Name

Kazuma Amaike

Mail Address

kazuma.amaike[a]riken.jp

Research Interest

Chemical biology

Education and Experience

2007.4~2011.3　　　B.S. in Chemistry, Nagoya University, Japan (Advisor: Prof. Kenichiro Itami)
2011.4~2013.3　　　M.S. Graduate Student in Chemistry, Nagoya University, Japan (Advisor: Prof. Kenichiro Itami)
2013.4~2016.3　　　Ph.D. Graduate Student in Chemistry, Nagoya University, Japan (Advisor: Prof. Kenichiro Itami)
2013.4~2016.4　　　JSPS Research Fellowship for Young Scientists (DC1)
2013.6~2013.8　　　Exchange Student, Massachusetts Institute of Technology, US (Prof. Mohammad Movassaghi)
2016.4~2019.6　　　Postdoctoral researcher, Kyoto University (Prof. Itaru Hamachi)
2017.4~2019.6　　　JSPS Research Fellowship for Young Scientists (SPD)
2019.7~2021.3　　　Designated Assistant Professor, Nagoya University (Prof. Kenichiro Itami)
2021.4~2024.7　　　Assistant Professor, Nagoya University (Prof. Kenichiro Itami)
2023.4~2024.7        Young Researcher Unit (Project leader)
2024.8~present    　Research Scientist, Molecule Creation Laboratory, Cluster for Pioneering Research, RIKEN（Chief Scientist: Dr. Kenichiro Itami）
(2025.4~ Pioneering Research Institute, RIKEN)
2025.4~present　    Research Scientist, Expanded Chemical Space Research Team, Center for Sustainable Resource Science, RIKEN （Team Director: Dr. Kenichiro Itami)

Publications
【Paper】
(23) Functionalization and solubilization of polycyclic aromatic compounds by sulfoniumization
Johannes E. Erchinger, Tsubasa Okumura, Kanami Nakata, Daisuke Shimizu, Constanstin G. Daniliuc, Kazuma Amaike*, Frank Glorius, Kenichiro Itami*, Hideto Ito*
Chem. Sci., 2025, Advance Article. DOI: 10.1039/D5SC01415H

(22) De novo generation of dual-target compounds using artificial intelligence
Kasumi Yasuda, Francois Berenger, Kazuma Amaike, Ayaka Ueda, Tomoya Nakagomi, Genki Hamasaki, Chen Li, Noriko Yuyama Otani, Kazuma Kaitoh, Koji Tsuda, Kenichiro Itami, Yoshihiro Yamanishi*
iScience, 2025, 28, 111526. DOI: 10.1016/j.isci.2024.111526

(21) Water-Soluble Aromatic Nanobelt with Unique Cellular Internalization
Konstantin Günther, Hideya Kono, Hiroki Shudo, Daisuke Shimizu, Reika Isoda, Masayoshi Nakamura, Akiko Yagi*, Kazuma Amaike*, Kenichiro Itami*
Angew. Chem., Int. Ed., 2025, 64, e202414645. DOI: 10.1002/anie.202414645

(20) C–H Amination of Unactivated Arenes and Heteroarenes Through a Dearomative (3+2) Cycloaddition
Sajan Pradhan, Fahimeh Mohammadi, Rikuo Tanase, Kazuma Amaike, Kenichiro Itami*, Jean Bouffard*
ChemRxiv, 2024, DOI: 10.26434/chemrxiv-2024-mj889-v2

(19) In-insect synthesis of oxygen-doped molecular nanocarbons
Atsushi Usami*, Hideya Kono, Vic Austen, Quan Manh Phung, Hiroki Shudo, Tomoki Kato, Hayato Yamada, Akiko Yagi, Kazuma Amaike, Kazuhiro Fujimoto*, Takeshi Yanai*, Kenichiro Itami*
ChemRxiv, 2024, DOI: 10.26434/chemrxiv-2024-1zd0b

