technology
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Technology
Pyrrole-Imidazole Polyamides
Pyrrole-Imidazole Polyamides (PI-Polyamides) are synthetic molecules developed by mimicking the structures of natural antibiotics, netropsin and distamycin. They have simple structures consisting of N-methylpyrrole, N-methylimidazole, and -alanine connected by amide bonds. Hairpin-shaped PI-Polyamides are often used to design to bind to a specific target DNA sequence. Professor Hiroshi Sugiyama has researched PI-Polyamides for more than 20 years and possesses methods and know-hows for the synthesis and evaluation of the activities.
PI-Polyamides as ON/OFF Switch of genes
PI-Polyamides which bind to a recognition sequence of a transcription factor can inhibit the binding of the transcription factor to DNA in live cells and suppress the transcription of the gene activated by the transcription factor (OFF switch). Conjugation of a DNA alkylating reagent with PI-Polyamides enables to suppress transcription even if their target sequences are not a binding site of a transcription factor.
Professor Hiroshi Sugiyama has also succeeded to enhance expression levels of gene clusters by using PI-Polyamides conjugates with HDAC inhibitor, HAT activator, and bromodomain inhibitor of HAT (ON switch).