2023
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Expert Opinion On Therapeutic Patents
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CDC7 kinase inhibitors: a survey of recent patent literature (2017-2022)
- Takayuki Irie, Masaaki Sawa
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Annual Meeting of the Japanese Cancer Association
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A novel ALK5 inhibitor, AL2 shows anti-tumor activity by modulating cancer immunity
- Masaaki Sawa, Mai Arai, Mitsuharu Hanada, Hideki Moriyama, Hiroshi Ohmoto, Kazuhito Naka
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Bioorganic & Medicinal Chemistry Letters
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Low entropic cost of binding confers high selectivity on an allosteric ERK2 inhibitor
- H. Sugiyama, M. Yoshida, H. Nagao, M. Sawa, T. Kinoshita
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Arteriosclerosis, Thrombosis, and Vascular Biology
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BCL6B (B-Cell CLL/Lymphoma 6 Member B Protein) Contributes to Ocular Vascular Diseases via Notch Signal Silencing
- M. Tanaka, S. Nakamura, T. Sakaue, T. Yamamoto, M. Maekawa , A. Nishinaka, H. Yasuda, K. Yunoki, Y. Sato, M. Sawa, K. Yoshino, M. Shimazawa, M. Hatano, T. Tokuhisa, S. Higashiyama, H. Hara
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AACR Annual Meeting 2023
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Discovery of a novel activin receptor-like kinases (ALKs) inhibitor targeting TGF-β signaling pathways
- M. Arai, M. Hanada, H. Moriyama, H. Ohmoto, K. Naka, M. Sawa
2022
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Biochemical and Biophysical Research Communications
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Bivalent binding mode of an amino-pyrazole inhibitor indicates the potentials for CK2α1-selective inhibitors
- A. Ikeda, M. Tsuyuguchi, D. Kitagawa, M. Sawa, S. Nakamura, I. Nakanishi, T. Kinoshita
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AACR Annual Meeting 2022
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Safety, pharmacokinetics, and pharmacodynamics of AS-1763, a highly selective, orally bioavailable, non-covalent BTK inhibitor, in healthy volunteers
- A. Arimura, K. Miyamoto, M. Velinova, M. van den Dobbelsteen, K. Mihara, R. M. Miller, M. Sawa
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AACR Annual Meeting 2022
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AS-1763: a highly potent, noncovalent and next generation BTK inhibitor for the treatment of patients with B-cell malignancies having C481S mutation in BTK
- W. Kawahata, T. Asami, T. Kiyoi, T. Irie, S. Kashimoto, H. Furuichi, K. Miyamoto, A. Arimura, M. Sawa
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Biochemical and Biophysical Research Communications
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Identification of a novel target site for ATP-independent ERK2 inhibitors
- M. Yoshida, H. Nagao, H. Sugiyama, M. Sawa, T. Kinoshita
2021
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The 50th Annual Meeting of The Japanese Society for Immunology
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Enhancement of anti-tumor effects of anti PD-1 Ab by new Bruton’s Tyrosine Kinase inhibitor through inhibiting immunosuppressive M2 like tumor associated macrophages
- R. Imagawa, T. Yaguchi, Y. Katoh, Y. Uno, M. Matsushita, M. Sawa, Y. Kawakami
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Acta Crystallographica Section F Structural Biology Communications
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Structure of mitogen-activated protein kinase kinase 1 in the DFG-out conformation
- S. Nakae, M. Kitamura, D. Fujiwara, M. Sawa, T. Shirai, I. Fujii, T. Tada
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Journal of Medicinal Chemistry
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Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers
- T. Irie, T. Asami, A. Sawa, Y. Uno, C. Taniyama, Y. Funakoshi, H. Masai, M. Sawa
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Annual Meeting of the Japanese Cancer Association
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A novel PIKfyve inhibitor, CB371 enhances the anti-tumor activity of anti-PD-1 antibody by modulating cancer immunity.
