Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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Yan-Jie Zhang, Yanwen Duan and X.F. Steven Zheng discuss the potential therapeutic value and issues of novel antineoplastic agents, with emphasis placed on those that have already entered clinical trials.

The mTOR signaling pathway is dysregulated in approximately 50% of all human malignancies and is a major cancer drug target. Although rapamycin analogs (rapalogs) have shown clinical efficacy in a subset of cancers, they do not fully exploit the antitumor potential of mTOR targeting. Because the mTOR kinase domain is important for rapamycin-sensitive and -insensitive functions, mTOR catalytic inhibitors have been developed recently as the second generation of anti-mTOR agents. Importantly, they have shown marked improvement of antitumor activity in vivo and in vitro.

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