Akari Tokuyama, Yasunobu Yamashita, Ryo Maeda, Toshiki Akiyama, Yuri Takada, Ryunosuke Yoshino, Hiroki Kato, Shengwang Yu, Yukihiro Itoh, Makoto Tachibana, Takayoshi Suzuki. Identification of a novel small-molecule inhibitor of heterochromatin protein 1. Bioorganic & Medicinal Chemistry Letters, 139, 118694, 2026.
Jiranan Chotitumnavee, Peeratchai Seemaung, Rapeewan Settacomkul, Ratchanon Sukprasert, Yukihiro Itoh, Takayoshi Suzuki, Sirada Srihirun, Christopher Power Pornpun Vivithanaporn. Targeted Degradation of Histone Deacetylase 8 Using Proteolysis Targeting Chimeras Technology: A Promising Approach for Glioblastoma Treatment. Drug Design, Development and Therapy, 20, 555228, 2026.
Review
Shengwang Yu, Yukihiro Itoh, Takayoshi Suzuki. From Inhibition to Degradation: Proteolysis-Targeting Chimeras for Epigenetic Enzymes in Modern Drug Discovery. Chemistry Letters, in press.
Yukihiro Itoh, Mirei Hayashi, Yasunobu Yamashita, Yuri Takada, Takayoshi Suzuki. Discovery of HDAC PROTACs via click chemistry-based library screening. The 55th Naito Conference, Sapporo, July 1st, 2026(Short Talk & Poster)
Original
Anirban Mukherjee, Yasunobu Yamashita, Ryo Maeda, Toshiki Akiyama, Katsunori Endo, Yuri Takada, Hiroki Tsumoto, Yukiko Moriyama, Akihiro Ito, Fumiyuki Shirai, Makoto Tachibana, Yukihiro Itoh, Takayoshi Suzuki. A Novel PROTAC G9a/GLP Degrader that Inhibits, Similar to G9a siRNA, the Migration of MCF-7 Breast-Cancer Cells without Affecting Proliferation. Journal of Medicinal Chemistry, 68, 18258–18271, 2025. Journal Cover
Yasunobu Yamashita, Yuuki Taki, Yoshinori Wakabayashi, Junichiro Kanazawa, Paddy RA Melsen, Yuri Takada, Yukihiro Itoh, Masanobu Uchiyama, Takayoshi Suzuki. A Deep-Learning-Aided Drug Screening Based on Visualization of a Hidden Layer as Chemical Space. ACS Medicinal Chemistry Letters, 16, 1299–1304, 2025. Journal Cover
International Conference
Yukihiro Itoh, Identification, Structural Optimization and PROTAC Application of HDAC8 Inhibitors, 15th AFMC INTERNATIONAL MEDICINAL CHEMISTRY SYMPOSIUM (AIMECS 2025) Hangzhou, September 26th, 2025
Yukihiro Itoh Drug discovery research based on strategic chemistry approaches. CSJ Annual Meeting (2025), Asian International Symposium, Sakai, March 27th, 2026.
Original
Tetsuya Iida, Yukihiro Itoh, Yukari Takahashi, Yuka Miyake, Farzad Zamani, Yasunobu Yamashita, Yuri Takada, Toshiki Akiyama, Jun Ibaraki, Kyoka Okuda, Yuto Tokuda, Tomoka Nishimura, Koto Hidaka, Hiiro Mori, Makoto Oba, Takayoshi Suzuki. Identification of proteolysis targeting chimeras (PROTACs) for lysine demethylase 5 and their neurite outgrowth-promoting activity. Chemical & Pharmaceutical Bulletin, 72, 638–647, 2024.
Yosuke Ota, Yukihiro Itoh, Yuri Takada, Yasunobu Yamashita, Chenliang Hu, Mano Horinaka, Yoshihiro Sowa, Mitsuharu Masuda, Toshiyuki Sakai, Takayoshi Suzuki. Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells. Bioorganic & Medicinal Chemistry, 100, 117632, 2024.
Yuri Takada, Kyohei Adachi, Yuka Fujinaga, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki. A Structure-Activity Relationship Study of SNAIL1 Peptides as Inhibitors of Lysine-Specific Demethylase 1. Chemical & Pharmaceutical Bulletin, 72, 155–160, 2024.
Atika Nurani, Yasunobu Yamashita, Yuuki Taki, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki. Identification of a histone deacetylase 8 inhibitor through drug screenings based on machine learning. Chemical & Pharmaceutical Bulletin, 72, 173–178, 2024.
Mitsuhiro Terao, Yasunobu Yamashita, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki. Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity. Bioorganic & Medicinal Chemistry, 98, 117579, 2024.
