Research Summary

Selected Publications

• 1. Shibata, N.; Cho, N.; Koyama, H.; Naito, N.
  "Development of a degrader against oncogenic fusion protein FGFR3-TACC3"
  Bioorg. Med. Chem. Lett., 60. 128584. (2022)
• 2. Cho, N.; Kikuzato, K.; Futamura, Y.; Shimuzu, 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-b-carboline derivatives possessing 2-((coumarin-5-yl)oxy)alkanoyl moiety"
  Bioorg. Med. Chem., 66, 116830. (2022)
• 3.Koda Y.; Sato S.; Yamamoto H.; Niwa H; Watanabe C.; Sato T; Watanabe H.; Nakamura K.; Tanaka A.; Shirouzu M.; Honma T.; Fukami T.; Koyama H.; Umehara T.
  "In silico design and synthesis of tranylcypromine-derived LSD1 inhibitors with improved hERG and microsomal stability profiles."
  ACS Med. Chem. Lett., 13, 848. (2022)
• 4. Yamamoto, H.; Sakai, N.; Ohte, S.; Sato, T.; Sekimata, K.; Matsumoto, T.; Nakamura, K.; Watanabe, H.; Mishima-Tsumagari, C.; Takaka, 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 progressive"
  Bioorg. Med. Chem. Lett., 28, 127858. (2021)
• 5. Nara, T.; Nakagawa, Y.; Tsuganezawa, K.; Yuki, H.; Sekimata, K.; Koyama, H.; Ogawa, N.; Honma, T.; Shirouzu, M.; Fukami, T.; Matsuo, Y.; Inaoka, D. K.; Kita, Y.; Tanaka, A.
  "The ubiquinone synthesis pathway is a promising drug target for Chagas disease"
  PLoS ONE, 16(2), e0243855. (2021)
• 6.Sekimata, K.; Sato, T.; Sakai, N.
  "ALK2: A Therapeutic Target for Fibrodysplasia Ossificans Progressiva and Diffuse Intrinsic Pontine Glioma."
  Chem. Pharm. Bull., 68(3) 194-200. (2020)
• 7. 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)
• 8.Sekimata, K.; Sato, T.; Sakai, N.; Watanabe, H.; Mishima-Tsumagari, C.; Taguri, T.; Matsumoto, T.; Fujii, Y.; Handa, N.; Honma, T.; Tanaka, A.; Shirouzu, M.; Yokoyama, S.; Miyazono, K.; Hashizume, Y.; Koyama, H.
  "Bis-Heteroaryl Pyrazoles: Identification of Orally Bioavailable Inhibitors of Activin Receptor-Like Kinase-2 (R206H)."
  Chem. Pharm. Bull., 67, 224–235. (2019)
• 9. Shirai, F.; Tsumura, T.; Yashiroda, Y.; Yuki, H.; Niwa, H.; Sato, S.; Chikada, T.; Koda, Y.; Washizuka, K.; Yoshimoto, N.; Abe, M.; Onuki, T.; Mazaki, Y.; Hirama, C.; Fukami, T.; Watanabe, H.; Honma, T.; Umehara, T.; Shirouzu, M.; Okue, M.; Kano, Y.; Watanabe, T.; Kitamura, K.; Shitara, E.; Muramatsu, Y.; Yoshida, H.; Mizutani, A.; Seimiya, H.; Yoshida, M; Koyama, H.
  "Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors."
  J. Med. Chem., 62(7), 3407-3427. (2019)
• 10. Tsuganezawa, K.; Sekimata, K.; Nakagawa, Y.; Utata, R.; Nakamura, K.; Ogawa, N.; Koyama, H.; Shirouzu, M.; Fukami, T.; Kita, K.; Tanaka, A.
  "Identification of small molecule inhibitors of human COQ7."
  Bioog. Med. Chem. , https://doi.org/10.1016/j.bmc.2019.115182. (2019)

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