(18) Nickel/Photoredox-Catalyzed Decarboxylative Coupling of Aryl Bromides with N-Protected Glycine as an Aminomethyl Source
Jaehyun Jung, Takumi Kinoshita, Yuta Makihara, Yota Sakakibara, Kazuma Amaike, Kei Murakami, Kenichiro Itami
Synlett, 2024, 35, 337–341. DOI: 10.1055/s-0041-1738444

(17) Development of a novel PET ligand, [¹¹C]GO289 targeting CK2 expressed in the brain
Aya Ogata, Takashi Yamada, Saori Hattori, Hiroshi Ikenuma, Junichiro Abe, Mari Tada, Masanori Ichise, Masaaki Suzuki, Kengo Ito, Takashi Kato, Kazuma Amaike, Tsuyoshi Hirota, Akiyoshi Kakita, Kenichiro Itami, Yasuyuki Kimura
Bioorg. Med. Chem. Lett. 2023, 90, 129327. DOI: 10.1016/j.bmcl.2023.129327

(16) C-H arylation enables synthesis of imidazole-4-carboxamide (ICA) based fairy chemicals with plant growth promoting activity
Ayaka Ueda, Kazuma Amaike,* Yoko Shirotani, Robin Warstat, Hideto Ito, Jae-Hoon Choi, Hirokazu Kawagishi,* Kenichiro Itami*
Can. J. Chem. 2023, 101, 449–452. DOI:10.1139/cjc-2022-0256

(15) Discovery of 2,6-Dihalopurines as Stomata Opening Inhibitors: Implication of an LRX-mediated H⁺-ATPase Phosphorylation Pathway
Ayaka Ueda, Yusuke Aihara, Shinya Sato, Keiko Kano, Emi Mishiro-Sato, Hiroyuki Kitano, Ayato Sato, Kazuhiro J. Fujimoto,* Takeshi Yanai, Kazuma Amaike,* Toshinori Kinoshita,* Kenichiro Itami*
ACS Chemical Biology, 2023, 18, 347–355.DOI:10.1021/acschembio.2c00771; ChemRxiv, 2022, DOI: 10.26434/chemrxiv-2022-6s89g

(14) Synthesis, properties, and material hybridization of bare aromatic polymers enabled by dendrimer support
Shusei Fujiki, Kazuma Amaike, Akiko Yagi, Kenichiro Itami
Nature Communications 2022, 13, 5358. DOI: 10.1038/s41467-022-33100-7

(13) Revisiting PFA-mediated tissue fixation chemistry: FixEL enables trapping of small molecules in the brain to visualize their distribution dynamics
Hiroshi Nonaka, Takeharu Mino, Seiji Sakamoto, Jae Hoon Oh, Yu Watanabe, Mamoru Ishikawa, Akihiro Tsushima, Kazuma Amaike, Shigeki Kiyonaka, Tomonori Tamura, A. Radu Aricescu, Wataru Kakegawa, Eriko Miura, Michisuke Yuzaki, Itaru Hamachi
Chem, 2023, 9, 523–540. DOI: 10.1016/j.chempr.2022.11.005; bioRxiv2021,DOI:10.1101/2021.12.21.473647

(12) Photopharmacological Manipulation of Mammalian CRY1 for Regulation of the Circadian Clock
Dušan Kolarski, Simon Miller, Tsuyoshi Oshima, Yoshiko Nagai, Yugo Aoki, Piermichele Kobauri, Ashutosh Srivastava, Akiko Sugiyama, Kazuma Amaike, Ayato Sato, Florence Tama, Wiktor Szymanski, Ben Feringa, Kenichiro Itami, Tsuyoshi Hirota
J. Am. Chem. Soc. 2021, 143, 4, 2078–2087.　DOI: 10.1021/jacs.0c12280

