Publications

Achievements

Original

  1. Yasunobu Yamashita, Juhyun Yun, Ayumu Asai, Hiroki Kato, Yuuki Taki, Moeha Izuhara, Takuya Yamanaka, Motonori Tsuji, Junya Nakamura, Yuri Takada, Yukihiro Itoh, Yasushi Sakurai, Takayoshi Suzuki. Identification of Non-Hydroxamate Histone Deacetylase 8 Inhibitors using Deep Learning-Based Screening of Two-Dimensional Molecular Images. Bioorganic & Medicinal Chemistry Letters, 131, 130469, 2026.
  2. 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.
  3. 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

  1. Shengwang Yu, Yukihiro Itoh, Takayoshi Suzuki. From Inhibition to Degradation: Proteolysis-Targeting Chimeras for Epigenetic Enzymes in Modern Drug Discovery. Chemistry Letters, in press.
  2. Yukihiro Itoh. Development of Protein and RNA Degraders for Drug Discovery. Yakugaku Zasshi, 146, 617–624, 2026.

International Conference

  1. 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

  1. 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
  2. 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

  1. Yukihiro Itoh, Identification, Structural Optimization and PROTAC Application of HDAC8 Inhibitors, 15th AFMC INTERNATIONAL MEDICINAL CHEMISTRY SYMPOSIUM (AIMECS 2025) Hangzhou, September 26th, 2025
  2. Yukihiro Itoh Drug discovery research based on strategic chemistry approaches. CSJ Annual Meeting (2025), Asian International Symposium, Sakai, March 27th, 2026.

Original

  1. 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.
  2. Siyao Ni, Yuri Takada, Takaaki Ando, Shengwang Yu, Yasunobu Yamashita, Yukari Takahashi, Miho Sawada, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki. Identification of a novel histone H2A mono-ubiquitination-inhibiting cell-active small molecule. Bioorganic & Medicinal Chemistry Letters, 105, 129759, 2024.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. Haiyan Li, Ayako Kawatake-Kuno, Hiromichi Inaba, Yuka Miyake, Yukihiro Itoh, Takatoshi Ueki, Naoya Oishi, Toshiya Murai, Takayoshi Suzuki, Shusaku Uchida. Discrete prefrontal neuronal circuits determine repeated stress-induced behavioral phenotypes in male mice. Neuron, 112, 786–804, 2024.

Review

  1. Yasunobu Yamashita, Yukihiro Itoh, Yuri Takada, Takayoshi Suzuki. Epigenetic Inhibitors as Alzheimer’s Disease Therapeutic Agents. Chemical & Pharmaceutical Bulletin, 72, 630-637, 2024.

Original

  1. Yukihiro Itoh, Peng Zhan, Toshifumi Tojo, Pattaporn Jaikhan, Yosuke Ota, Miki Suzuki, Ying Li, Zi Hui, Yukiko Moriyama, Yuri Takada, Yasunobu Yamashita, Makoto Oba, Shusaku Uchida, Mitsuharu Masuda, Shinji Ito, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki. Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation. Journal of Medicinal Chemistry, 66, 15171-15188, 2023.
    Journal Cover
  2. Hirokazu Mishima, Yukihiro Itoh, Takashi Kurohara, Takayoshi Suzuki, Naoya Asada, Ken-ichi Kusakabe, Yuko Okamoto. Origin of the kinetic HDAC2-selectivity of an HDAC inhibitor. Journal of Computational Chemistry, 44, 1604–1609, 2023.

Original

  1. Yosuke Ota, Yukihiro Itoh, Takashi Kurohara, Ritesh Singh, Elghareeb E Elboray, Chenliang Hu, Farzad Zamani, Anirban Mukherjee, Yuri Takada, Yasunobu Yamashita, Mie Morita, Mano Horinaka, Yoshihiro Sowa, Mitsuharu Masuda, Toshiyuki Sakai, Takayoshi Suzuki. Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. ACS Medicinal Chemistry Letters 13, 1568–1573, 2022.
  2. Wei Zhe, Naomi Hoshina, Yukihiro Itoh, Toshifumi Tojo, Takayoshi Suzuki, Koji Hase, Daisuke Takahashi. A Novel HDAC1-Selective Inhibitor Attenuates Autoimmune Arthritis by Inhibiting Inflammatory Cytokine Production. Biological & Pharmaceutical Bulletin 45, 1364–1372, 2022.
  3. Jiranan Chotitumnavee, Yasunobu Yamashita, Yukari Takahashi, Yuri Takada, Tetsuya Iida, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki. Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC). Chemical Communications, 68, 4635–4638, 2022.

