Works
Osaka University, Sanken
Assistant professor
2012 B.Sc. Faculty of Pharmaceutical Sciences, Keio University,
2014 M.Sc. Graduate School of Pharmaceutical Sciences, Keio University
2017 Ph.D. Graduate School of Pharmaceutical Sciences, Keio University
2015-2017 JSPS Research Fellowship for Young Scientists (DC2)
2017-2019 Post doctoral researcher at Bielefeld University
2020- Assistant professor at Osaka University, Sanken
2022– Guest researcher at RIKEN
Awards
2015 the Best Student Presentation Award at the 135th Annual Meeting of the Pharmaceutical Society of Japan
2018 Humboldt Research Fellowship for postdocs
2022 Ajinomoto Award in Synthetic Organic Chemistry, Japan
所属学会
- Epigenetic Inhibitors as Alzheimer’s Disease Therapeutic Agents
Yasunobu Yamashita, Yukihiro Itoh, Yuri Takada, Takayoshi Suzuki.
Chem. Pharm. Bull. 2024, 72, 630-637. - 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. Bull. 2024, 72, 638-647. - 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. Chem. Lett. 2024, 105, 129749. - 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. Chem. 2024, 100, 1117632. - 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. - 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. Bull. 2024, 72, 155-160. - 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. Bull. 2024, 72, 173-178. - 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. - 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. Lett. 2022, 13, 1568–1573. - Medicinal Chemistry Research on Targeting Epigenetic Complexes
Yuri Takada, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki
J. Synth. Org. Chem. Jpn. 2022, 80, 664-675. - 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. 2022, 58, 4635-4638. - 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 2021, 22, 3158-3163. - 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. Chem. 2021, 64, 15810–15824. - 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 2021, 16, 1609-1618. - Learning about enzyme stability against organic co-solvents from structural insight by ion mobility mass spectrometry
Jens Sproß, Yasunobu Yamashita, Harald Gröger
ChemBioChem 2020, 21, 1968-1971. - 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. 2020, 10, 5383-5392. - 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. 2019, 27, 3339-3346. - 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 2019, 51, 1178-1184. - 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 2018, 9, 344. - 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. 2018, 37, 1700120. - 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. Biochem. 2017, 81, 1279-1284. - 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 2017, 95, 370-379. - 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. 2016, 64, 961-965. - 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. - 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 2016, 47, 387. - 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 2014, 4, 1. - 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. 2014, 22, 3488-3497. - 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. 2014, 22, 2529. - 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. 2013, 4, 2686. - 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. - 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 2013, 69, 6527-6532.