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

Yan Jie Zhang, Yanwen Duan, X. F.Steven Zheng

Research output: Contribution to journalReview articlepeer-review

145 Scopus citations


The mTOR signaling pathway is dysregulated in ∼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. This review will detail the potential therapeutic value and issues of these novel antineoplastic agents, with emphasis placed on those that have already entered clinical trials.

Original languageEnglish (US)
Pages (from-to)325-331
Number of pages7
JournalDrug Discovery Today
Issue number7-8
StatePublished - Apr 2011

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery

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