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

doi:10.1158/1535-7163.mct-14-0219

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

Molecular Cancer Therapeutics ◽

10.1158/1535-7163.mct-14-0219 ◽

2014 ◽

Vol 14 (1) ◽

pp. 14-22 ◽

Cited By ~ 43

Author(s):

Shuichi Ohkubo ◽

Yasuo Kodama ◽

Hiromi Muraoka ◽

Hiroko Hitotsumachi ◽

Chihoko Yoshimura ◽

...

Keyword(s):

Heat Shock ◽

Antitumor Activity ◽

Heat Shock Protein ◽

Selective Inhibitor ◽

Ocular Toxicity ◽

Preclinical Models

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In vivo-in vitro correlation of antitumor activity of heat shock protein 90 (HSP90) inhibitors with a pharmacokinetics/pharmacodynamics analysis using NCI-N87 xenograft mice

Xenobiotica ◽

10.1080/00498254.2021.1942588 ◽

2021 ◽

pp. 1-30

Author(s):

Noriaki Ohminato ◽

Miho Nagayasu ◽

Kazuhisa Ozeki ◽

Ryoichi Saitoh ◽

Naomi Ono ◽

...

Keyword(s):

Heat Shock ◽

Antitumor Activity ◽

Heat Shock Protein ◽

Heat Shock Protein 90 ◽

Hsp90 Inhibitors ◽

Xenograft Mice

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Abstract C212: A critical role for the tissue distribution profile in heat shock protein (Hsp) 90 inhibitor-induced ocular toxicity in rats.

10.1158/1535-7163.targ-11-c212 ◽

2011 ◽

Cited By ~ 6

Author(s):

Dan Zhou ◽

Yuan Liu ◽

Josephine Ye ◽

Weiwen Ying ◽

Shijie Zhang ◽

...

Keyword(s):

Heat Shock ◽

Heat Shock Protein ◽

Tissue Distribution ◽

Critical Role ◽

Ocular Toxicity ◽

Distribution Profile ◽

Hsp 90 ◽

Tissue Distribution Profile

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Antitumor activity of NVP-AUY922, a novel heat shock protein 90 inhibitor, in human gastric cancer cells is mediated through proteasomal degradation of client proteins

Cancer Science ◽

10.1111/j.1349-7006.2011.01944.x ◽

2011 ◽

Vol 102 (7) ◽

pp. 1388-1395 ◽

Cited By ~ 34

Author(s):

Kyung-Hun Lee ◽

Ju-Hee Lee ◽

Sae-Won Han ◽

Seock-Ah Im ◽

Tae-You Kim ◽

...

Keyword(s):

Gastric Cancer ◽

Heat Shock ◽

Antitumor Activity ◽

Heat Shock Protein ◽

Cancer Cells ◽

Heat Shock Protein 90 ◽

Proteasomal Degradation ◽

Human Gastric Cancer ◽

Gastric Cancer Cells ◽

Client Proteins

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375 A Phase 1 dose escalation study of the oral heat shock protein 90 (Hsp90) inhibitor PF-04929113/SNX-5422 (PF-113) and its associated ocular toxicity

European Journal of Cancer Supplements ◽

10.1016/s1359-6349(10)72082-6 ◽

2010 ◽

Vol 8 (7) ◽

pp. 119 ◽

Cited By ~ 5

Author(s):

J. Infante ◽

G. Weiss ◽

S. Jones ◽

R. Tibes ◽

J. Bendell ◽

...

Keyword(s):

Heat Shock ◽

Heat Shock Protein ◽

Dose Escalation ◽

Phase 1 ◽

Heat Shock Protein 90 ◽

Hsp90 Inhibitor ◽

Ocular Toxicity ◽

Dose Escalation Study

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Preclinical antitumor activity of the novel heat shock protein 90 inhibitor CH5164840 against human epidermal growth factor receptor 2 (HER2)-overexpressing cancers

Cancer Science ◽

10.1111/j.1349-7006.2011.02144.x ◽

2011 ◽

Vol 103 (2) ◽

pp. 342-349 ◽

Cited By ~ 18

Author(s):

Naomi Ono ◽

Toshikazu Yamazaki ◽

Yoshito Nakanishi ◽

Toshihiko Fujii ◽

Kiyoaki Sakata ◽

...

