山下 泰信 Yasunobu Yamashita

経歴

大阪大学 産業科学研究所 助教
博士(薬学)

2012  慶應義塾大学 薬学部 薬科学科 学士 (薬科学)
2014  慶應義塾大学大学院 薬学研究科 修士 (薬科学)
2017  慶應義塾大学大学院 薬学研究科 博士 (薬科学)
現在に至る

受賞等

2015年 日本薬学会 第 135 年会優秀発表賞
2018年 アレキサンダー・フォン・フンボルト財団 ポストドクトラルフェロー
2022年 有機合成化学協会 味の素研究企画賞

研究歴

2015.04-2017.03  日本学術振興会特別研究員(DC2)
2017.04-2017.07  次世代天然物化学技術研究組合
2017.08-2018.03  ドイツ・Bielefeld大学特別研究員(ONE FLOW PROJECT)
2018.03-2019.12  ドイツ・Bielefeld大学特別研究員 (フンボルト財団)
2020.01-                  大阪大学産業科学研究所助教
2022.04 –                 理化学研究所客員研究員 

所属学会

日本薬学会
日本化学会
有機合成化学協会
日本物理学会
CBI学会

  1. Epigenetic Inhibitors as Alzheimer’s Disease Therapeutic Agents
    Yasunobu Yamashita, Yukihiro Itoh, Yuri Takada, Takayoshi Suzuki.
    Chem. Pharm. Bull. 2024, 72, 630-637.
  2. Identification of Proteolysis Targeting Chimeras (PROTACs) for Lysine Demethylase 5 and their Neurite Outgrowth-Promoting Activity
    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. 
    Chem. Pharm. Bull202472, 638-647.
  3. Identification of a novel histone H2A mono-ubiquitination-inhibiting cell-active small molecule
    Siyao Ni, Yuri Takada, Takaaki Ando, Shengwang Yu, Yasunobu Yamashita, Yukari Takahashi, Miho Sawada, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki
    Bioorg. Med. ChemLett. 2024, 105, 129749.
  4. Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells
    Yosuke Ota, Yukihiro Itoh, Yuri Takada, Yasunobu Yamashita, Chenliang Hu, Mano Horinaka, Yoshihiro Sowa, Mitsuharu Masuda, Toshiyuki Sakai, Takayoshi Suzuki. 
    Bioorg. Med. Chem2024, 100, 1117632.
  5. Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity
    Mitsuhiro Terao, Yasunobu Yamashita, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki
    Bioorg. Med. Chem. 2024, 98, 117579.
  6. A Structure-Activity Relationship Study of SNAIL1 Peptides as Inhibitors of Lysine-Specific Demethylase 1
    Yuri Takada, Kyohei Adachi, Yuka Fujinaga, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki
    Chem. Pharm. Bull202472, 155-160.
  7. Identification of a Histone Deacetylase 8 Inhibitor through Drug Screenings Based on Machine Learning
    Atika Nurani, Yasunobu Yamashita, Yuuki Taki, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki
    Chem. Pharm. Bull202472, 173-178.
  8. Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation
    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.
    J. Med. Chem. 2023, 66, 15171-15188.
  9. Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates
    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.
    ACS Med. Chem. Lett202213, 1568–1573.
  10. Medicinal Chemistry Research on Targeting Epigenetic Complexes
    Yuri Takada, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki 
    J.
     Synth. Org. Chem. Jpn. 202280, 664-675.
  11. Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC)
    Jiranan Chotitumnavee, Yasunobu Yamashita, Yukari Takahashi, Yuri Takada, Tetsuya Iida, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki
    Chem. Commun. 202258, 4635-4638. 
  12. Identification of novel histone deacetylase 6-selective inhibitors bearing 3,3,3-trifluorolactic amide (TFLAM) motif as a zinc binding group
    Takashi Kurohara, Keita Tanaka, Daisuke Takahashi, Satoshi Ueda, Yasunobu Yamashita, Yuri Takada, Hirokazu Takeshima, Shengwang Yu, Yukihiro Itoh, Koji Hase, Takayoshi Suzuki 
    ChemBioChem 202122, 3158-3163.
  13. Identification of Potent and Selective Inhibitors of Fat Mass Obesity Associated Protein Using a Fragment-Merging Approach
    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, and Takayoshi Suzuki
    J. Med. Chem202164, 15810–15824.
  14. Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5C Degraders
    Tetsuya Iida, Yukihiro Itoh, Yukari Takahashi, Yasunobu Yamashita, Takashi Kurohara, Yuka Miyake, Makoto Oba, Takayoshi Suzuki.
    ChemMedChem 202116, 1609-1618.
  15. Learning about enzyme stability against organic co-solvents from structural insight by ion mobility mass spectrometry
    Jens Sproß, Yasunobu Yamashita, Harald Gröger
    ChemBioChem 202021, 1968-1971.
  16. Metalloprotein-catalyzed click reaction for In situ generation of a potent inhibitor
    Yuka Miyake, Yukihiro Itoh, Yoshinori Suzuma, Hidehiko Kodama, Takashi Kurohara, Yasunobu Yamashita, Remy Narozny, Yutaro Hanatani, Shusaku Uchida, Takayoshi Suzuki
    ACS Catal. 202010, 5383-5392.
  17. Chemical modification-mediated optimization of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity
    Yasunobu Yamashita, Ken-Ichiro Tanaka, Naoki Yamakawa, Teita Asano, Yuki Kanda, Ayaka Takafuji, Masahiro Kawahara, Mitsuko Takenaga, Yoshifumi Fukunishi, Tohru Mizushima
    Bioorg. Med. Chem. 201927, 3339-3346.
  18. An asymmetric organocatalytic aldol reaction of a hydrophobic aldehyde in aqueous medium running in flow mode
    Lukas Schober, Shahilan Ratnam, Yasunobu Yamashita, Niklas Adebar, Matthias Pieper, Albrecht Berkessel, Volker Hessel, Harald Gröger
    Synthesis 201951, 1178-1184.
  19. Identification of mepenzolate derivatives with long-acting bronchodilatory activity
    Ken-Ichiro Tanaka, Naoki Yamakawa Yasunobu Yamashita, Teita Asano, Yuki Kanda, Ayaka Takafuji, Masahiro Kawahara, Mitsuko Takenaga, Yoshifumi Fukunishi, Tohru Mizushima
    Frontiers in Pharmacology 20189, 344.
  20. Prediction of protein-compound binding energies from known activity data: docking-score-based method and its applications
    Yoshifumi Fukunishi, Yasunobu Yamashita, Tadaaki Mashimo, Haruki Nakamura
    Mol. Inf. 201837, 1700120.
  21. Short-step syntheses of naturally occurring polyoxygenated aromatics based on site-selective transformation
    Yasunobu Yamashita, Alan Biard, Kengo Hanaya, Mitsuru Shoji, Takeshi Sugai
    Biosci. Biotechnol. Biochem201781, 1279-1284.
  22. Preparation of (R)-3-hydroxy-N-methylpiperidine, a synthetic key intermediate of (R)-mepenzolate, based on the lipase-catalyzed resolution of the racemic form
    Yasunobu Yamashita, Kengo Hanaya, Mitsuru Shoji, Takeshi Sugai
    Heterocycles 201795, 370-379.
  23. Simple synthesis of sakuranetin and selinone via common intermediate, utilizing complementary regioselectivity in the deacetylation of naringenin triacetate
    Yasunobu Yamashita, Kengo Hanaya, Mitsuru Shoji, Takeshi Sugai
    Chem. Pharm. Bull. 201664, 961-965.
  24. Ex situ enantioconvergent approaches for effective use of undesired isomers: stereochemical convergence of substrates with multiple chiral centers and recycling of decarboxylated byproduct
    Yasunobu Yamashita, Tohru Kurihara, Takanobu Horiguchi, Atsushi Miki, Mitsuru Shoji, Takeshi Sugai, Kengo Hanaya
    Synthesis 2016, 48, 2191-2200.
  25. Recent advances for synthesis of scyphostatin and utilization of oxabicyclo[2.2.1]heptane toward ethyl shikimate
    Kazuaki Kuwata, Yasunobu Yamashita, Kengo Hanaya, Takeshi Sugai, Tohru Mizushima, Mitsuru Shoji
    Studies in Natural Products Chemistry 201647, 387.
  26. Superiority of pulmonary administration of mepenzolate bromide over other routes as treatment for chronic obstructive pulmonary disease
    Ken-Ichiro Tanaka, Shota Kurotsu, Teita Asano, Naoki Yamakawa, Daisuke Kobayashi, Yasunobu Yamashita, Hiroshi Yamazaki, Tomoaki Ishihara, Hiroshi Watanabe, Toru Maruyama, Hidekazu Suzuki, Tohru Mizushima
    Scientific Report 20144, 1.
  27. Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activity
    Yasunobu Yamashita, Ken-Ichiro Tanaka, Teita Asano, Naoki Yamakawa, Daisuke Kobayashi, Tomoaki Ishihara, Kengo Hanaya, Mitsuru Shoji, Takeshi Sugai, Mitsuhito Wada, Tadaaki Mashimo, Yoshifumi Fukunishi, Tohru Mizushima
    Bioorg. Med. Chem. 201422, 3488-3497.
  28. Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity
    Naoki Yamakawa, Koichiro Suzuki, Yasunobu Yamashita, Takashi Katsu, Kengo Hanaya, Mitsuru Shoji, Takeshi Sugai, Tohru Mizushima
    Bioorg. Med. Chem. 201422, 2529.
  29. Mepenzolate bromide displays beneficial effects in a mouse model of chronic obstructive pulmonary disease
    Ken-Ichiro Tanaka, Tomoaki Ishihara, Toshifumi Sugizaki, Daisuke Kobayashi, Yasunobu Yamashita, Kayoko Tahara, Naoki Yamakawa, Kumiko Iijima, Kaoru Mogushi, Hiroshi Tanaka, Keizo Sato, Hidekazu Suzuki, Tohru Mizushima
    Nat. Commun. 20134, 2686.
  30. Prostaglandin E1-encapsulated nanoparticles improve walking activity in an experimental rat model of intermittent claudication
    Tomoaki Ishihara, Yasunobu Yamashita, Naoko Takasaki, Shuhei Yamamoto, Erika Hayashi, Kayoko Tahara, Mitsuko Takenaga, Naoki Yamakawa, Tsutomu Ishihara, Tadashi Kasahara, Tohru Mizushima
    J. Pharm. Pharmacol. 2013, 65, 1187.
  31. Chemo-enzymatic enantioconvergent approach toward ethyl shikimate from ethyl 5-hydroxy-3,4-isopropylidenedioxycyclohex-1-enecarboxylate
    Yasunobu Yamashita, Kengo Hanaya, Takeshi Sugai, Tohru Mizushima, Mitsuru Shoji
    Tetrahedron 201369, 6527-6532.