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本文引用的文献

1
Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7.基于结构导向的多梳抑制蛋白CBX7染色质结构域选择性拮抗剂的发现
ACS Med Chem Lett. 2016 Feb 29;7(6):601-5. doi: 10.1021/acsmedchemlett.6b00042. eCollection 2016 Jun 9.
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Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb Family.选择性抑制CBX6:一种多梳家族中的甲基赖氨酸读取蛋白。
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A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.一种靶向多梳抑制复合物1染色质结构域的细胞化学探针。
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Peptide-based inhibitors of protein-protein interactions.基于肽的蛋白质-蛋白质相互作用抑制剂。
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Regulation of gene transcription by Polycomb proteins.多梳蛋白对基因转录的调控。
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Chemical Inhibitors of Epigenetic Methyllysine Reader Proteins.表观遗传甲基赖氨酸识别蛋白的化学抑制剂
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Chemical basis for the recognition of trimethyllysine by epigenetic reader proteins.表观遗传阅读蛋白识别三甲基赖氨酸的化学基础。
Nat Commun. 2015 Nov 18;6:8911. doi: 10.1038/ncomms9911.
8
Unlocking the potential of chemical probes for methyl-lysine reader proteins.挖掘化学探针在甲基赖氨酸识别蛋白方面的潜力。
Future Med Chem. 2015;7(14):1831-3. doi: 10.4155/fmc.15.119. Epub 2015 Sep 22.
9
The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer.L3MBTL3 甲基赖氨酸识别结构域以二聚体形式发挥作用。
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The promise and peril of chemical probes.化学探针的前景与风险
Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867.

用于甲基赖氨酸识别结构域的化学探针。

Chemical probes for methyl lysine reader domains.

作者信息

James Lindsey I, Frye Stephen V

机构信息

Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, 125 Mason Farm Road, Marsico Hall, UNC-Chapel Hill, NC 27599-7363, United States.

Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, 125 Mason Farm Road, Marsico Hall, UNC-Chapel Hill, NC 27599-7363, United States.

出版信息

Curr Opin Chem Biol. 2016 Aug;33:135-41. doi: 10.1016/j.cbpa.2016.06.004. Epub 2016 Jun 25.

DOI:10.1016/j.cbpa.2016.06.004
PMID:27348158
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5018434/
Abstract

The primary intent of a chemical probe is to establish the relationship between a molecular target, usually a protein whose function is modulated by the probe, and the biological consequences of that modulation. In order to fulfill this purpose, a chemical probe must be profiled for selectivity, mechanism of action, and cellular activity, as the cell is the minimal system in which 'biology' can be explored. This review provides a brief overview of progress towards chemical probes for methyl lysine reader domains with a focus on recent progress targeting chromodomains.

摘要

化学探针的主要目的是建立分子靶点(通常是一种其功能可被探针调节的蛋白质)与该调节作用的生物学后果之间的关系。为了实现这一目的,必须对化学探针的选择性、作用机制和细胞活性进行分析,因为细胞是能够探索“生物学”的最小系统。本综述简要概述了针对甲基赖氨酸识别结构域的化学探针的研究进展,重点关注靶向色域结构域的最新进展。