 μM, 522 μM, and 1.41 mM as determined by the two methods, respectively). In addition, their contents were confirmed to be 15.58, 19.80, and 2.22 mg/g, respectively, by HPLC/DAD analysis. These results indicate that the aromatase inhibitory effect of MHT results from the synergistic action of its active components and that MHT has potential as a preventive agent against aromatase activity.

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