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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...
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The organization of prokaryotic genes in their genome is notably different from that of eukaryotes. Prokaryotic genes are organized, such that the genes for proteins involved in the same biochemical process or function are located together in groups. This group of genes, along with their regulatory elements, are collectively known as an operon. The functional genes in an operon are transcribed together to give a single strand of mRNA known as polycistronic mRNA.
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Transcriptional attenuation occurs when RNA transcription is prematurely terminated due to the formation of a terminator mRNA hairpin structure.  Bacteria use these hairpins to regulate the transcription process and control the synthesis of several amino acids including histidine, lysine, threonine, and phenylalanine. Transcription attenuation takes place in the non-coding regions of mRNA.
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Updated: Nov 1, 2025

In Vitro Transcription Assays and Their Application in Drug Discovery
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Norstictic Acid Is a Selective Allosteric Transcriptional Regulator.

Julie M Garlick1,2, Steven M Sturlis1,2, Paul A Bruno1,2

  • 1Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109, United States.

Journal of the American Chemical Society
|June 17, 2021
PubMed
Summary

Norstictic acid blocks Med25-mediated transcription by targeting a dynamic loop, offering new therapeutic strategies. This discovery opens avenues for inhibiting protein-protein interactions (PPIs) in cancer, particularly triple-negative breast cancer.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Transcriptional protein-protein interactions (PPIs) are crucial for cellular processes, including stress response and motility.
  • Dysregulation of PPI networks, like those involving Med25, is linked to cancer development and metastasis.
  • Traditional binding sites on proteins like Med25 are large and lack topology, posing challenges for small-molecule inhibitor discovery.

Purpose of the Study:

  • To identify novel therapeutic strategies targeting Med25-mediated transcriptional regulation.
  • To explore alternative binding sites on Med25 for inhibitor development.
  • To investigate the potential of norstictic acid as an inhibitor of Med25-transcriptional activator PPIs.

Main Methods:

  • In vitro assays to assess the inhibitory activity of norstictic acid on Med25-transcriptional activator PPIs.
  • Cell culture experiments to evaluate the effects of norstictic acid on Med25-driven transcription.
  • Utilized a patient-derived model of triple-negative breast cancer for in vivo validation.

Main Results:

  • Norstictic acid effectively blocks Med25-transcriptional activator PPIs.
  • The natural product norstictic acid targets a unique, highly dynamic loop on Med25, distinct from canonical binding sites.
  • Norstictic acid modulates Med25-driven transcription both orthosterically and allosterically, impacting cancer cell behavior.
  • Demonstrated efficacy in a triple-negative breast cancer model.

Conclusions:

  • Med25 represents a promising therapeutic target for cancer treatment.
  • Structurally dynamic loops on proteins offer new opportunities for inhibitor discovery, even for challenging targets.
  • Norstictic acid serves as a valuable lead compound for developing novel anti-cancer therapeutics targeting PPIs.