Review

  1. Yuri Takada, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki. Medicinal Chemistry Research on Targeting Epigenetic Complexes. Journal of Synthetic Organic Chemistry Japan, 80, 664–675, 2022.
  2. Yukihiro Itoh, Yuri Takada, Yasunobu Yamashita, Takayoshi Suzuki. Recent progress on small molecules targeting epigenetic complexes. Current Opinion in Chemical Biology, 67, 102130, 2022.

International Conference

  1. 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

  1. 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.
  2. Takashi Kurohara, Keita Tanaka, Daisuke Takahashi, Satoshi Ueda, Yasunobu Yamashita, Yuri Takada, Hirokazu Takeshima, Shengwang Yu, Yukihiro Itoh, Koji Hase, Takayoshi Suzuki. Identification of Novel Histone Deacetylase 6-Selective Inhibitors Bearing 3,3,3-Trifluorolactic Amide (TFLAM) Motif as a Zinc Binding Group. ChemBioChem, 22, 3158–3163, 2021.
    Journal Cover
  3. Tetsuya Iida, Yukihiro Itoh, Yukari Takahashi, Yasunobu Yamashita, Takashi Kurohara, Yuka Miyake, Makoto Oba, Takayoshi Suzuki. Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5C Degraders. ChemMedChem 16, 1609-1618, 2021.
    Journal Cover

Original

  1. Yuka Miyake, Yukihiro Itoh, Yoshinori Suzuma, Hidehiko Kodama, Shusaku Uchida, Takayoshi Suzuki. Metalloprotein-Catalyzed Click Reaction for In Situ Generation of a Potent Inhibitor. ACS Catalysis, 10, 5383–5392, 2020.
  2. Keng Yoon Yeong, Kooi Yeong Khaw, Yukari Takahashi, Yukihiro Itoh, Vikneswaran Murugaiyah, Takayoshi Suzuki. Discovery of gamma-mangostin from Garcinia mangostana as a potent and selective natural SIRT2 inhibitor. Bioorganic Chemistry 94, 103403, 2020.
  3. Shusuke Ogihara, Toru Komatsu, Yukihiro Itoh, Yuka Miyake, Takayoshi Suzuki, Kouichi Yanagi, Yusuke Kimura, Tasuku Ueno, Kenjiro Hanaoka, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Yasuteru Urano. Metabolic-Pathway-Oriented Screening Targeting S-Adenosyl-l-methionine Reveals the Epigenetic Remodeling Activities of Naturally Occurring Catechols. Journal of the American Chemical Society, 142, 21–26, 2020.

Review

  1. Yukihiro Itoh, Takashi Kurohara, Takayoshi Suzuki. N+-C-H…O Hydrogen Bonds in Protein-Ligand Complexes and their Application to Drug Design. Journal of Synthetic Organic Chemistry Japan, 78, 71151-1162, 2020.
  2. Yukihiro Itoh. Drug Discovery Researches on Modulators of Lysine-Modifying Enzymes Based on Strategic Chemistry Approaches. Chemical and Pharmaceutical Bulletin, 68, 34-45, 2020.

Original

  1. Yukihiro Itoh, Yusuke, Nakashima, Shuichiro Tsukamoto, Takashi Kurohara, Miki Suzuk,Yoshitake Sakae, Masayuki Oda, Yuko Okamoto, Takayoshi Suzuki. N+-C-H…O Hydrogen bonds in protein-ligand complexes. Sci. Rep. 9, 767, 2019.  
  2. Paolo Mellini, Yukihiro Itoh, Elghareeb E. Elboray, Hiroki Tsumoto, Ying Li, Miki Suzuki, Yukari Takahashi, Toshifumi Tojo, Takashi Kurohara, Yuka Miyake, Yuri Miura, Yuki Kitao, Masayuki Kotoku, Tetsuya Iida, Takayoshi Suzuki. Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the “Selectivity Pocket”, Substrate-Binding Site, and NAD+-Binding Site. Journal of Medicinal Chemistry, 62, 5844-5862, 2019.
    Journal Cover
  3. Pattaporn Jaikhan, Benjaporn Buranrat, Yukihiro Itoh, Jiranan Chotitumnavee, Takashi Kurohara, Takayoshi Suzuki. Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors. Bioorganic & Medicinal Chemistry Letters, 29, 1173-1176, 2019.
  4. Yuka Miyake, Yukihiro Itoh, Atsushi Hatanaka, Yoshinori Suzuma, Miki Suzuki, Hidehiko Kodama, Yoshinobu Arai, Takayoshi Suzuki. Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy. Bioorganic & Medicinal Chemistry, 27, 1119-1129, 2019.
  5. 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.

