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Drug Discov Today. 2011 Apr;16(7-8):325-31. doi: 10.1016/j.drudis.2011.02.008. Epub 2011 Feb 17.

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

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  • 1Cancer Institute of New Jersey, Department of Pharmacology, UMDNJ-Robert Wood Johnson Medical School, Piscataway, NJ 08854, USA.

Abstract

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.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21333749
[PubMed - indexed for MEDLINE]
PMCID:
PMC3073023
Free PMC Article
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