Research Summary

Selected Publications

• 1. Nishigaya, Y.; Takase, S.; Sumiya, T.; Sato, T.; Niwa, H.; Sato, S.; Nakata, A.; Matsuoka, S.; Maemoto, Y.; Hashimoto, N.; Namie, R.; Honma, Umehara, T.; Shirouzu, M.; Koyama, H.; Yoshida, M.; Ito, A.; Shirai, F.
  "Structure-based development of novel substrate-type G9a inhibitors as epigenetic modulators for sickle cell disease treatment"
  Bioorg. Med. Chem. Lett., 110, 129856. (2024)
• 2. Shinjo, K.; Umehara, T.; Niwa, H.; Sato, S.; Katsushima, K.; Sato, S.; Wang, X.; Murofushi, Y.; Suzuki, M. M.; Koyama, H.; Kondo, Y.
  "Novel pharmacologic inhibition of lysine-specific demethylase 1 as a potential therapeutic for glioblastoma"
  Cancer Gene Therapy (2024)
  doi.org/10.1038/s41417-024-00847-8 Published online 11/05
• 3. Furutani, Y.; Hirano. Y.; Toguchi, M.; Higuchi, S.; Qin, X-Y.; Yanaka, K.; Sato-Shiozaki, Y.; Takahashi, M.; Sakai, M.; Kongpracha. P.; Suzuki, t.; Kobayashi, K.; Masaki, T.; Koyama, H.; Sekiya, K.; Otsuka, M.; Koike, K.; Kohara, M.; Kojima, S.; Kakeya, H.; Matsuura. T.
  "A small molecule iCDM-34 identified by in silico screening suppresses HBV DNA through activation of aryl hydrocarbon receptor"
  Cell Death Discovery, 9, 467. (2023)
• 4. Nishigaya, Y.; Takase, S.; Kikuzato, K.; Sato, T.; Niwa, H.; Sato, S.; Nakata, A.; Sonoda, T.; Hashimoto, N.; Namie, R.; Honma, T.; Umehara, T.; Shirouzu, M.; Koyama, H.; Yoshida, M.; Ito, A.; Shirai, F.
  "Discovery of novel substrate-competitive Lysine methyl transferase G9a inhibitors as anti-cancer agents"
  J. Med. Chem., 66(6), 4059-4085. (2023)
• 5. Takase, S.; Hiroyama, T.; Shirai, F.; Maemoto, Y.; Nakata, A.; Matsuoka, S.; Sonoda, T.; Niwa, H.; Sato, S.; Umehara, T.; Shirouzu, M.; Nishigaya, Y.; Sumiya, T.; Hashimoto, N.; Namie, R.; Usui, M.; Ohishi, T.; Ohba, S-I,; Kawada, M.; Hayashi, Y.; Harada, H.; Yamaguchi, T.; Shinkai, Y.; Nakamura, Y.; Yoshida, M.; Ito, A.
  "A specific G9a inhibitor unveils BGLT3 Inc RNA as a universal mediator of chemically induced fetal globin gene expression"
  Nature commun., Jan 14;23 (1):23. (2023)
• 6. Cho, N.; Kikuzato, K.; Futamura, Y.; Shimizu, T.; Hayase, H.; Kamisaka, K.; Takaya, D.; Yuki, H.; Honma, T.; Niikura, M.; Kobayashi, F.; Watanabe, N.; Osada, H.; Koyama, H.
  "New antimalarials identified by a cell-based phenotypic approach: Structure-activity relationships of 2,3,4,9- tetrahydro-1H--caroboline derivatives possessing a 2-((courmarin-5-yl)oxy)alkanoyl moiety"
  Bioorg. Med. Chem. Lett., 60, 128584. (2022)
• 7. Shibata, N.; Cho, N.; Koyama, H.; Naito, M.
  "Development of a degrader against oncogenic fusion protein FGFR3-TACCS3"
  Bioorg. Med. Chem. Lett., 60, 128584. (2022)
• 8. Koda, Y.; Sato, S.; Yamamoto, H.; Niwa, H.; Watanabe, H.; Watanabe, C.; Sato, T.; Nakamura, K.; Tanaka, A.; Shirouzu, M.; Honma, T.; Fukami, T.; Koyama, H.; Umehara, T.
  "Design and synthesis of tranylcypromine-derived LSD1 inhibitors with improved hERG and microsomal stability profiles"
  ACS Med. Chem. Lett., 13(5), 848. (2022)
• 9. Yamamoto, H.; Sakai, N.; Ohte, S.; Sato, T.; Sekimata, K.; Matsumoto, T.; Nakamura, K.; Watanabe, H.; Mishima-Tsumagari, C.; Tanaka, A.; Hashizume, Y.; Honma, T.; Katagiri, T.; Miyazono, K.; Tomoda, H.; Shirouzu, M.; Koyama, H.
  "Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva"
  Bioorg. Med. Chem. Lett., 28, 127858. (2021)
• 10. Shirai, F.; Mizutani, A.; Yashiroda, Y.; Tsumura, T.; Kano, Y.; Muramatsu, Y.; Chikada, T.; Yuki, H.; Niwa, H.; Sato, S.; Washizuka, K.; Koda, Y.; Mazaki, Y.; Jan, M-K.; Yoshida, H.; Nagamori, A.; Okue, M.; Watanabe, T.; Kitamura, K.; Shitara, E.; Honma, T.; Umehara, T.; Shirouzu, M.; Fukami, T.; Seimiya, H.; Yoshida, M.; Koyama, H.
  "Design and Discovery of an orally efficacious spiroindolinone-based tankyrase Inhibitor for the treatment of colon cancer."
  J. Med. Chem., 63, 4183-4204. (2020)

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