Original

  1. Yukihiro Itoh, Miki Suzuki. Design, synthesis, and biological evaluation of novel ubiquitin-activating enzyme inhibitors. Bioorganic & Medicinal Chemistry Letters, 28, 2723-2727, 2018.
  2. Yusuke Ota, Taeko Kakizawa, Yukihiro Itoh, Takayoshi Suzuki. Design, Synthesis, and In Vitro Evaluation of Novel Histone H3 Peptide-Based LSD1 Inactivators Incorporating α,α-Disubstituted Amino Acids with γ-Turn-Inducing Structures. Molecules, 23, 1099, 2018.
  3. Shuichiro Tsukamoto, Yoshitake Sakae, Yukihiro Itoh, Takayoshi Suzuki, Yuko Okamoto. Computational analysis for selectivity of histone deacetylase inhibitor by replica-exchange umbrella sampling molecular dynamics simulations. The Journal of Chemical Physics, 148, 125102, 2018.
  4. Yosuke Ota, Shin Miyamura, Misaho Araki, Yukihiro Itoh, Shusuke Yasuda, Mitsuharu Masuda, Tomoyuki Taniguchi, Yoshihiro Sowa, Toshiyuki Sakai, Kenichiro Itami, Junichiro Yamaguchi, Takayoshi Suzuki. Design, synthesis and evaluation of γ-turn mimetics as LSD1-selective inhibitors. Bioorganic & Medicinal Chemistry, 26, 775-785, 2018.
  5. Taeko Kakizawa, Yusuke Ota, Yukihiro Itoh, Takayoshi Suzuki. Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors. Bioorganic & Medicinal Chemistry Letters, 28, 167-169, 2018.

Review

  1. Yukihiro Itoh. Chemical Protein Degradation Approach and its Application to Epigenetic Targets. The Chemical Record, 2018, 9, 1681-1700.

Original

  1. 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.
  2. Keiichiro Okuhira, Takuji Shoda, Risa Omura, Nobumichi Ohoka, Takayuki Hattori, Norihito Shibata, Yosuke Demizu, Ryo Sugihara, Asato Ichino, Haruka Kawahara, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Masaaki Kurihara, Hiroyuki Saito, Mikihiko Naito. Targeted degradation of proteins localized in subcellular compartments by hybrid small molecules. Molecular pharmacology, 91, 159-166, 2017.

Review

  1. Yukihiro Itoh, Takayoshi Suzuki. “Drug” Discovery with the Help of Organic Chemistry. Yakugaku Zasshi, 137, 283-292, 2017.

Original

  1. Yosuke Ota, Yukihiro Itoh, Asako Kaise, Kiminori Ohta, Yasuyuki Endo, Mitsuharu Masuda, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki. Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen. Angewandte Chemie International Edition, 55, 16115-161118, 2016.
  2. Shin Miyamura, Misaho Araki, Yosuke Ota, Yukihiro Itoh, Shusuke Yasuda, Mitsuharu Masuda, Tomoyuki Taniguchi, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki, Kenichiro Itami, Junichiro Yamaguchi. C-H Activation Enables Rapid Structure-Activity Relationship Study of Arylcylclopropyl Amines for Potent and Selective LSD1 Inhibitors. Organic & Biomolecular Chemistry 14, 8576-8585, 2016.
  3. Yukihiro Itoh, Miki Suzuki, Taiji Matsui, Yusuke Ota, Zi Hui, Kazunori Tsubaki, Takayoshi Suzuki. False HDAC inhibition by aurone compound. Chemical & Pharmaceutical Bulletin, 64, 1124-1128, 2016.
  4. Fumihiro Higuchi, Shusaku Uchida, Hirotaka Yamagata, Naoko Abe-Higuchi, Teruyuki Hobara, Kumiko Hara, Ayumi Kobayashi, Tatsushi Shintaku, Yukihiro Itoh, Takayoshi Suzuki, Yoshifumi Watanabe. Hippocampal microRNA-124 enhances chronic stress resilience in mice. Journal of Neuroscience, 36, 7253-7267, 2016.
  5. Yukihiro Itoh, Keisuke Aihara, Paolo Mellini, Toshifumi Tojo, Yosuke Ota, Hiroki Tsumoto, Viswas Raja Solomon, Peng Zhan, Miki Suzuki, Daisuke Ogasawara, Akira Shigenaga, Tsubasa Inokuma, Hidehiko Nakagawa, Naoki Miyata, Tamio Mizukami, Akira Otaka, and Takayoshi Suzuki. Identification of SNAIL1 Peptide-Based Irreversible Lysine Specific Demethylase 1-Selective Inactivators. Journal of Medicinal Chemistry, 59, 1531-1544, 2016.
  6. Taeko Kakizawa, Tamio Mizukami, Yukihiro Itoh, Makoto Hasegawa, Ryuzo Sasaki, Takayoshi Suzuki. Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide. Bioorganic & Medicinal Chemistry Letters, 25, 1193-1195, 2016.

