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Epigenetic Regulation

Epigenetic Regulation

Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.

Epigenetic Regulation

Epigenetic Regulation

Epigenetic changes alter the physical structure of the DNA without changing the genetic sequence and often regulate whether genes are turned on or off. This regulation ensures that each cell produces only proteins necessary for its function. For example, proteins that promote bone growth are not produced in muscle cells. Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
X-chromosome...

Chromatin Immunoprecipitation- ChIP

Chromatin Immunoprecipitation- ChIP

Chromatin immunoprecipitation, or ChIP, is an antibody-based technique used to identify sites on DNA that bind to transcription factors of interest or histone proteins. It also helps determine the type of histone modifications such as acetylation, phosphorylation, or methylation.
Types of ChIP
ChIP can be divided into two types - X-ChIP and N-ChIP. X-ChIP involves in vivo cross-linking of histones and regulatory proteins to DNA, fragmenting the DNA by sonication, and isolating the protein-DNA...

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Updated: Feb 28, 2026

Epigenetic Engineering of K562 Cells: Dual-Vector Episomal Strategy for Stable Targeted DNA Methylation using dCas9-DNMT3A and -HDAC1 Fusion Proteins

Epigenetic Engineering of K562 Cells: Dual-Vector Episomal Strategy for Stable Targeted DNA Methylation using dCas9-DNMT3A and -HDAC1 Fusion Proteins

Published on: October 31, 2025

クリック・ケミストリーは,標的となるエピジェネティック・セラピーの臨床前評価を可能にする.

Dean S Tyler^1,2, Johanna Vappiani³, Tatiana Cañeque^4,5,6

¹Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, Victoria, Australia.

Science (New York, N.Y.)

|June 17, 2017

まとめ

この要約は機械生成です。

研究者は,分子プローブとして,クリック化学互換のBETブロモドメイン阻害剤を開発した. これらの探査はBRD4を明らかにした.

さらに関連する動画

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing

Published on: May 5, 2023

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors

Published on: August 5, 2022

関連する実験動画

Last Updated: Feb 28, 2026

Epigenetic Engineering of K562 Cells: Dual-Vector Episomal Strategy for Stable Targeted DNA Methylation using dCas9-DNMT3A and -HDAC1 Fusion Proteins

Epigenetic Engineering of K562 Cells: Dual-Vector Episomal Strategy for Stable Targeted DNA Methylation using dCas9-DNMT3A and -HDAC1 Fusion Proteins

Published on: October 31, 2025

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing

Published on: May 5, 2023

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors

Published on: August 5, 2022

科学分野:

エピジェネティクス
化学生物学
癌生物学

背景:

薬のメカニズムを理解することは新しい治療法の開発に不可欠です
BETブロモドメイン阻害剤は,がん治療における潜在的エピジェネティックベースの治療法である.
既存のBET阻害剤には,詳細なメカニズム研究のためのツールがない.

研究の目的:

BETブロモドメイン阻害剤の研究のための新しい分子探査機を開発する.
BRD4 (タンパク質4を含むブロモドメイン) の遺伝子調節機能を調査する.
BET阻害剤によって誘発された転写変化を in vivo で分析する.

主な方法:

クリック化学の互換性のためにBETブロモドメイン阻害剤の修正.
クリックプロテオミクスとクリックシーケンシングの応用
マウス白血病モデルにおける高解像度顕微鏡検査とフローサイトメトリーを用いて.

主要な成果:

BET 阻害剤の研究におけるクリック化学ベースのプローブの有用性を実証した.
BRD4の遺伝子調節作用とBET阻害剤による転写変化を明らかにした.
正常および悪性細胞における異質な薬物活性および差異的な分布を観察した.

結論:

エピジェネティック・ドラッグ・ディスカバリーのための多様な分子探査機を開発した.
BET阻害メカニズムと細胞効果についての洞察を提供した.
エピジェネティック・セラピーの臨床前評価の枠組みを確立した.