Yukihiro Itoh Proteolysis targeting chimeras (PROTACs) targeting epigenetic enzymes International Congress on Pure & Applied Chemistry Kota Kinabalu 2022 (ICPAC KK 2022) Online, November 23th, 2022
Original
Muthuraj Prakash, Yukihiro Itoh, Yoshie Fujiwara, Yukari Takahashi, Yuri Takada, Paolo Mellini, Elghareeb E Elboray, Mitsuhiro Terao, Yasunobu Yamashita, Chika Yamamoto, Takao Yamaguchi, Masayuki Kotoku, Yuki Kitao, Ritesh Singh, Rohini Roy, Satoshi Obika, Makoto Oba, Dan Ohtan Wang, Takayoshi Suzuki. Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach. Journal of Medicinal Chemistry, 64, 15810-15824, 2021.
Yusuke Ota, Arisa Nakamura, Elghareeb E. Elboray, Yukihiro Itoh, Takayoshi Suzuki. Design, synthesis, and biological evaluation of a conjugate of 5-fluorouracil and an LSD1 inhibitor. Chemical & Pharmaceutical Bulletin, 66, 192-195, 2019.
Paolo Mellini, Yukihiro Itoh, Hiroki Tsumoto, Ying Li, Miki Suzuki, Natsu ko Tokuda, Taeko Kakizawa, Yuri Miura, Jun Takeuchi, Maija Lahtela-Kakkonene Takayoshi Suzuki. Potent mechanism-based sirtuin-2-selective inhibition by an in situ-generated occupant of the substrate-binding site, “selectivity pocket” and NAD+-binding site. Chemical Science 8, 6400-6408, 2017.
Takayoshi Suzuki, Yosuke Ota, Masaki Ri, Masashige Bando, Aogu Gotoh, Yukihiro Itoh, Hiroki Tsumoto, Prima R. Tatum, Tamio Mizukami, Hidehiko Nakagawa, Shunsuke Iida, Ryuzo Ueda, Katsuhiko Shirahige, Naoki Miyata. Rapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries. Journal of Medicinal Chemistry, 55, 9562-9575, 2012.
Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Keiichiro Okuhira, Mikihiko Naito, Yuichi Hashimoto. Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist. Bioorganic & Medicinal Chemistry Letters, 22, 4453-4457, 2012.
Takayoshi Suzuki, Mohammed Naseer Ahmed Khan, Hideyuki Sawada, Erika Imai, Yukihiro Itoh, Katsura Yamatsuta, Natsuko Tokuda, Jun Takeuchi, Takuya Seko, Hidehiko Nakagawa, and Naoki Miyata. Design, Synthesis, and Biological Activity of a Novel Series of Human Sirtuin 2-selective Inhibitors. Journal of Medicinal Chemistry, 55, 5760-5773, 2012.
Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Shinichi Sato, Mikihiko Naito, Yuichi Hashimoto. Development of target protein-selective degradation inducer for protein knockdown. Bioorganic & Medicinal Chemistry, 19, 3229-3241, 2011.
Keiichiro Okuhira, Nobumichi Ohoka, Kimie Sai, Tomoko Nishimaki-Mogami, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Mikihiko Naito. Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein. FEBS Letters, 585, 1147-1152, 2011.
Original
Shohei Hamada, Takayoshi Suzuki, Koshiki Mino, Koichi Koseki, Felix Oehme, Ingo Flamme, Hiroki Ozasa, Yukihiro Itoh, Daisuke Ogasawara, Haruka Komaarashi, Aiko Kato, Hiroki Tsumoto, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata. Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. Journal of Medicinal Chemistry, 53, 5629-5638, 2010.
Yukihiro Itoh, Minoru Ishikawa, Mikihiko Naito M, Yuichi Hashimoto. Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins. Journal of the American Chemical Society, 132, 5820-5826, 2010.
Original
Shohei Hamada Tae-Dong Kim, Takayoshi Suzuki, Yukihiro Itoh, Hiroki Tsumoto, Hidehiko Nakagawa, Ralf Janknechtb, Naoki Miyata. Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors. Bioorganic & Medicinal Chemistry Letters, 19, 2852-2855, 2009.
Yukihiro Itoh, Takayoshi Suzuki, Akiyasu Kouketsu, Nobuaki Suzuki, Satoko Maeda, Minoru Yoshida, Hidehiko Nakagawa, Naoki Miyata. Design, Synthesis, Structure-Selectivity Relationship, and Effect on Human Cancer Cells of a Novel Series of Histone Deacetylase 6 Inhibitors. Journal of Medicinal Chemistry, 50, 5425-5438, 2007.