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Journal Articles

TAS0612, a Novel RSK, AKT, and S6K Inhibitor, Exhibits Antitumor Effects in Preclinical Tumor Models

Koji Ichikawa, Satoshi Ito, Emi Kato, Naomi Abe, Takumitsu Machida, Junya Iwasaki, Gotaro Tanaka, Hikari Araki, Kentaro Wakayama, Hideki Jona, Tetsuya Sugimoto, Kazutaka Miyadera, Shuichi Ohkubo

Mol Cancer Ther (2024) 23 (2): 174–186.

https://doi.org/10.1158/1535-7163.MCT-21-1037

Published: 01 February 2024

View article titled, TAS0612, a Novel RSK, AKT, and S6K Inhibitor, Exhibits Antitumor Effects in Preclinical Tumor Models

Includes: Supplementary data

Journal Articles

Abstract P06-02: Discovery of TAS0953/HM06, a novel next generation RET-specific inhibitor capable of inhibiting RET solvent front mutations

Isao Miyazaki, Keiji Ishida, Masanori Kato, Tatsuya Suzuki, Hidenori Fujita, Shuichi Ohkubo, Yoshikazu Iwasawa

Mol Cancer Ther (2021) 20 (12_Supplement): P06-02.

https://doi.org/10.1158/1535-7163.TARG-21-P06-02

Published: 01 December 2021

View article titled, Abstract P06-02: Discovery of TAS0953/HM06, a novel next generation RET-specific inhibitor capable of inhibiting RET solvent front mutations

Journal Articles

Abstract A126: Acquired resistance to trastuzumab/pertuzumab, or to T-DM1 in vivo can be overcome by HER2 inhibition with TAS0728

Hiroki Irie, Rumi Kawabata, Yayoi Fujioka, Fumio Nakagawa, Hideki Nagase, Hiraku Itadani, Kimihiro Ito, Junji Uchida, Shuichi Ohkubo, Kenichi Matsuo, Takeshi Sagara, Teruhiro Utsugi

Mol Cancer Ther (2019) 18 (12_Supplement): A126.

https://doi.org/10.1158/1535-7163.TARG-19-A126

Published: 01 December 2019

View article titled, Abstract A126: Acquired resistance to trastuzumab/pertuzumab, or to T-DM1 <em>in vivo</em> can be overcome by HER2 inhibition with TAS0728

Journal Articles

TAS4464, A Highly Potent and Selective Inhibitor of NEDD8-Activating Enzyme, Suppresses Neddylation and Shows Antitumor Activity in Diverse Cancer Models

Chihoko Yoshimura, Hiromi Muraoka, Hiroaki Ochiiwa, Shingo Tsuji, Akihiro Hashimoto, Hiromi Kazuno, Fumio Nakagawa, Yu Komiya, Satoshi Suzuki, Toru Takenaka, Masafumi Kumazaki, Naoya Fujita, Takashi Mizutani, Shuichi Ohkubo

Mol Cancer Ther (2019) 18 (7): 1205–1216.

https://doi.org/10.1158/1535-7163.MCT-18-0644

Published: 01 July 2019

View article titled, TAS4464, A Highly Potent and Selective Inhibitor of NEDD8-Activating Enzyme, Suppresses Neddylation and Shows Antitumor Activity in Diverse Cancer Models

Includes: Supplementary data

Journal Articles

TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models

Hiroki Irie, Kimihiro Ito, Yayoi Fujioka, Kei Oguchi, Akio Fujioka, Akihiro Hashimoto, Hirokazu Ohsawa, Kenji Tanaka, Kaoru Funabashi, Hikari Araki, Yuichi Kawai, Tadashi Shimamura, Renu Wadhwa, Shuichi Ohkubo, Kenichi Matsuo

Mol Cancer Ther (2019) 18 (4): 733–742.

https://doi.org/10.1158/1535-7163.MCT-18-1085

Published: 01 April 2019

View article titled, TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models

Includes: Supplementary data

Journal Articles

First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors

Akihiko Shimomura, Noboru Yamamoto, Shunsuke Kondo, Yutaka Fujiwara, Shigenobu Suzuki, Noriko Yanagitani, Atsushi Horiike, Satoru Kitazono, Fumiyoshi Ohyanagi, Toshihiko Doi, Yasutoshi Kuboki, Akihito Kawazoe, Kohei Shitara, Izumi Ohno, Udai Banerji, Raghav Sundar, Shuichi Ohkubo, Elizabeth M. Calleja, Makoto Nishio

Mol Cancer Ther (2019) 18 (3): 531–540.

https://doi.org/10.1158/1535-7163.MCT-18-0831

Published: 01 March 2019

View article titled, First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors

Journal Articles

Abstract B136: NEDD8-activating enzyme inhibitor TAS4464 inhibits tumor growth in endometrial cancer mouse model accompanied by DNA damage response

