Science

• Bioorganic & Medicinal Chemistry Letters

  The discrepancies in amino acid sequence of the phosphate-binding loop lead to distinctive binding modes of a covalent inhibitor for MAP2K1 and MAP2K6: Structural insights for producing selective inhibitors

  Seigo Yumura, Kei Moritsugu, Daisuke Kitagawa, Masaaki Sawa, Takayoshi Kinoshita

• AACR Annual Meeting 2025

  Triplet combination of monzosertib, a potent CDC7 inhibitor, with DNMT and BCL2 inhibitors is highly active in human AML xenograft mouse models

  H. Furuichi, H. Endo, A. Arimura, Y. Nishioka, M. Sawa

• Bioorganic & Medicinal Chemistry Letters

  Identification of small molecule activators targeting TYK2 pseudokinase domain

  Hirokazu Matsumoto, Tien-Cheng Wang, Haruka Taniguchi, Yu Nishioka, Mariko Hatakeyama, Takayoshi Kinoshita, Masaaki Sawa

• Journal of Medicinal Chemistry

  Discovery of HM-279, a Potent Inhibitor of ALK5 for Improving Therapeutic Efficacy of Cancer Immunotherapy

  Mai Arai, Mitsuharu Hanada, Haruka Taniguchi, Fumio Nakajima, Hiroshi Ohmoto, Tsuyoshi Inoue, Kazuhito Naka, Masaaki Sawa

• Bioorganic & Medicinal Chemistry Letters

  Design and synthesis of novel triazine derivatives as antimalarial agents

  Yuko Asamitsu, Aki Ishiyama, Yui Iwamae, Rina Nagao, Rei Hokari, Masato Iwatsuki, Kazuhiko Otoguro, Masaaki Sawa

• The 66th ASH Annual Meeting & Exposition

  Preliminary Results from a Phase 1b Study of Non-Covalent Pan-Mutant BTK Inhibitor Docirbrutinib (AS-1763) in Patients with Previously Treated B-Cell Malignancies

  Nitin Jain, Catherine C. Coombs, James D'Olimpio, Nirav N. Shah, Jacqueline C. Barrientos, Seung Tae Lee, Andrew Gillis-Smith, Shuo Ma, Shirou Kirita, Masaaki Sawa, Kyoko Miyamoto, Akinori Arimura, William G. Wierda, Varsha Gandhi, Javier Pinilla-lbarz

• The 66th ASH Annual Meeting & Exposition

  Impact of Docirbrutinib (AS-1763) Treatment in CLL: Preclinical Data and Early Clinical Biomarkers

  Natalia Timofeeva, Breana Herrera, Shady I. Tantawy, Hitomi Fujiwara, Mariko Hatakeyama, Lizbeth Loza, Tokiko Asami, Hiroshi Ohmoto, Kyoko Miyamoto, Yu Nishioka, Akinori Arimura, Masaaki Sawa, Nitin Jain, Varsha Gandhi

• Clinical and Translational Science

  Safety, pharmacokinetics, and pharmacodynamics of sofnobrutinib, a novel non-covalent BTK inhibitor, in healthy subjects: First-in-human phase I study

  Kyoko Miyamoto, Robert M. Miller, Christine Voors-Pette, Jart A. F. Oosterhaven, Marieke van den Dobbelsteen, Katsuhiro Mihara, Marian Geldof, Yuji Sato, Naomi Matsuda, Shirou Kirita, Masaaki Sawa, Akinori Arimura

• EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics

  Discovery of HM-279, a novel, potent and orally active inhibitor of ALK5 for cancer immunotherapy

  Mai Arai, Mitsuharu Hanada, Haruka Taniguchi, Hideki Moriyama, Hiroshi Ohmoto, Tsuyoshi Inoue, Kazuhito Naka, Masaaki Sawa

• Bioorganic & Medicinal Chemistry Letters

  Conserved gatekeeper methionine regulates the binding and access of kinase inhibitors to ATP sites of MAP2K1, 4, and 7: Clues for developing selective inhibitors