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Heat Shock ◽

Epidermal Growth Factor ◽

Antitumor Activity ◽

Heat Shock Protein ◽

Growth Factor Receptor ◽

Heat Shock Protein 90 ◽

The Novel ◽

Epidermal Growth

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Abstract 3433: Deciphering the mechanism of synergy between the Heat Shock Protein 90 inhibitor retaspimycin HCl and docetaxel in preclinical models of non-small cell lung cancer.

10.1158/1538-7445.am2013-3433 ◽

2013 ◽

Author(s):

Katie O'Callaghan ◽

Brenda C. O'Connell ◽

Bonnie Tillotson ◽

Mark Douglas ◽

Howard Stern ◽

...

Keyword(s):

Lung Cancer ◽

Heat Shock ◽

Heat Shock Protein ◽

Small Cell Lung Cancer ◽

Cell Lung Cancer ◽

Heat Shock Protein 90 ◽

Small Cell ◽

Preclinical Models ◽

Small Cell Lung

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592 TAS-116, a highly selective inhibitor of heat shock protein 90a/β, inhibits tumor growth in biliary tract cancer mouse models

European Journal of Cancer ◽

10.1016/s0959-8049(14)70718-x ◽

2014 ◽

Vol 50 ◽

pp. 191

Author(s):

S. Ohkubo ◽

H. Muraoka ◽

Y. Kodama ◽

K. Ito ◽

S. Ito ◽

...

Keyword(s):

Heat Shock ◽

Heat Shock Protein ◽

Tumor Growth ◽

Mouse Models ◽

Biliary Tract ◽

Biliary Tract Cancer ◽

Selective Inhibitor ◽

Tract Cancer

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Antitumor activity of mixed heat shock protein/peptide vaccine and cyclophosphamide plus interleukin-12 in mice sarcoma

Journal of Experimental & Clinical Cancer Research ◽

10.1186/1756-9966-30-24 ◽

2011 ◽

Vol 30 (1) ◽

pp. 24 ◽

Cited By ~ 14

Author(s):

Quan-Yi Guo ◽

Mei Yuan ◽

Jiang Peng ◽

Xue-Mei Cui ◽

Ge Song ◽

...

Keyword(s):

Heat Shock ◽

Antitumor Activity ◽

Heat Shock Protein ◽

Peptide Vaccine ◽

Interleukin 12

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Discovery of a covalent inhibitor of heat shock protein 90 with antitumor activity that blocks the co-chaperone binding via C-terminal modification

Cell Chemical Biology ◽

10.1016/j.chembiol.2021.03.016 ◽

2021 ◽

Author(s):

Li Li ◽

Nannan Chen ◽

Dandan Xia ◽

Shicheng Xu ◽

Wei Dai ◽

...

Keyword(s):

Heat Shock ◽

Antitumor Activity ◽

Heat Shock Protein ◽

Heat Shock Protein 90 ◽

Chaperone Binding ◽

Covalent Inhibitor

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Abstract 2770: Antitumor activity of heat shock protein 90 (HSP90) inhibitor AT13387 in head and neck squamous cell carcinoma

10.1158/1538-7445.am2012-2770 ◽

2012 ◽

Author(s):

Kristy Truong ◽

Christopher Gouveia ◽

Jamie Coupar ◽

Tomoko Smyth ◽

John Lyons ◽

...

Keyword(s):

Squamous Cell Carcinoma ◽

Heat Shock ◽

Antitumor Activity ◽

Heat Shock Protein ◽

Cell Carcinoma ◽

Head And Neck ◽

Squamous Cell ◽

Heat Shock Protein 90 ◽

Hsp90 Inhibitor ◽

Neck Squamous Cell Carcinoma

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