Publications

2017

  • 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

2016

  • 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

2015

  • 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
Masato Iwatsuki, Aki Ishiyama, 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

2014

  • 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

2013

  • 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

2012

  • 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

2011

  • 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

2010

  • 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

2008

  • 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

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