  S. Yumura, D. Kitagawa, K. Moritsugu, A. Nakayama, T. Shinada, M. Sawa, T. Kinoshita

• EHA 2024 Hybrid Congress

  Preliminary safety and efficacy results from a Phase 1b study of oral non-covalent BTK inhibitor AS-1763 in patients with previously treated B-cell malignancies

  N. Jain, C.C. Coombs, J. D’Olimpio, N. N. Shah, J. Barrientos, S. T. Lee, A. Gillis-Smith, S. Ma, S. Kirita, M. Sawa, K. Miyamoto, A. Arimura, W. G. Wierda, V. Gandhi, J. Pinilla-Ibarz

• Bioorganic & Medicinal Chemistry Letters

  Design and synthesis of novel thiazole-derivatives as potent ALK5 inhibitors

  Mai Arai, Mitsuharu Hanada, Hideki Moriyama, Hiroshi Ohmoto, Takahiro Miyake, Kazuhito Naka, Masaaki Sawa

• AACR Annual Meeting 2024

  Synergistic effect of the CDC7 inhibitor, monzosertib (AS-0141) with current therapies in AML models

  H. Endo, H. Furuichi, A. Arimura, Y. Nishioka, M. Sawa

• Biochemical and Biophysical Research Communications

  Distinct binding modes of a benzothiazole derivative confer structural bases for increasing ERK2 or p38α MAPK selectivity

  Seisuke Hasegawa, Mayu Yoshida, Haruna Nagao, Hajime Sugiyama, Masaaki Sawa, Takayoshi Kinoshita

• Nature Communications

  Single-molecule localization microscopy reveals STING clustering at the trans-Golgi network through palmitoylation-dependent accumulation of cholesterol

  Haruka Kemmoku, Kanoko Takahashi, Kojiro Mukai, Toshiki Mori, Koichiro Hirosawa, Fumika Kiku, Yasunori Uchida, Yoshihiko Kuchitsu, Yu Nishioka, Masaaki Sawa, Takuma Kishimoto, Kazuma Tanaka, Yasunari Yokota, Hiroyuki Arai, and Kenichi Suzuki, Tomohiko Taguchi

• The 65th ASH Annual Meeting & Exposition

  Trial in Progress: A Phase 1b Study of AS-1763, an Oral, Potent and Selective Noncovalent BTK Inhibitor, in Patients with Previously Treated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma or Non-Hodgkin Lymphoma

  Nitin Jain, James D’Olimpio, Andrew Gillis-Smith, Seung Tae Lee, Nirav N. Shah, Javier Pinilla-Ibarz, Catherine Coombs, Jacqueline Barrientos, Shuo Ma, Masaaki Sawa, Kyoko Miyamoto, Akinori Arimura, Varsha Gandhi, William G. Wierda

• The 65th ASH Annual Meeting & Exposition

  Characterization and Preclinical Evaluation of AS-1763, an oral, Potent and Selective Noncovalent BTK inhibitor, in Chronic Lymphocytic Leukemia

  Shady I. Tantawy, Natalia Timofeeva, Hitomi Fujiwara, Mariko Hatakeyama, Breana Herrea, Lizbeth Loza, Tokiko Asami, Hiroshi Ohmoto, Kyoko Miyamoto, Yu Nishioka, Akinori Arimura, Masaaki Sawa, Nitin Jain, Varsha Gandhi

• Expert Opinion On Therapeutic Patents

  CDC7 kinase inhibitors: a survey of recent patent literature (2017-2022)

  Takayuki Irie, Masaaki Sawa

• Annual Meeting of the Japanese Cancer Association

  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

• Bioorganic & Medicinal Chemistry Letters

  Low entropic cost of binding confers high selectivity on an allosteric ERK2 inhibitor

