Research Summary

Selected Publications

• 1. Niwa, H., Watanabe, C., Sato, S., Harada, T., Watanabe, H., Tabusa, R., Fukasawa, S., Shiobara, A., Hashimoto, T., Ohno, O., Nakamura, K., Tsuganezawa, K., Tanaka, A., Shirouzu, M., Honma, T., Matsuno, K. and Umehara, T.:
  "Structure-activity relationship and in silico evaluation of cis- and trans-PCPA-derived inhibitors of LSD1 and LSD2"
  ACS Med. Chem. Lett. 13 1485-1492. 2022.
• 2. Kikuchi, M., Morita, S., Goto, M., Wakamori, M., Katsura, K., Hanada, K., Shirouzu, M. and Umehara, T.:
  "Elucidation of binding preferences of YEATS domains to site-specific acetylated nucleosome core particles"
  J. Biol. Chem. 298 102164. 2022.
• 3. 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. and Yoshida, M.:
  "Visualization of the dynamic interaction between nucleosomal histone H3K9 tri-methylation and HP1α chromodomain in living cells"
  Cell Chem. Biol. 29 1153-1161. 2022.
• 4. 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. and Umehara, T.:
  "Design and synthesis of tranylcypromine-derived LSD1 inhibitors with improved hERG and microsomal stability profiles"
  ACS Med. Chem. Lett. 13 848-854. 2022.
• 5. Kitagawa, H., Kikuchi, M., Sato, S., Watanabe, H., Umezawa, N., Kato, M., Hisamatsu, Y., Umehara, T. and Higuchi, T.:
  "Structure-based identification of potent lysine-specific demethylase 1 inhibitor peptides and temporary cyclization to enhance proteolytic stability and cell growth-inhibitory activity"
  J. Med. Chem. 64 3707-3719. 2021.
• 6. Wakamori, M., Okabe, K., Ura, K., Funatsu, T., Takinoue, M. and Umehara, T.:
  "Quantification of the effect of site-specific histone acetylation on chromatin transcription rate"
  Nucleic Acids Res. 48 12648-12659. 2020.
• 7. Wu, H.D., Kikuchi, M., Dagliyan, O., Aragaki, A.K., Nakamura, H., Dokholyan, N.V., Umehara, T. and Inoue, T.:
  "Rational design and implementation of a chemically inducible hetero-trimerization system"
  Nature Methods. 17 928-936. 2020.
• 8. Furukawa, A., Wakamori, M., Arimura, Y., Ohtomo, H., Tsunaka, Y., Kurumizaka, H., Umehara, T. and Nishimura, Y.:
  "Acetylated histone H4 tail enhances histone H3 tail acetylation by altering their mutual dynamics in the nucleosome"
  Proc. Natl. Acad. Sci. USA. 117 19661-19663. 2020.
• 9. Saito, S., Kikuchi, J., Koyama, D., Sato, S., Koyama, H., Osada, N., Kuroda, Y., Akahane, K., Inukai, T., Umehara, T. and Furukawa, Y.:
  "Eradication of central nervous system leukemia of T-cell origin with a brain-permeable LSD1 inhibitor"
  Clin. Cancer Res. 25 1601-1611. 2019.
• 10. Handoko, L., Kaczkowski, B., Hon, C.C., Lizio, M., Wakamori, M., Matsuda, T., Ito, T., Jeyamohan, P., Sato, Y., Sakamoto, K., Yokoyama, S., Kimura, H., Minoda, A. and Umehara, T.:
  "JQ1 affects BRD2-dependent and independent transcription regulation without disrupting H4-hyperacetylated chromatin states"
  Epigenetics. 13 410-431. 2018.

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