(11) Effect of nanocarbon molecules on the Arabidopsis thaliana transcriptome
Norihito Nakamichi, Ayato Sato, Yusuke Aihara, Toshinori Kinoshita, Yasutomo Segawa, Kazuma Amaike, Kenichiro Itami
bioRxiv 2020, DOI: 10.1101/2020.05.22.110171

(10) An Isoform-Selective Modulator of Cryptochrome 1 Regulates Circadian Rhythms in Mammals
Simon Miller, Yoshiki Aikawa, Akiko Sugiyama, Yoshiko Nagai, Aya Hara, Tsuyoshi Oshima, Kazuma Amaike, Steve A. Kay, Kenichiro Itami, Tsuyoshi Hirota
Cell Chem. Biol. 2020, 27, 1192–1198.　DOI: 10.1016/j.chembiol.2020.05.008

(9) Construction of a Fluorescent Screening System of Allosteric Modulators for the GABA_A Receptor Using a Turn-On Probe
Seiji Sakamoto, Kei Yamaura, Tomohiro Numata, Fumio Harada, Kazuma Amaike, Ryuji Inoue, Shigeki Kiyonaka, and Itaru Hamachi
ACS Cent. Sci. 2019, 5, 1541–1553.　DOI: 10.1021/acscentsci.9b00539

(8) Affinity-guided oxime chemistry for selective protein acylation in live tissue systems
Tomonori Tamura, Zhining Song, Kazuma Amaike, Shin Lee, Sifei Yin, Shigeki Kiyonaka, and Itaru Hamachi
J. Am. Chem. Soc. 2017, 139, 14181–14191.　DOI: 10.1021/jacs.7b07339

(7) Synthesis of multiply arylated pyridines
Takashi Asako, Wakana Hayashi, Kazuma Amaike, Shin Suzuki, Kenichiro Itami, Kei Muto, and Junichiro Yamaguchi
Tetrahedron 2017, 73, 3669–3676.　DOI: 10.1016/j.tet.2017.03.095

(6) Synthesis of Triarylpyridines in Thiopeptide Antibiotics by Using a C−H Arylation/Ring-Transformation Strategy
Kazuma Amaike, Kenichiro Itami, and Junichiro Yamaguchi
Chem. Eur. J. 2016, 22, 4384–4388.　DOI: 10.1002/chem.201600351

(5) Direct C7 Functionalization of Tryptophan. Synthesis of Methyl (S)-2-((tert-Butoxycarbonyl)amino)-3-(7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indol-3-yl)propanoate
Kazuma Amaike, Richard P. Loach and Mohammad Movassaghi
Org. Synth. 2015, 92, 373–385.　DOI: 10.15227/orgsyn.092.0373

(4) C7-Derivatization of C3-Alkylindoles Including Tryptophans and Tryptamines
Richard P. Loach, Owen S. Fenton, Kazuma Amaike, Dustin S. Siegel, Erhan Ozkal, and Mohammad Movassaghi
J. Org. Chem. 2014, 79, 11254–11263.　DOI: 10.1021/jo502062z
Most Read Articles in November 2014

(3) β-Selective C–H Arylation of Pyrroles Leading to Concise Syntheses of Lamellarins C and I
Kirika Ueda, Kazuma Amaike, Richard M. Maceiczyk, Kenichiro Itami, and Junichiro Yamaguchi
J. Am. Chem. Soc. 2014, 136, 13226–13232.　DOI: 10.1021/ja508449y
Most Read Articles in September 2014

(2) Late-Stage C–H Coupling Enables Rapid Identification of HDAC Inhibitors: Synthesis and Evaluation of NCH-31 Analogues
Hiromi Sekizawa, Kazuma Amaike, Yukihiro Itoh,  Takayoshi Suzuki, Kenichiro Itami, and Junichiro Yamaguchi
ACS. Med. Chem. Lett. 2014, 5, 582–586.　DOI: 10.1021/ml500024s
Most Read Articles in March 2014

