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Prepublished online as a Blood First Edition Paper on August 14, 2003; DOI 10.1182/blood-2003-02-0633. This Article Full Text (PDF) All Versions of this Article: 2003-02-0633v1 102/12/3880    most recent Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Rights and Permissions Citing Articles Citing Articles via HighWire Citing Articles via CrossRef Citing Articles via Google Scholar Google Scholar Articles by Lancet, J. E Articles by Karp, J. E Search for Related Content PubMed PubMed Citation Articles by Lancet, J. E Articles by Karp, J. E Social Bookmarking                   What's this? Submitted February 27, 2003 Accepted June 24, 2003 Farnesyltransferase inhibitors in hematologic malignancies: new horizons in therapy Jeffrey E Lancet* and Judith E Karp James P. Wilmot Cancer Center, University of Rochester, Rochester, NY, USA The Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD, USA * Corresponding author; email: jeffrey_lancet{at}urmc.rochester.edu. Farnesyltransferase inhibitors (FTIs) are small-molecule inhibitors that selectively inhibit farnesylation of a number of intracellular substrate proteins such as Ras. Preclinical work has revealed their ability to effectively inhibit tumor growth across a wide range of malignant phenotypes. Many hematologic malignancies appear to be reasonable disease targets, in that they express relevant biologic targets, such as Ras, Mitogen-Activated Protein Kinase (MAPK), AKT, and others that may depend upon farnesyl protein transferase (FTase) activity to promote proliferation and survival. A host of phase I trials has been recently launched to assess the applicability of FTIs in hematologic malignancies, many of which demonstrate effective enzyme target inhibition, low toxicity, and some clinical responses. As a result, phase II trials have been initiated in a variety of hematologic malignancies and disease settings, in order to further validate clinical activity and to identify downstream signal transduction targets that may be modified by these agents. It is anticipated that these studies will serve to define the optimal roles of FTIs in patients with hematologic malignancies and provide insight into effective methods by which to combine FTIs with other agents. CiteULike    Connotea    Del.icio.us    Digg    Reddit    Technorati    What's this? This article has been cited by other articles: J. E. Karp, B. D. Smith, I. Gojo, J. E. Lancet, J. Greer, M. Klein, L. Morris, M. J. Levis, S. D. Gore, J. J. Wright, et al. 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