RIKEN Center for Sustainable Resource Science Drug Discovery Platforms Cooperation Division

Division Director: Minoru Yoshida (D.Agr.)

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Research Summary

Recent rapid advances in decoding vast amounts of genomic information have revealed numerous new drug-discovery targets. To maximize the application and utilization of this information born from such brilliant basic research achievements, developing new technologies and evaluation methods to connect it to actual medical practice is essential. This is becoming the next challenge for many life scientists. Academic drug discovery—research conducted by universities and public research institutes—is a global trend. RIKEN aims to accelerate this through its Drug Discovery and Medical Technology Platform Program (DMP), providing RIKEN's outstanding scientific and technological capabilities as a platform. As a member of the DMP, our division contributes to academic drug discovery by providing a platform with a diverse natural/synthetic compound library, appropriate assay systems and instrumentation for high-throughput screening, and structural optimization through exceptional medicinal chemistry.

Main Research Fields

Biology

Related Research Fields

Chemistry

Keywords

Chemical Biology
Epigenetics
Mode of Action
Transcriptional Regulation
Chemical Screening for Drug Discovery

Selected Publications

1. Hoshikawa, Y., Shirota, N., Tsugawa, H., Kimura, S., Matsuyama, A., Yashiroda, Y., Kakeya, H., Arita, M., Iizumi, R., Yoshida, M., Nishimura, S.:
"Formation of giant ER sheets by pentadecanoic acid causes lipotoxicity in fission yeast."
Proc. Natl. Acad. Sci U. S. A. 122(22):e2422126122 (2025)
2. Schneider-Poetsch, T., Dang, Y., Iwasaki, W., Arata, M., Shichino, Y., Al Mourabit, A., Moriou, C., Romo, D., Liu, J.O., Ito, T., Iwasaki, S., Yoshida, M.:
"Girolline is a sequence context-selective modulator of eIF5A activity."
Nat. Commun. 16(1):223 (2025)
3. 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)
4. Takase, S., Hiroyama, T., Shirai, F., Maemoto, Y., Nakata, A., Arata, M., 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., Kawada, M., Hayashi, Y., Harada, H., Yamaguchi, T., Shinkai, Y., Nakamura, Y., Yoshida, M., Ito, A.:
"A specific G9a inhibitor unveils BGLT3 lncRNA as a universal mediator of chemically induced fetal globin gene expression."
Nat. Commun. 14, 23 (2023)
5. Sasaki, K., Suzuki, M., Sonoda, T., Schneider-Poetsch, T., Ito, A., Takagi, M., Fujishiro, S., Sohtome, Y., Dodo, K., Umehara, T., Aburatani, H., Shin-ya, K., Nakao, Y., Sodeoka, M., Yoshida, M.:
"Visualization of the dynamic interaction between nucleosomal histone H3K9 tri-methylation and HP1α chromodomain in living cells."
Cell Chem. Biol. 29(7), 1153-1161.e5. (2022)
6. Chhipi-Shrestha, J.K., Schneider-Poetsch, T., Suzuki, T., Mito, M., Khan, K., Dohmae, N., Iwasaki, S., Yoshida, M.:
"Splicing modulators elicit global translational repression by condensate-prone proteins translated from introns."
Cell Chem. Biol. 29(2), 259-275 (2022)
7. Yoshimoto, R., Chhipi-Shrestha, J.K., Schneider-Poetsch, T., Furuno, M., Burroughs, A.M., Noma, S., Suzuki, H., Hayashizaki, Y., Mayeda, A., Nakagawa, S., Kaida, D., Iwasaki, S., Yoshida, M.:
"Spliceostatin A interaction with SF3B1 limits U1 snRNP availability and causes premature cleavage and polyadenylation."
Cell Chem. Biol. 28(9), 1356-1365.e4. (2021)
8. Kobayashi, H., Hatakeyama, H., Nishimura, H., Yokota, M., Suzuki, S., Tomabechi, Y., Shirouzu, M., Osada, H., Mimaki, M., Goto, Y., Yoshida, M.:
"Chemical reversal of abnormalities in cells carrying mitochondrial DNA mutations."
Nat. Chem. Biol. 17(3), 335-343 (2021)
9. Schneider-Poetsch, T., Yoshida, M.:
"Along the central dogma-controlling gene expression with small molecules."
Annu. Rev. Biochem. 87, 391-420 (2018)
10. Piotrowski, J.S., Li, S.C., Deshpande, R., Simpkins, S.W., Nelson, J., Yashiroda, Y., Barber, J.M., Safizadeh, H., Wilson, E., Okada, H., Gebre, A.A., Kubo, K., Torres, N., Leblanc, M.B., Andrusiak, K., Okamoto, R., Yoshimura, M., van Leeuwen, J., Shirahige, K., Baryshnikova, A., Brown, G., Saito, T., Costanzo, M., Andrews, B., Ohya, Y., Osada, H., Yoshida, M., Myers, C.L., Boone, C.:
"Functional annotation of chemical libraries across diverse biological processes."
Nat. Chem. Biol. 13(9), 982-993 (2017)