- Y. Uno, H. Matsumoto, H. Endo, Y. Katoh,T. Yaguchi, Y. Kawakami, M. Sawa
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Journal of Medicinal Chemistry
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Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton’s Tyrosine Kinase
- W. Kawahata, T. Asami, T. Kiyoi, T. Irie, S. Kashimoto, H. Furuichi, M. Sawa
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Cancers
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Possible Therapeutic Strategy Involving the Purine Synthesis Pathway Regulated by ITK in Tongue Squamous Cell Carcinoma
- K. Onidani, N. Miura, Y. Sugiura, Y. Abe, Y. Watabe, T. Kakuya, T. Mori, S. Yoshimoto, J. Adachi, T. Kiyoi, Y. Kabe, M. Suematsu , T. Tomonaga, T. Shibahara, K. Honda
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Scientific Reports
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A cell-free assay implicates a role of sphingomyelin and cholesterol in STING phosphorylation
- K. Takahashi, T. Niki, E. Ogawa, K. Fumika, Y. Nishioka, M. Sawa, H. Arai, K. Mukai, T. Taguchi
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Bioorganic & Medicinal Chemistry Letters
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Identification of an allosteric and Smad3-selective inhibitor of p38αMAPK using a substrate-based approach
- H. Nagao, D. Kitagawa, F. Nakajima, M. Sawa, T. Kinoshita
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JCI Insight
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Direct conversion of osteosarcoma to adipocytes by targeting TNIK
- T. Hirozane, M. Masuda, T. Sugano, T. Sekita, N. Goto, T. Aoyama, T. Sakagami, Y. Uno, H. Moriyama, M. Sawa, N. Asano, M. Nakamura, M. Matsumoto, R. Nakayama, T. Kondo, A. Kawai, E. Kobayashi, T. Yamada
2020
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British Journal of Cancer
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Pharmacological blockage of transforming growth factor-β signalling by a Traf2- and Nck-interacting kinase inhibitor, NCB-0846
- T. Sugano, M. Masuda, F. Takeshita, N. Motoi, T. Hirozane, N. Goto, S. Kashimoto, Y. Uno, H. Moriyama, M. Sawa, Y. Nagakawa, A. Tsuchida, M. Seike, A. Gemma, T. Yamada
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Cancers
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Feasibility of Targeting Traf2-and-Nck-Interacting Kinase in Synovial Sarcoma
- T. Sekita, T. Yamada, E. Kobayashi, A. Yoshida, T. Hirozane, A. Kawai, Y. Uno, H. Moriyama, M. Sawa, Y. Nagakawa, A. Tsuchida, M. Matsumoto, M. Nakamura, R. Nakayama, M. Masuda
2019
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Scientific Reports
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Cdc7 kinase stimulates Aurora B kinase in M-phase.
- S. Ito, H. Goto, K. Kuniyasu, M. Shindo, M. Yamada, K. Tanaka, GT. Toh, M. Sawa, M. Inagaki, J. Bartek, H. Masai
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Bioorganic & Medicinal Chemistry Letters
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An isoform-selective inhibitor of tropomyosin receptor kinase A behaves as molecular glue.
- N. Furuya, T. Momose, K. Katsuno, N. Fushimi, H. Muranaka, C. Handa, M. Sawa, T. Ozawa, T. Kinoshita
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Translational and Regulatory Sciences
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Development of split luciferase complementation probes sensing KRAS/effector interaction
- K. Miyamoto, K. Ishihara, M. Sawa
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Biochemical and Biophysical Research Communications
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Ensemble structural analyses depict the regulatory mechanism of non-phosphorylated human MAP2K4.
- T. Matsumoto, A. Yamano, Y. Murakawa, H. Fukada, M. Sawa, T. Kinoshita
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Acta Crystallographica
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A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1
- M. Tsuyuguchi, T. Nakaniwa, M. Sawa, I. Nakanishi, T. Kinoshita
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International Journal of Microgravity Science and Application
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A Microgravity Environment Improves Structural Resolution and Endows Cues for Specific Inhibition of Mitogen-Activated Protein Kinase Kinase 7
- T. Kinoshita, T. Hashimoto, T. Murakawa, T. Sogabe, T. Matsumoto, M. Sawa
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Scientific Reports
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Development of Highly Sensitive Biosensors of RAF Dimerization in Cells
- K. Miyamoto, M. Sawa
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Molecular Cancer Therapeutics
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Combined cellular and biochemical profiling to identify predictive drug response biomarkers for kinase inhibitors approved for clinical use between 2013 and 2017
- JCM. Uitdehaag, JJ. Kooijman, JADM. de Roos, MBW. Prinsen, J. Dylus, N. Willemsen-Seegers, Y. Kawase, M. Sawa, J. de Man, SJC. van Gerwen, RC. Buijsman, GJR. Zaman
2018
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16th Annual Discovery on Target
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Discovery of AS-871, a Selective and Non-Covalent BTK Inhibitor for the Treatment of Rheumatoid Arthritis
- Masaaki Sawa
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Journal of Medicinal Chemistry
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Design and Synthesis of Novel Amino-triazine Analogs as Selective Bruton’s Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis
- W. Kawahata, T. Asami, T. Kiyoi, T. Irie, H. Taniguchi, Y. Asamitsu, T. Inoue, T. Miyake, M. Sawa
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Cytotechnology
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A luciferase complementation assay system using transferable mouse artificial chromosomes to monitor protein-protein interactions mediated by G protein-coupled receptors.