Yu Komiya, Chihoko Yoshimura, Hiromi Muraoka, Shuichi Ohkubo, Fumio Nakagawa, Hiroaki Ochiiwa, Hiroshi Sootome, Takashi Mizutani, Kenichi Matsuo, Teruhiro Utsugi, Yoshikazu Iwasawa

Mol Cancer Ther (2018) 17 (1_Supplement): B136.

https://doi.org/10.1158/1535-7163.TARG-17-B136

Published: 01 January 2018

View article titled, Abstract B136: NEDD8-activating enzyme inhibitor TAS4464 inhibits tumor growth in endometrial cancer mouse model accompanied by DNA damage response

Journal Articles

Abstract C178: TAS4464, a novel NEDD8 activating enzyme inhibitor, potently induces cell death via both intrinsic and extrinsic apoptotic pathways in acute myeloid leukemia

Hiroaki Ochiiwa, Chihoko Yoshimura, Hiromi Muraoka, Keiji Ishida, Tomonori Haruma, Shingo Tsuji, Akihiro Hashimoto, Takashi Mizutani, Shuichi Ohkubo, Kenichi Matsuo, Teruhiro Utsugi, Yoshikazu Iwasawa

Mol Cancer Ther (2015) 14 (12_Supplement_2): C178.

https://doi.org/10.1158/1535-7163.TARG-15-C178

Published: 01 December 2015

View article titled, Abstract C178: TAS4464, a novel NEDD8 activating enzyme inhibitor, potently induces cell death via both intrinsic and extrinsic apoptotic pathways in acute myeloid leukemia

Journal Articles

Abstract C177: TAS4464, a novel and highly potent inhibitor of NEDD8 activating enzyme, overcomes insensitivity to BTK, PI3Kδ, and IRAK4 inhibitors in activated B-cell like diffuse large B-cell lymphoma via inactivation of the NF-κB pathway

Hiromi Muraoka, Chihoko Yoshimura, Shingo Tsuji, Akihiro Hashimoto, Takashi Mizutani, Shuichi Ohkubo, Kenichi Matsuo, Teruhiro Utsugi, Yoshikazu Iwasawa

Mol Cancer Ther (2015) 14 (12_Supplement_2): C177.

https://doi.org/10.1158/1535-7163.TARG-15-C177

Published: 01 December 2015

View article titled, Abstract C177: TAS4464, a novel and highly potent inhibitor of NEDD8 activating enzyme, overcomes insensitivity to BTK, PI3Kδ, and IRAK4 inhibitors in activated B-cell like diffuse large B-cell lymphoma via inactivation of the NF-κB pathway

Journal Articles

Abstract C176: TAS4464, a novel, highly potent, and selective inhibitor of NEDD8 activating enzyme demonstrates sustained target inhibition and antitumor activity in a preclinical model

Chihoko Yoshimura, Hiromi Muraoka, Hiroaki Ochiiwa, Shingo Tsuji, Akihiro Hashimoto, Toru Takenaka, Hiromi Kazuno, Keiji Ishida, Takashi Mizutani, Shuichi Ohkubo, Kenichi Matsuo, Teruhiro Utsugi, Yoshikazu Iwasawa

Mol Cancer Ther (2015) 14 (12_Supplement_2): C176.

https://doi.org/10.1158/1535-7163.TARG-15-C176

Published: 01 December 2015

View article titled, Abstract C176: TAS4464, a novel, highly potent, and selective inhibitor of NEDD8 activating enzyme demonstrates sustained target inhibition and antitumor activity in a preclinical model

Journal Articles

Abstract B87: First-in-human phase I dose escalation study of TAS-116, a novel, orally active HSP90α and HSP90β selective inhibitor, in patients with advanced solid tumors

Akihiko Shimomura, Atsushi Horiike, Yuichi Tambo, Fumiyoshi Ohyanagi, Noriko Yanagitani, Satoru Kitazono, Yutaka Fujiwara, Yuko Tanabe, Shuichi Ohkubo, Noboru Yamamoto, Makoto Nishio

Mol Cancer Ther (2015) 14 (12_Supplement_2): B87.

https://doi.org/10.1158/1535-7163.TARG-15-B87

Published: 01 December 2015

View article titled, Abstract B87: First-in-human phase I dose escalation study of TAS-116, a novel, orally active HSP90α and HSP90β selective inhibitor, in patients with advanced solid tumors

Journal Articles

TAS-116, a Highly Selective Inhibitor of Heat Shock Protein 90α and β, Demonstrates Potent Antitumor Activity and Minimal Ocular Toxicity in Preclinical Models

Shuichi Ohkubo, Yasuo Kodama, Hiromi Muraoka, Hiroko Hitotsumachi, Chihoko Yoshimura, Makoto Kitade, Akihiro Hashimoto, Kenjiro Ito, Akira Gomori, Koichi Takahashi, Yoshihiro Shibata, Akira Kanoh, Kazuhiko Yonekura

Mol Cancer Ther (2015) 14 (1): 14–22.

https://doi.org/10.1158/1535-7163.MCT-14-0219

Published: 13 January 2015

View article titled, TAS-116, a Highly Selective Inhibitor of Heat Shock Protein 90α and β, Demonstrates Potent Antitumor Activity and Minimal Ocular Toxicity in Preclinical Models

Includes: Supplementary data

Journal Articles

Abstract C129: TAS-116, an orally available HSP90α and β selective inhibitor, exhibits synergistic effects in combination with taxanes in EGFR-tyrosine kinase inhibitor-resistant human NSCLC xenograft models through the downregulation of key molecules involved in drug resistance of cancer chemotherapy.

