Transcriptional Switches: Chemical Approaches to Gene Regulation*

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.

• Publication year

  2010

• Venue

  Journal of Biological Chemistry

• Publication date

  2010-02-10

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1074/jbc.R109.075044PMID 20147748PMCID PMC2856975
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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• A surface on the androgen receptor that allosterically regulates coactivator binding

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• Structural Details on mdm2-p53 Interaction*

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• Discovery of Small Molecule Inhibitors of the Interaction of the Thyroid Hormone Receptor with Transcriptional Coregulators*

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• In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2

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• Solution structure of the KIX domain of CBP bound to the transactivation domain of c-Myb.

  2004cited by this paper
• Identification of small-molecule antagonists that inhibit an activator: coactivator interaction.

  2004cited by this paper
• Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway.

  2004cited by this paper
• A small molecule transcriptional activation domain.

  2004cited by this paper
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  2003cited by this paper
• A gene-expression inhibitor that targets an alpha-helix-mediated protein interaction.

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• Recruitment of a 19S Proteasome Subcomplex to an Activated Promoter

  2002cited by this paper
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  2002cited by this paper
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  2002cited by this paper
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  2002cited by this paper
• Androgen receptor mutations and androgen insensitivity.

  2002cited by this paper
• The Gal4 Activation Domain Binds Sug2 Protein, a Proteasome Component, in Vivo and in Vitro *

  2001cited by this paper
• CREB-binding Protein and p300 in Transcriptional Regulation*

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  1999cited by this paper
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• Implementation and Optimization of an in vivo Photo-crosslinking Methodology to Define Direct Targets of Transcriptional Activators

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