- N. Uno, T. Fujimoto, S. Komoto, G. Kurosawa, M. Sawa, T. Suzuki, Y. Kazuki, M. Oshimura
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AACR Annual Meeting 2018
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Traf2-and Nck-interacting kinase (TNIK) inhibitor, NCB-0846, suppresses TGF-β1-induced epithelial-mesenchymal transition in lung cancer
- T. Sugano, M. Masuda, Y. Uno, N. Goto, M. Seike, M. Sawa, A. Gemma, T. Yamada
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AACR Annual Meeting 2018
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TRAF2 and NCK-interacting protein kinase (TNIK) regulates cancer stemness and adipogenesis of osteosarcoma cells
- T. Hirozane, M. Masuda, N. Goto, T. Sugano, N. Asano, E. Kobayashi, K. Horiuchi, H. Morioka, A. Kawai, M. Sawa, M. Matsumoto, M. Nakamura, T. Yamada
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Chemical and Pharmaceutical Bulletin
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7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors
- Takayuki Irie, Masaaki Sawa
2017
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Bioorganic & Medicinal Chemistry Letters
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Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors
- Wataru Kawahata, Tokiko Asami, Takayuki Irie, Masaaki Sawa
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AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics
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CB1763, a highly selective, novel non-covalent BTK inhibitor, targeting ibrutinib-resistant BTK C481S mutant
- Tokiko Asami, Wataru Kawahata, Shigeki Kashimoto, Masaaki Sawa
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AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics
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A novel TNIK inhibitor potently downregulates cancer stem cell population through attenuation of Wnt signaling
- Yuko Uno, Hideki Moriyama, Shigeki Kashimoto, Mari Masuda, Masaaki Sawa, Tesshi Yamada
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Medicinal Chemistry Symposium
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Design and synthesis of highly selective, non-covalent pyrimidine-based BTK inhibitor for the treatment of rheumatoid arthritis
- Wataru Kawahata, Tokiko Asami, Takayuki Irie and Masaaki Sawa
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Annual Meeting of the Japanese Cancer Association
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TNIK inhibitor reduces cancer stem cell side population by impairing Wnt signaling
- Yuko Uno, Mari Masuda, Hideki Moriyama, Masaaki Sawa, Tesshi Yamada
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Annual Meeting of the Japanese Cancer Association
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Suppression of epithelial mesenchymal transition by a novel Traf2- and Nck-interacting kinase inhibitory compound
- Teppei Sugano, Mari Masuda, Yuko Uno, Hideki Moriyama, Naoko Goto, Masahiro Seike, Masaaki Sawa, Akihiko Gemma, Tesshi Yamada
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Annual Meeting of the Japanese Cancer Association
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Preclinical development of NCB-0846, a novel TNIK inhibitor that blocks Wnt signaling in colorectal cancer
- Mari Masuda, Yuko Uno, Hideki Moriyama, Toru Hirozane, Naoko Goto, Masaaki Sawa, Tesshi Yamada
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Annual Meeting of the Japanese Cancer Association
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TRAF2 and NCK-Interacting protein kinase is a novel molecular target for osteosarcoma treatment
- Toru Hirozane, Mari Masuda, Naoko Goto, Naofumi Asano, Eisuke Kobayashi, Akira Kawai, Keisuke Horiuchi, Masaaki Sawa, Tesshi Yamada
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Biochemical and Biophysical Research Communications
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High-resolution structure discloses the potential for allosteric regulation of mitogen-activated protein kinase kinase 7
- Takayoshi Kinoshita, Takuma Hashimoto, Yuri Sogabe, Harumi Fukada, Takashi Matsumoto, Masaaki Sawa
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AACR Annual Meeting 2017
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Development of novel Btk inhibitor, CB988 targering ibrutinib-resistant Btk C481S mutant
- Wataru Kawahata, Tokiko Asami, Takayuki Irie, Yasuhiro Iwata, Takao Kiyoi, Masaaki Sawa
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European Journal of Medicinal Chemistry
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Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.
- Takayuki Irie, Tokiko Asami, Ayako Sawa, Yuko Uno, Mitsuharu Hanada, Chika Taniyama, Yoko Funakoshi, Hisao Masai, and Masaaki Sawa
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Journal of Molecular Biology
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Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.