Hiromi Muraoka, Akira Kanoh, Akihiro Hashimoto, Kenjiro Ito, Takamasa Suzuki, Kouichi Takahashi, Chihoko Yoshimura, Makoto Kitade, Kazuhiko Yonekura, Shuichi Ohkubo, Teruhiro Utsugi

Mol Cancer Ther (2013) 12 (11_Supplement): C129.

https://doi.org/10.1158/1535-7163.TARG-13-C129

Published: 01 November 2013

View article titled, Abstract C129: TAS-116, an orally available HSP90α and β selective inhibitor, exhibits synergistic effects in combination with taxanes in EGFR-tyrosine kinase inhibitor-resistant human NSCLC xenograft models through the downregulation of key molecules involved in drug resistance of cancer chemotherapy.

Journal Articles

Abstract C128: TAS-116, an orally available HSP90α/β selective inhibitor, has potent antitumor activity in small cell lung cancer as a single agent and in combination with an anthracycline derivative, amrubicin.

Hiromi Muraoka, Chihoko Yoshimura, Akihiro Hashimoto, Kenjiro Ito, Makoto Kitade, Kazuhiko Yonekura, Shuichi Ohkubo, Teruhiro Utsugi

Mol Cancer Ther (2013) 12 (11_Supplement): C128.

https://doi.org/10.1158/1535-7163.TARG-13-C128

Published: 01 November 2013

View article titled, Abstract C128: TAS-116, an orally available HSP90α/β selective inhibitor, has potent antitumor activity in small cell lung cancer as a single agent and in combination with an anthracycline derivative, amrubicin.

Journal Articles

Abstract C127: TAS-116, an orally available HSP90α/β selective inhibitor: Synthesis and biological evaluation.

Takao Uno, Makoto Kitade, Satoshi Yamashita, Hiromi Oshiumi, Yuichi Kawai, Takashi Mizutani, Chihoko Yoshimura, Yasuo Kodama, Hiromi Muraoka, Kouichi Takahashi, Kazuhiko Yonekura, Shuichi Ohkubo, Teruhiro Utsugi

Mol Cancer Ther (2013) 12 (11_Supplement): C127.

https://doi.org/10.1158/1535-7163.TARG-13-C127

Published: 01 November 2013

View article titled, Abstract C127: TAS-116, an orally available HSP90α/β selective inhibitor: Synthesis and biological evaluation.

NARROW

TAS0612, a Novel RSK, AKT, and S6K Inhibitor, Exhibits Antitumor Effects in Preclinical Tumor Models

Abstract P06-02: Discovery of TAS0953/HM06, a novel next generation RET-specific inhibitor capable of inhibiting RET solvent front mutations

Abstract A126: Acquired resistance to trastuzumab/pertuzumab, or to T-DM1 in vivo can be overcome by HER2 inhibition with TAS0728

TAS4464, A Highly Potent and Selective Inhibitor of NEDD8-Activating Enzyme, Suppresses Neddylation and Shows Antitumor Activity in Diverse Cancer Models

TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models

First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors

Abstract B136: NEDD8-activating enzyme inhibitor TAS4464 inhibits tumor growth in endometrial cancer mouse model accompanied by DNA damage response

Abstract C178: TAS4464, a novel NEDD8 activating enzyme inhibitor, potently induces cell death via both intrinsic and extrinsic apoptotic pathways in acute myeloid leukemia

Abstract C177: TAS4464, a novel and highly potent inhibitor of NEDD8 activating enzyme, overcomes insensitivity to BTK, PI3Kδ, and IRAK4 inhibitors in activated B-cell like diffuse large B-cell lymphoma via inactivation of the NF-κB pathway

Abstract C176: TAS4464, a novel, highly potent, and selective inhibitor of NEDD8 activating enzyme demonstrates sustained target inhibition and antitumor activity in a preclinical model

Abstract B87: First-in-human phase I dose escalation study of TAS-116, a novel, orally active HSP90α and HSP90β selective inhibitor, in patients with advanced solid tumors

TAS-116, a Highly Selective Inhibitor of Heat Shock Protein 90α and β, Demonstrates Potent Antitumor Activity and Minimal Ocular Toxicity in Preclinical Models

Abstract C128: TAS-116, an orally available HSP90α/β selective inhibitor, has potent antitumor activity in small cell lung cancer as a single agent and in combination with an anthracycline derivative, amrubicin.

Abstract C127: TAS-116, an orally available HSP90α/β selective inhibitor: Synthesis and biological evaluation.

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