  H. Sugiyama, M. Yoshida, H. Nagao, M. Sawa, T. Kinoshita

• Arteriosclerosis, Thrombosis, and Vascular Biology

  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

• AACR Annual Meeting 2023

  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

• Biochemical and Biophysical Research Communications

  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

• AACR Annual Meeting 2022

  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

• AACR Annual Meeting 2022

  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

• Biochemical and Biophysical Research Communications

  Identification of a novel target site for ATP-independent ERK2 inhibitors

  M. Yoshida, H. Nagao, H. Sugiyama, M. Sawa, T. Kinoshita

• The 50th Annual Meeting of The Japanese Society for Immunology

  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

• Acta Crystallographica Section F Structural Biology Communications

  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

• Journal of Medicinal Chemistry

  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

• Annual Meeting of the Japanese Cancer Association

  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

• Journal of Medicinal Chemistry

  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

• Cancers

  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

• Scientific Reports

  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

• Bioorganic & Medicinal Chemistry Letters

  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

• JCI Insight

  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

• British Journal of Cancer

  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

• Cancers

  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

• Scientific Reports

  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

• Bioorganic & Medicinal Chemistry Letters

  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

• Translational and Regulatory Sciences

  Development of split luciferase complementation probes sensing KRAS/effector interaction

  K. Miyamoto, K. Ishihara, M. Sawa

• Biochemical and Biophysical Research Communications

  Ensemble structural analyses depict the regulatory mechanism of non-phosphorylated human MAP2K4.

  T. Matsumoto, A. Yamano, Y. Murakawa, H. Fukada, M. Sawa, T. Kinoshita

• Acta Crystallographica

  A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1

  M. Tsuyuguchi, T. Nakaniwa, M. Sawa, I. Nakanishi, T. Kinoshita

• International Journal of Microgravity Science and Application

  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

• Scientific Reports

  Development of Highly Sensitive Biosensors of RAF Dimerization in Cells

  K. Miyamoto, M. Sawa

• Molecular Cancer Therapeutics

  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

• 16th Annual Discovery on Target

  Discovery of AS-871, a Selective and Non-Covalent BTK Inhibitor for the Treatment of Rheumatoid Arthritis

  Masaaki Sawa

• Journal of Medicinal Chemistry

  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

• Cytotechnology

  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

• AACR Annual Meeting 2018

  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

• AACR Annual Meeting 2018

  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

• Chemical and Pharmaceutical Bulletin

  7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors

  Takayuki Irie, Masaaki Sawa

• Bioorganic & Medicinal Chemistry Letters

  Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors

  Wataru Kawahata, Tokiko Asami, Takayuki Irie, Masaaki Sawa

• AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics

  CB1763, a highly selective, novel non-covalent BTK inhibitor, targeting ibrutinib-resistant BTK C481S mutant

  Tokiko Asami, Wataru Kawahata, Shigeki Kashimoto, Masaaki Sawa

• AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics

  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

• Medicinal Chemistry Symposium

  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

• Annual Meeting of the Japanese Cancer Association

  TNIK inhibitor reduces cancer stem cell side population by impairing Wnt signaling

  Yuko Uno, Mari Masuda, Hideki Moriyama, Masaaki Sawa, Tesshi Yamada

• Annual Meeting of the Japanese Cancer Association

  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

• Annual Meeting of the Japanese Cancer Association

  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

• Annual Meeting of the Japanese Cancer Association

  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

• Biochemical and Biophysical Research Communications

  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

• AACR Annual Meeting 2017

  Development of novel Btk inhibitor, CB988 targering ibrutinib-resistant Btk C481S mutant

  Wataru Kawahata, Tokiko Asami, Takayuki Irie, Yasuhiro Iwata, Takao Kiyoi, Masaaki Sawa

• European Journal of Medicinal Chemistry

  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

• Journal of Molecular Biology

  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

• EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics

  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

• EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics

  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

• EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics

  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

• EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics

  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

• Annual Meeting of the Japanese Cancer Association

  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

• Annual Meeting of the Japanese Cancer Association

  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

• Annual Meeting of the Japanese Cancer Association

  Inhibition of TNIK impairs cancer cell motility through attenuation of Wnt signaling

