カルナバイオサイエンス株式会社

カルナバイオサイエンス株式会社

Science発表・論文

2024

2023

  • 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
  • 日本癌学会学術総会

    新規ALK5阻害剤AL2による腫瘍免疫を介した抗腫瘍効果の検討
    澤匡明、新井真以、花田充治、森山英樹、大本弘志、仲一仁
  • 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

2022

  • 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

2021

2020

2019

2018

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
  • メディシナルケミストリーシンポジウム

    関節リウマチ治療薬を目指したピリミジン骨格を有する非共有結合型選択的BTK 阻害剤の創製研究
    川畑亘,浅見斉子,入江隆行,澤匡明
  • 日本癌学会学術総会

    TNIK 阻害剤はWnt シグナルを減弱させてがん幹細胞画分を減少させる
    宇野佑子、増田万里、森山英樹、澤匡明、山田哲司
  • 日本癌学会学術総会

    新規TNIK 阻害薬によるEMT 制御
    菅野哲平、増田万里、宇野佑子、森山英樹、後藤尚子、清家正博、澤匡明、弦間昭彦、山田哲司
  • 日本癌学会学術総会

    大腸がん幹細胞を標的とする新規TNIK 阻害剤NCB-0846 が作用する分子ネットワークの解明
    増田万里、宇野佑子、森山英樹、弘實透、後藤尚子、澤匡明、山田哲司
  • 日本癌学会学術総会

    TNIK は骨肉腫の新規治療標的となりうる
    弘實透、増田万里、後藤尚子、浅野尚文、小林英介、川井章、堀内圭輔、澤匡明、山田哲司
  • 日本分子腫瘍マーカー研究会

    骨肉腫治療におけるTNIK 阻害剤の可能性
    弘實 透、増田 万里、後藤 尚子、菅野 哲平、浅野 尚文、小林 英介、川井 章、堀内 圭輔、松本 守雄、中村 雅也、澤 匡明、森岡 秀夫、山田 哲司
  • 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
  • 日本癌学会学術総会

    新規TNIK阻害薬によるEMT制御
    菅野哲平、増田万里、宇野佑子、森山英樹、後藤尚子、清家正博、澤 匡明、弦間昭彦、山田哲司
  • 日本癌学会学術総会

    Wntシグナル遮断による大腸がん幹細胞根絶を目的としたTNIK阻害剤の開発
    増田万里、宇野佑子、大畑広和、森山英樹、後藤尚子、岡本康司、澤 匡明、山田哲司
  • 日本癌学会学術総会

    TNIK阻害剤はWntシグナルを遮断して細胞遊走を抑制する
    宇野佑子、増田万里、森山英樹、澤 匡明、山田哲司
  • 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

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
  • 日本癌学会学術総会

    TNIK キナーゼを標的とした分子治療薬の開発
    山田哲司、増田万里、澤匡明
  • (株)シーエムシー出版

    タンパク質結晶の最前線 第VI編 第2章 キナーゼ結晶構造情報を活用したドラッグデザイン
    三宅隆弘、澤匡明
  • 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

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

  • メディシナルケミストリーシンポジウム

    キナーゼ選択性プロファイリングを活用したキナーゼ阻害薬研究
    澤 匡明
  • International Chemical Congress of Pacific Basin Societies (PACIFICHEM 2010)

    Rapid discovery of kinase inhibitors using click chemistry
    Takayuki Irie and Masaaki Sawa

2008