相关实验视频

Updated: Jul 15, 2025

Assays for Validating Histone Acetyltransferase Inhibitors

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

讨论组织分类和调节功能的基因素脱乙酶及其抑制剂的讨论

Han Han¹, Xue Feng², Ting He²

¹Department of Biochemistry and Molecular Biology, Shenyang Medical College, Shenyang City, P. R. China.

Chemical biology & drug design

|September 30, 2023

概括

基斯脱乙酶 (HDAC) 抑制剂是有前途的癌症药物. 本综述详细介绍了HDAC的分类,结构和功能,有助于合理设计用于癌症治疗的新型HDAC抑制剂.

科学领域:

生物化学生物化学
分子生物学分子生物学
药理学药理学是指药理学的学科.

背景情况:

通过蛋白质翻译后修改进行表观遗传调节是癌症化疗的关键.
基因组脱乙酶 (HDACs) 是恢复瘤学中的表观遗传平衡的关键药物标.
HDACs可去乙基化基因和非基因蛋白,调节各种生物过程.

研究的目的:

审查人类素脱乙酶 (HDACs) 的分类,结构和功能.
探索HDAC抑制剂的结构-活性关系.
提供对HDAC抑制剂的抑制机制和合理设计的见解.

主要方法:

对HDAC分类,结构和功能的现有文献的审查.
对HDAC及其抑制剂的结构信息的分析.
经FDA批准的HDAC抑制剂的分类基于它们的药理动力学部分.

主要成果:

人类HDACs的四个类别的详细分类和功能特征.
阐明HDAC子组之间的结构差异,解释抑制剂选择性.
在六种FDA批准的HDAC抑制剂中确定一种常见的药理动力学部分 (CAP,ZBG,Linker).
根据ZBG类型将抑制剂分为异胺酸,胺酸和循环类.

结论:

了解HDAC结构-功能和药模型对于阐明抑制机制至关重要.
结构洞察力促进了新型和选择性HDAC抑制剂的合理设计.
HDAC 抑制剂是一个重要的治疗策略,特别是在血液和一些固体瘤中.

关键词:

这是HDACICI.这就是HDACs.这是分类分类的分类.功能功能功能功能.药物动力学组是药物动力学组.结构效应关系是结构效应关系.

更多相关视频

Purification of H3 and H4 Histone Proteins and the Quantification of Acetylated Histone Marks in Cells and Brain Tissue

Purification of H3 and H4 Histone Proteins and the Quantification of Acetylated Histone Marks in Cells and Brain Tissue

Published on: November 30, 2018

Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates

Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates

Published on: February 27, 2016

相关概念视频

Histone Modification

Histone Modification

The histone proteins have a flexible N-terminal tail extending out from the nucleosome. These histone tails are often subjected to post-translational modifications such as acetylation, methylation, phosphorylation, and ubiquitination. Particular combinations of these modifications form “histone codes” that influence the chromatin folding and tissue-specific gene expression.
Acetylation
The enzyme histone acetyltransferase adds acetyl group to the histones. Another enzyme, histone...

Spreading of Chromatin Modifications

Spreading of Chromatin Modifications

The histone proteins in the nucleosomes are post-translationally modified (PTM) to increase or decrease access to DNA. The commonly observed PTMs are methylation, acetylation, phosphorylation, and ubiquitination of lysine amino acids in the histone H3 tail region. These histone modifications have specific meaning for the cell. Hence, they are called "histone code". The protein complex involved in histone modification is termed as "reader-writer" complex.
Writers
The writer...

Co-activators and Co-repressors

Co-activators and Co-repressors

Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...

Heterochromatin

Heterochromatin

The extent of chromatin compaction can be studied by staining chromatin using specific DNA binding dyes. Under the microscope, the dense-compacted regions that take up more dye are called heterochromatin. Heterochromatin is further classified into two forms – constitutive heterochromatin and facultative heterochromatin.
Constitutive heterochromatin: It is a highly compact region of chromatin that is mostly concentrated in the centromere and telomere. Unlike euchromatin, the amino acid at...

The Nucleosome Core Particle

The Nucleosome Core Particle

Nucleosomes are the DNA-histone complex, where the DNA strand is wound around the histone core. The histone core is an octamer containing two copies of H2A, H2B, H3, and H4 histone proteins.
Nucleosomes, paradoxically, perform two opposite functions simultaneously. On the one hand, their primary aim is to protect the delicate DNA strands from physical damage and help achieve a higher compaction ratio. On the other hand, they must allow polymerase enzymes to access histone-bound DNA during...

Inheritance of Chromatin Structures

Inheritance of Chromatin Structures

Epigenetics is the study of inherited changes in a cell's phenotype without changing the DNA sequences. It provides a form of memory for the differential gene expression pattern to maintain cell lineage, position-effect variegation, dosage compensation, and maintenance of chromatin structures such as telomeres and centromeres. For example, the structure and location of the centromere on chromosomes are epigenetically inherited. Its functionality is not dictated or ensured by the underlying...