Session1-2 Epigenetic Drug Discovery by Gene Switch

Shuji Ikeda　~ReguGene Co., Ltd.~

[Summary]

ReguGene Co., Ltd. is a pharmaceutical venture company founded on 3rd Sep 2018 by Professor Hiroshi Sugiyama at Graduate School of Science of Kyoto University and Professor Yasuhiko Kamikubo at Graduate School of Medicine of Kyoto University. Our aim is to supply medicine for intractable and rare diseases by developing DNA-targeting drugs utilizing cell permeable pyrrole-imidazole polyamides.
Pyrrole-Imidazole Polyamides (PI-Polyamides) are synthetic molecules developed by mimicking the structures of natural antibiotics, netropsin and distamycin. PI-Polyamides have simple structures consisting of N-methylpyrrole, N-methylimidazole, and β-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 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).
We possess PI-Polyamides libraries to regulate transcription. Our main pipeline is a RUNX inhibitor which shows anticancer and antimetastatic effects on various cancer cells. RUNX family transcription factors, RUNX1-3, take important roles in differentiation of blood and immune cells, formation of bone, and neurogenesis. The RUNX inhibitor binds to the DNA consensus sequence of RUNX1-3 and inhibits the binding of RUNX1-3 to DNA to activate or suppress transcription of RUNX-regulated genes.
We are looking for companies and/or investors to develop the RUNX inhibitor in cooperation. If you are interested in our PI-Polyamides libraries, please contact us via our homepage.

[Profile]

Ph.D. Managing Director of ReguGene Co., Ltd. and researcher at Chemistry Department, Graduate School of Kyoto University after working as assistant professor and researcher at university, national research institute, and venture company in Singapore.