  Yuko Uno, Mari Masuda, Hideki Moriyama, Masaaki Sawa, Tesshi Yamada

• Molecular Cancer Therapeutics

  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

• Nature Communications

  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

• International Symposium for Medicinal Sciences

  Fast Identification of Novel HGK Inhibitors via Click Chemistry

  Takayuki Irie, Hiroshi Ohmoto, Ikuo Fujii and Masaaki Sawa

• Biochemical and Biophysical Research Communications

  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

• AACR Special Conference on Developmental Biology and Cancer

  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

• Pharmacology & Therapeutics

  Therapeutic targets in the Wnt signaling pathway: Feasibility of targeting TNIK in colorectal cancer (Review)

  Mari Masuda, Masaaki Sawa and Tesshi Yamada

• AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics

  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

• Expert Opinion on Therapeutic Targets

  Targeting the Wnt signaling pathway in colorectal cancer (Review)

  Masaaki Sawa, Mari Masuda and Tesshi Yamada

• Annual Meeting of the Japanese Cancer Association

  Development of TNIK inhibitor as Wnt signal pathway modulator

  Yuko Uno, Mari Masuda, Masaaki Sawa, Tesshi Yamada

• Bioorganic & Medicinal Chemistry Letters

  TR-FRET binding assay targeting unactivated form of Bruton’s tyrosine kinase

  Tokiko Asami, Wataru Kawahata and Masaaki Sawa

• Bioorganic & Medicinal Chemistry Letters

  “Turn On/Off” fluorescence probe for the screening of unactivated Bruton’s tyrosine kinase

  Wataru Kawahata, Tokiko Asami, Ikuo Fujii, and Masaaki Sawa

• Journal of Antibiotics

  Antimalarial activity of kinase inhibitor, nilotinib, in vitro and in vivo

  Aki Ishiyama, Masato Iwatsuki, Rei Hokari, Masaaki Sawa, Satoshi Omura, and Kazuhiko Otoguro

• Bioorganic & Medicinal Chemistry Letters

  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

• EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics

  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

• AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics

  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

• Annual Meeting of the Japanese Cancer Association

  Development of a small-molecule inhibitor targeting TNIK protein kinase

  Tesshi Yamada, Mari Masuda, Masaaki Sawa

• CMC Publishing Co., Ltd.

  Frontiers of Protein Crystals, the chapter VI, "Crystallography and structure-based design of protein kinase inhibitors”

  Takahiro Miyake, Masaaki Sawa

• Wnt symposium 2013

  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

• Workshop on Innovation and Pioneering Technology

  Targeting kinases for non-oncology indications

  Masaaki Sawa

• Annual Meeting of the Pharmaceutical Society of Japan: Japan-Korea Joint Symposium

  Development of kinase inhibitors in non-oncology indications

  Masaaki Sawa

• Bioorganic & Medicinal Chemistry Letters

  Design and combinatorial synthesis of a novel kinase-focused library using click chemistry-based fragment assembly

  Takayuki Irie, Ikuo Fujii and Masaaki Sawa

• MEDCHEM NEWS

  Drug Discovery Research at Carna Biosciences

  Masaaki Sawa

• AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics

  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

• AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics

  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

• AFMC International Medicinal Chemistry Symposium

  Role of Triazole Ring in Kinase-­‐focused Evolved Fragment (KFEF) Library

  Takayuki Irie and Masaaki Sawa

• Medicinal Chemistry Symposium

  Strategies for the design of selective protein kinase inhibitors.

  Masaaki Sawa

• International Chemical Congress of Pacific Basin Societies (PACIFICHEM 2010)

  Rapid discovery of kinase inhibitors using click chemistry

  Takayuki Irie and Masaaki Sawa

• CMC Publishing Co., Ltd.

  Hilight in Medicinal and Process Research, the 11th chapter "Kinase Inhibitor -Impact on Drug Discovery-"

  Masaaki Sawa

• Mini Reviews in Medicinal Chemistry

  Strategies for the Design of Selective Protein Kinase Inhibitors

  Masaaki Sawa

• Drug Design, Development and Therapy

  Drug design with Cdc7 kinase: a potential novel cancer therapy target

  Masaaki Sawa and Hisao Masai