- Nicole Willemsen-Seegers, Joost C.M. Uitdehaag, Martine B.W. Prinsen, Judith R.F. de Vetter, Jos de Man, Masaaki Sawa, Yusuke Kawase, Rogier C. Buijsman, Guido J.R. Zaman
2016
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EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics
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A Novel TNIK inhibitor, N5355 potently induced apoptotic cell death through down-regulation of Wnt signaling.
- Yuko Uno, Hideki Moriyama, Shigeki Kashimoto, Mari Masuda, Masaaki Sawa, Tesshi Yamada
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EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics
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Development of high-throughput screening assay to identify inhibitors of diacylglycerol kinases (DGKs): Utilization of DGK assay panel for the selectivity profiling of inhibitors.
- Ryoko Nakai, Mariko Hatakeyama, Yu Nishioka, Yasuyuki Kirii, Masaaki Sawa
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EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics
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Compound selectivity and target residence time of kinase inhibitors studied with surface plasmon resonance.
- N. Willemsen-Seegers, J. Uitdehaag, M. Prinsen, J. De Vetter, J. De Man, M. Sawa, Y. Kawase, R. Buijsman, G. Zaman
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EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics
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Cell panel profiling of pre-clinical and clinical anti-cancer agents reveals conserved therapeutic clusters and differentiates the mechanism of action of different PI3K/mTOR, Aurora kinase and EZH2 inhibitors.
- J.C.M. Uitdehaag, J.A.D.M. De Roos, M.B.W. Prinsen, N. Willemsen-Seegers, J.R.F. De Vetter, J. Dylus, A.M. Van Doornmalen, J. Kooijman, M. Sawa, S.J.C. Van Gerwen, J. De Man, R.C. Buijsman, G.J.R. Zaman
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Annual Meeting of the Japanese Cancer Association
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A Novel Traf2- and Nck-Interacting Kinase Inhibitor Suppresses Epithelial Mesenchymal Transition
- Teppei Sugano, Mari Masuda, Yuko Uno, Hideki Moriyama, Naoko Goto, Masahiro Seike , Masaaki Sawa, Akihiko Gemma, Tesshi Yamada
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Annual Meeting of the Japanese Cancer Association
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Developing therapeutic intervention of Wnt signaling pathway in colorectal cancer
- Mari Masuda, Yuko Uno, Hirokazu Ohata, Hideki Moriyama, Naoko Goto, Koji Okamoto, Masaaki Sawa, Tesshi Yamada
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Annual Meeting of the Japanese Cancer Association
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Inhibition of TNIK impairs cancer cell motility through attenuation of Wnt signaling
- Yuko Uno, Mari Masuda, Hideki Moriyama, Masaaki Sawa, Tesshi Yamada
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Molecular Cancer Therapeutics
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Cell panel profiling reveals conserved therapeutic clusters and differentiates the mechanism of action of different PI3K/mTOR, Aurora kinase and EZH2 inhibitors
- Joost C.M. Uitdehaag, Jeroen A.D.M. de Roos, Martine B.W. Prinsen, Nicole Willemsen-Seegers, Judith R.F. de Vetter, Jelle Dylus, Antoon M. van Doornmalen, Jeffrey Kooijman, Masaaki Sawa, Suzanne J.C. van Gerwen, Jos de Man, Rogier C. Buijsman, Guido J.R. Zaman
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Nature Communications
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TNIK inhibition abrogates colorectal cancer stemness
- Mari Masuda, Yuko Uno, Naomi Ohbayashi, Hirokazu Ohata, Ayako Mimata, Mutsuko Kukimoto-Niino, Hideki Moriyama, Shigeki Kashimoto, Tomoko Inoue, Naoko Goto, Koji Okamoto, Mikako Shirouzu, Masaaki Sawa & Tesshi Yamada
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International Symposium for Medicinal Sciences
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Fast Identification of Novel HGK Inhibitors via Click Chemistry
- Takayuki Irie, Hiroshi Ohmoto, Ikuo Fujii and Masaaki Sawa
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Biochemical and Biophysical Research Communications
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A crucial role of Cys218 in configuring an unprecedented auto-inhibition form of MAP2K7
- Yuri Sogabe, Takuma Hashimoto, Takashi Matsumoto, Yasuyuki Kirii, Masaaki Sawa, Takayoshi Kinoshita
2015
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AACR Special Conference on Developmental Biology and Cancer
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Traf2- and NCK-interacting kinase (TNIK) inhibitor down-regulates Wnt signaling pathway in cancer cells
- Yuko Uno, Hideki Moriyama, Shigeki Kashimoto, Mari Masuda, Masaaki Sawa, and Tesshi Yamada
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Pharmacology & Therapeutics
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Therapeutic targets in the Wnt signaling pathway: Feasibility of targeting TNIK in colorectal cancer (Review)
- Mari Masuda, Masaaki Sawa and Tesshi Yamada
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AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics
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Discovery of furanone derivatives as novel Cdc7 inhibitors with anti-tumor activity
