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Regulation of gene expression by small molecules

Author

Listed:
  • Joel M. Gottesfeld

    (The Scripps Research Institute)

  • Laura Neely

    (The Scripps Research Institute)

  • John W. Trauger

    (California Institute of Technology)

  • Eldon E. Baird

    (California Institute of Technology)

  • Peter B. Dervan

    (California Institute of Technology)

Abstract

Small molecules that target specific DNA sequences have the potential to control gene expression. Ligands designed for therapeutic application must bind any predetermined DNA sequence with high affinity and permeate living cells. Synthetic polyamides containing N-methylimidazole and N-methylpyrrole amino acids have an affinity and specificity for DNA comparable to naturally occurring DNA-binding proteins1. We report here that an eight-ring polyamide targeted to a specific region of the transcription factor TFIIIA binding site interferes with 5S RNA gene expression in Xenopus kidney cells. Our results indicate that pyrrole-imida-zole polyamides are cell-permeable and can inhibit the transcription of specific genes.

Suggested Citation

  • Joel M. Gottesfeld & Laura Neely & John W. Trauger & Eldon E. Baird & Peter B. Dervan, 1997. "Regulation of gene expression by small molecules," Nature, Nature, vol. 387(6629), pages 202-205, May.
    • Handle: RePEc:nat:nature:v:387:y:1997:i:6629:d:10.1038_387202a0
    DOI: 10.1038/387202a0
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    Cited by:

    1. Maritere Uriostegui-Arcos & Steven T. Mick & Zhuo Shi & Rufuto Rahman & Ana Fiszbein, 2023. "Splicing activates transcription from weak promoters upstream of alternative exons," Nature Communications, Nature, vol. 14(1), pages 1-12, December.

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