Review

  1. Yukihiro Itoh, Takayoshi Suzuki. Molecular Technology for Controlling Epigenetics: Regulation of Histone Acetylation and Methylation by Small Molecules. Journal of Synthetic Organic Chemistry, Japan. 74, 441-452, 2016.

Original

  1. Yukihiro Itoh, Hideyuki Sawada, Miki Suzuki, Toshifumi Tojo, Ryuzo Sasaki, Makoto Hasegawa, Tamio Mizukami, Takayoshi Suzuki. Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells. ACS Medicinal Chemistry Letters, 6, 665-670, 2015.
  2. Taeko Kakizawa, Yusuke Ota, Yukihiro Itoh, Hiroki Tsumoto, Takayoshi Suzuki. Histone H3 peptide based LSD1-selective inhibitors. Bioorganic & Medicinal Chemistry Letters, 25, 1925-1928, 2015.
  3. Mohammed Naseer Ahmed Khan, Hiroki Tsumoto, Yukihiro Itoh, Yosuke Ota, Miki Suzuki, Daisuke Ogasawara, Hidehiko Nakagawa, Tamio Mizukami, Naoki Miyata, Takayoshi Suzuki. Design, synthesis, and biological activity of N-alkylated analogue of NCL1, a selective inhibitor of lysine-specific demethylase 1. MedChemComm, 6, 407-412, 2015.

Review

  1. Peng Zhan, Yukihiro Itoh, Takayoshi Suzuki, Xinyong Liu. Strategies for the Discovery of Target-specific or Isoform-selective Modulators. Journal of Medicinal Chemistry, 58, 7611-7633, 2015.

Original

  1. Hiromi Sekizawa, Kazuma Amaike, Yukihiro Itoh, Takayoshi Suzuki, Kenichiro Itami, Junichiro Yamaguchi. Late-Stage C-H Coupling Enables Rapid Identification of HDAC Inhibitors: Synthesis and Evaluation of NCH-31 Analogues. ACS Medicinal Chemistry Letters, 5, 582-586, 2014.
  2. Prima R. Tatum, Hideyuki Sawada, Yosuke Ota, Yukihiro Itoh, Peng Zhan, Naoya Ieda, Hidehiko Nakagawa, Naoki Miyata, Takayoshi Suzuki. Identification of novel SIRT2-selective inhibitors using a click chemistry approach. Bioorganic & Medicinal Chemistry Letters, 24, 1871-1874, 2014.
  3. Takayoshi Suzuki, Nobusuke Muto, Masashige Bando, Yukihiro Itoh, Ayako Masaki, Masaki Ri, Yosuke Ota, Hidehiko Nakagawa, Shinsuke Iida, Katsuhiko Shirahige, Naoki Miyata. Design, synthesis, and biological activity of NCC149 derivatives as histone deacetylase 8-selective inhibitors. ChemMedChem, 9, 657-664, 2014.
  4. Yukihiro Itoh, Daisuke Ogasawara, Yosuke Ota, Tamio Mizukami, Takayoshi Suzuki. Synthesis, LSD1 Inhibitory Activity, and LSD1 Binding Model of Optically Pure Lysine-PCPA Conjugates. Computational and Structural Biotechnology Journal, 9, e201402002, 2014.

Review

  1. Peng Zhan, Yu’ning Song, Yukihiro Itoh, Takayoshi Suzuki, Xinyong Liu. Recent Advances in the Structure-based Rational Design of TNKSIs. Molecular Biosystems, 10, 2783-2799, 2014.
  2. Yukihiro Itoh, Naoki Miyata, Takayoshi Suzuki. Target-guided Synthesis: Medicinal Chemistry Strategy to Allow Target Enzymes Themselves to Synthesize their Own Inhibitors. Journal of Synthetic Organic Chemistry Japan, 72, 702-716, 2014.