(1) Decarbonylative C–H Coupling of Azoles and Aryl Esters: Unprecedented Nickel Catalysis and Application to Synthesis of Muscoride A
Kazuma Amaike, Kei Muto, Junichiro Yamaguchi, Kenichiro Itami
J. Am. Chem. Soc. 2012, 134, 13573–13576.　DOI: 10.1021/ja306062c
Highlighted in Newspapers (Chu-nichi, Asahi, The Chemical Daily, Yahoo!News, Mynavi-News)
Most Read Articles in August 2012

【Review】
(5) メチレン架橋シクロパラフェニレンの化学と展開
八木 亜樹子、河野 英也、天池 一真、伊丹 健一郎
有機合成化学協会誌, Vol. 83 (2025)8, No. 5, 446–454. DOI: 10.5059/yukigoseikyokaishi.83.446

(4) Small Molecules Modulating Mammalian Biological Clocks: Exciting New Opportunities for Synthetic Chemistry
Kazuma Amaike, Tsuyoshi Oshima, Nicola Stephanie Skoulding, Yoshifumi Toyama, Tsuyoshi Hirota, Kenichiro Itami
Chem, 2020, 6, 2186-2198. DOI: 10.1016/j.chempr.2020.08.011

(3) AGOX化学による生体組織の内在タンパク質の触媒的ラベリング
天池一真
生体機能関連化学部会NEWS LETTER, 2018, 33, 1, 7–11.

(2) Recognition-driven chemical labeling of endogenous proteins in multi-molecular crowding live cells
Kazuma Amaike, Tomonori Tamura, Itaru Hamachi
Chem. Commun., 2017, 53, 11972–11983.　DOI: 10.1039/C7CC07177A

(1) ニッケル触媒を用いたヘテロ芳香族化合物の直接的カップリング
山口 潤一郎, 武藤 慶, 天池 一真, 山本 拓矢, 伊丹 健一郎
有機合成化学協会誌, Vol. 71 (2013), No. 6, 576–587.　DOI: 10.5059/yukigoseikyokaishi.71.576

【Book】
(2) Synthesis of Natural Products and Pharmaceuticals via Catalytic C–H Functionalization
Junichiro Yamaguchi, Kazuma Amaike and Kenichiro Itami
Transition Metal-Catalyzed Heterocycle Synthesis via C–H Activation, Wiley-VCH book, 2016, 505–550.

(1)「触媒の設計･反応制御 事例集」
ニッケル触媒を用いた新しいクロスカップリング反応とその応用
伊丹 健一郎, 山口 潤一郎, 天池 一真, 武藤 慶

Research Presentation
(4) Nucleic acid delivery using cationic polycyclic aromatic hydrocarbons (Contributed Oral Presentation)
Kazuma Amaike, Erika Kato, Miu Fukatsu, Dominik Zetschok, Luca Hagemeyer, Atsushi Usami, Hayato Yamada, Kenichiro Itami
IKCOC-15, OP-55, Rihga Royal Hotel KYOTO, JAPAN, 2023.11.23

(3) 分子ナノカーボンを用いたケミカルバイオロジー(Invited lecture)
第448回触媒科学研究所コロキウム、北海道大学、2023.5.9

(2) カチオン性ペリレンを用いた核酸輸送
天池一真、加藤江莉佳 、深津美羽、Dominik Zetschok、宇佐見享嗣、山田 早人、伊丹健一郎
第16回バイオ関連化学シンポジウム、名古屋大学・東山キャンパス、2022.9.10–12

(1) Chemical biology in mammalian, plant and insect (Invited lecture)
ITbM workshop, Nagoya University
2021.4.9（online）

Awards
2014年　第5回大津会議メンバー（会員No.071）
2015年　ITbM/IGER Chemistry Workshop　ポスター賞
2018年　日本化学会第98春季年会優秀講演賞(学術)
2019年　有機合成化学協会　日本触媒 研究企画賞