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Tax protein of HTLV-1 inhibits CBP/p300-mediated transcription by interfering with recruitment of CBP/p300 onto DNA element of E-box or p53 binding site.人类嗜T淋巴细胞病毒1型(HTLV-1)的Tax蛋白通过干扰CBP/p300与E-box或p53结合位点的DNA元件的结合,抑制CBP/p300介导的转录。
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本文引用的文献

1
Direct inhibition of hypoxia-inducible transcription factor complex with designed dimeric epidithiodiketopiperazine.用设计的二聚体表二硫二肽抑制缺氧诱导因子复合物。
J Am Chem Soc. 2009 Dec 23;131(50):18078-88. doi: 10.1021/ja807601b.
2
Discovery of a small-molecule inhibitor of the KIX-KID interaction.KIX-KID相互作用的小分子抑制剂的发现。
Chembiochem. 2009 Nov 23;10(17):2721-4. doi: 10.1002/cbic.200900552.
3
Inhibition of ErbB2(Her2) expression with small molecule transcription factor mimics.用小分子转录因子模拟物抑制 ErbB2(Her2)表达。
Bioorg Med Chem Lett. 2009 Nov 1;19(21):6233-6. doi: 10.1016/j.bmcl.2009.08.090. Epub 2009 Sep 1.
4
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.新型氟灭酸类似物作为雄激素受体介导转录的抑制剂。
ACS Chem Biol. 2009 Oct 16;4(10):834-43. doi: 10.1021/cb900143a.
5
Amphipathic small molecules mimic the binding mode and function of endogenous transcription factors.两亲性小分子模拟内源性转录因子的结合模式和功能。
ACS Chem Biol. 2009 May 15;4(5):335-44. doi: 10.1021/cb900028j.
6
Wrenchnolol derivative optimized for gene activation in cells.为细胞中的基因激活而优化的扭体洛尔衍生物。
J Am Chem Soc. 2009 Apr 8;131(13):4774-82. doi: 10.1021/ja900669k.
7
Cell-permeable beta-peptide inhibitors of p53/hDM2 complexation.p53/hDM2 复合物形成的细胞穿透性β-肽抑制剂。
Chembiochem. 2009 Apr 17;10(6):990-3. doi: 10.1002/cbic.200900049.
8
Mapping the interactions of the p53 transactivation domain with the KIX domain of CBP.绘制p53反式激活结构域与CBP的KIX结构域之间的相互作用图谱。
Biochemistry. 2009 Mar 17;48(10):2115-24. doi: 10.1021/bi802055v.
9
FoxO1 mediates PTEN suppression of androgen receptor N- and C-terminal interactions and coactivator recruitment.FoxO1介导PTEN对雄激素受体N端和C端相互作用以及共激活因子募集的抑制作用。
Mol Endocrinol. 2009 Feb;23(2):213-25. doi: 10.1210/me.2008-0147. Epub 2008 Dec 12.
10
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy.MDM2-p53 蛋白-蛋白相互作用的小分子抑制剂以重新激活 p53 功能:一种癌症治疗的新方法。
Annu Rev Pharmacol Toxicol. 2009;49:223-41. doi: 10.1146/annurev.pharmtox.48.113006.094723.

转录开关:化学方法调控基因表达。

Transcriptional switches: chemical approaches to gene regulation.

机构信息

Department of Chemistry, University of Michigan, Ann Arbor, Michigan 48109, USA.

出版信息

J Biol Chem. 2010 Apr 9;285(15):11033-8. doi: 10.1074/jbc.R109.075044. Epub 2010 Feb 10.

DOI:10.1074/jbc.R109.075044
PMID:20147748
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2856975/
Abstract

Given the role of transcriptional misregulation in the pathogenesis of human disease, there is enormous interest in the development of molecules that exogenously control transcription in a defined manner. The past decade has seen many exciting advancements in the identification of molecules that mimic or inhibit the interactions between natural transcriptional activators and their binding partners. In this minireview, we focus on four activator.target protein complexes, highlighting recent advances as well as challenges in the field.

摘要

鉴于转录失调在人类疾病发病机制中的作用,人们对外源性以特定方式控制转录的分子的开发产生了巨大的兴趣。在过去的十年中,人们在鉴定模拟或抑制天然转录激活因子与其结合伙伴之间相互作用的分子方面取得了许多令人兴奋的进展。在这篇小综述中,我们重点介绍了四个激活剂-靶蛋白复合物,突出了该领域的最新进展和挑战。