Original

  1. Takayoshi Suzuki, Hiroki Ozasa, Yukihiro Itoh, Peng Zhan, Hideyuki Sawada, Koshiki Mino, Louise Walport, Rei Ohkubo, Akane Kawamura, Masato Yonezawa, Yuichi Tsukada, Anthony Tumber, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Christopher J. Schofield, Naoki Miyata. Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity. Journal of Medicinal Chemistry, 56, 7222-7231, 2013.
  2. Yuji Matsuya, Yuta Kobayashia, Sayumi Uchida, Yukihiro Itoh, Hideyuki Sawada, Takayoshi Suzuki, Naoki Miyata, Kenji Sugimoto, Naoki Toyooka. Search for a Novel SIRT1 Activator: Structural Modification of SRT1720 and Biological Evaluation. Bioorganic & Medicinal Chemistry Letters, 23, 4907-4910, 2013.
  3. Daisuke Ogasawara, Yukihiro Itoh, Hiroki Tsumoto, Taeko Kakizawa, Koshiki Mino, Kiyoshi Fukuhara, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata, Takayoshi Suzuki. Lysine-Specific Demethylase 1-Selective Inactivators Based on Protein-Targeted Drug Delivery Mechanism. Angewandte Chemie International Edition, 52, 8620-8624, 2013.
  4. Takayoshi Suzuki, Yuki Kasuya, Yukihiro Itoh, Yosuke Ota, Peng Zhan, Kaori Asamitsu, Hidehiko Nakagawa, Takashi Okamoto, Naoki Miyata. Identification of Highly Selective and Potent Histone Deacetylase 3 Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly, PLoS ONE, 8, e68669, 2013.

Review

  1. Yukihiro Itoh, Takayoshi Suzuki, Naoki Miyata. Small-molecular modulators of cancer-related epigenetic mechanisms. Molecular BioSystems, 9, 873-896, 2013.

Original

  1. 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.
  2. 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.
  3. 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.

Original

  1. Yukihiro Itoh, Risa Kitaguchi, Minoru Ishikawa, Mikihiko Naito, Yuichi Hashimoto. Design, Synthesis and Biological Evaluation of Nuclear Receptor-degradation Inducers. Bioorganic & Medicinal Chemistry, 19, 6768-6778, 2011.
  2. 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.
  3. 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

  1. 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.
  2. 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

  1. 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.

Original

  1. Takayoshi Suzuki, Sou-ichi Igari, Akira Hirasawa, Mie Hata, Masaji Ishiguro, Hiroki Fujieda, Yukihiro Itoh, Tatsuya Hirano, Hidehiko Nakagawa, Michitaka Ogura, Makoto Makishima, Gozoh Tsujimoto, Naoki Miyata. Identification of GPR120-selective agonists derived from PPARg agonists. Journal of Medicinal Chemistry, 51, 7640-7644, 2008.

Review

  1. Yukihiro Itoh, Takayoshi Suzuki, Naoki Miyata. Isoform Selective Histone Deacetylase Inhibitors. Current Pharmaceutical Design, 14, 529-544, 2008.

Original

  1. 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.
  2. Takayoshi Suzuki, Shinya Hisakawa, Yukihiro Itoh, Nobuaki Suzuki, Katsumasa Takahashi, Masatoshi Kawahata, Kentaro Yamaguchi, Hidehiko Nakagawa, Naoki Miyata. Design, synthesis and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors. Bioorganic & Medicinal Chemistry Letters, 17, 4208-4212, 2007.
  3. Takayoshi Suzuki, Shinya Hisakawa, Yukihiro Itoh, Sakiko Maruyama, Mineko Kurotaki, Hidehiko Nakagawa, Naoki Miyata. Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor. Bioorganic & Medicinal Chemistry Letters, 17, 1558-1561, 2007.

Original

  1. Takayoshi Suzuki, Akiyasu Kouketsu, Yukihiro Itoh, Shinya Hisakawa, Satoko Maeda, Minoru Yoshida, Hidehiko Nakagawa, Naoki Miyata. Highly Potent and Selective Histone Deacetylase 6 Inhibitors Designed Based on a Small-Molecular Substrate. Journal of Medicinal Chemistry, 49, 4809-4812, 2006.

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