Old and New Approaches to Target the Hsp90 Chaperone

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Menezes D.L.; Taverna P.; Jensen M.R.; Abrams T.; Stuart D.; Yu G.K.; Duhl D.; Machajewski T.; Sellers W.R.; Pryer N.K.; Gao Z.; The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. Mol Cancer Ther 2012,11(3),730-739

Ohkubo S.; Kodama Y.; Muraoka H.; Hitotsumachi H.; Yoshimura C.; Kitade M.; Hashimoto A.; Ito K.; Gomori A.; Takahashi K.; Shibata Y.; Kanoh A.; Yonekura K.; TAS-116, a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol Cancer Ther 2015,14(1),14-22

Shimomura A.; Yamamoto N.; Kondo S.; Fujiwara Y.; Suzuki S.; Yanagitani N.; Horiike A.; Kitazono S.; Ohyanagi F.; Doi T.; Kuboki Y.; Kawazoe A.; Shitara K.; Ohno I.; Banerji U.; Sundar R.; Ohkubo S.; Calleja E.M.; Nishio M.; First-in-human phase I study of an oral HSP90 inhibitor, TAS-116, in patients with advanced solid tumors. Mol Cancer Ther 2019,18(3),531-540

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