- Takayuki Irie, Tokiko Asami, Ayako Sawa, Yuko Uno, Chika Taniyama, Yoko Funakoshi, Hisao Masai, and Masaaki Sawa
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Expert Opinion on Therapeutic Targets
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Targeting the Wnt signaling pathway in colorectal cancer (Review)
- Masaaki Sawa, Mari Masuda and Tesshi Yamada
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Annual Meeting of the Japanese Cancer Association
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Development of TNIK inhibitor as Wnt signal pathway modulator
- Yuko Uno, Mari Masuda, Masaaki Sawa, Tesshi Yamada
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Bioorganic & Medicinal Chemistry Letters
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TR-FRET binding assay targeting unactivated form of Bruton’s tyrosine kinase
- Tokiko Asami, Wataru Kawahata and Masaaki Sawa
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Bioorganic & Medicinal Chemistry Letters
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“Turn On/Off” fluorescence probe for the screening of unactivated Bruton’s tyrosine kinase
- Wataru Kawahata, Tokiko Asami, Ikuo Fujii, and Masaaki Sawa
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Journal of Antibiotics
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Antimalarial activity of kinase inhibitor, nilotinib, in vitro and in vivo
- Aki Ishiyama, Masato Iwatsuki, Rei Hokari, Masaaki Sawa, Satoshi Omura, and Kazuhiko Otoguro
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Bioorganic & Medicinal Chemistry Letters
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5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.
- Yuri Sogabe, Takashi Matsumoto, Takuma Hashimoto, Yasuyuki Kirii, Masaaki Sawa, Takayoshi Kinoshita
2014
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EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics
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Inhibition of Wnt pathway by novel thiazole-based Traf2- and NCK-interacting kinase (TNIK) inhibitor
- Yuko Uno, Hideki Moriyama, Shigeki Kashimoto, Mari Masuda, Masaaki Sawa, and Tesshi Yamada
2013
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AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics
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Targeting Wnt signaling: Discovery and characterization of novel thiazole-based Traf2- and NCK-interacting kinase (TNIK) inhibitors
- Yuko Uno, Hideki Moriyama, Shigeki Kashimoto, Yusuke Kawase, Miki Shitashige, Masaaki Sawa, and Tesshi Yamada
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Annual Meeting of the Japanese Cancer Association
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Development of a small-molecule inhibitor targeting TNIK protein kinase
- Tesshi Yamada, Mari Masuda, Masaaki Sawa
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CMC Publishing Co., Ltd.
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Frontiers of Protein Crystals, the chapter VI, "Crystallography and structure-based design of protein kinase inhibitors”
- Takahiro Miyake, Masaaki Sawa
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Wnt symposium 2013
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Development of a small-molecule inhibitor targeting TNIK protein kinase
- Yuko Uno, Mari Masuda, Ayako Mimata, Hideki Moriyama, Shigeki Kashimoto, Yusuke Kawase, Masaaki Sawa, and Tesshi Yamada
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Workshop on Innovation and Pioneering Technology
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Targeting kinases for non-oncology indications
- Masaaki Sawa
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Annual Meeting of the Pharmaceutical Society of Japan: Japan-Korea Joint Symposium
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Development of kinase inhibitors in non-oncology indications
- Masaaki Sawa
2011
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AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics
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The design and synthesis of a novel fluorogenic probe targeting inactive forms of Burton's tyrosine kinase for high-throughput binding assay
- Wataru Kawahata, Tokiko Asami, and Masaaki Sawa
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AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics
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A novel binding assay to identify inhibitors that bind to inactive forms of Bruton's tyrosine kinase based on fluorescence resonance energy transfer
- Tokiko Asami, Wataru Kawahata, and Masaaki Sawa
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AFMC International Medicinal Chemistry Symposium
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Role of Triazole Ring in Kinase-‐focused Evolved Fragment (KFEF) Library
- Takayuki Irie and Masaaki Sawa
2010
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Medicinal Chemistry Symposium
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Strategies for the design of selective protein kinase inhibitors.
- Masaaki Sawa
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International Chemical Congress of Pacific Basin Societies (PACIFICHEM 2010)
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Rapid discovery of kinase inhibitors using click chemistry
- Takayuki Irie and Masaaki Sawa