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This Article Full Text Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Citation Map 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 Deininger, M. W.N. Articles by Melo, J. V. Search for Related Content PubMed PubMed Citation Articles by Deininger, M. W.N. Articles by Melo, J. V. Related Collections Neoplasia Social Bookmarking                   What's this?  Previous Article  |  Table of Contents  |  Next Article  The Tyrosine Kinase Inhibitor CGP57148B Selectively Inhibits the Growth of BCR-ABL-Positive Cells Michael W.N. Deininger, John M. Goldman, Nicholas Lydon, and Junia V. Melo From the Leukaemia Research Fund Centre for Adult Leukaemia, Department of Haematology, Royal Postgraduate Medical School, London, UK; and Novartis, Basel, Switzerland. The Philadelphia chromosome found in virtually all cases of chronic myeloid leukemia (CML) and in about one third of the cases of adult acute lymphoblastic leukemia is formed by a reciprocal translocation between chromosomes 9 and 22 that results in the fusion of BCR and ABL genetic sequences. This BCR-ABL hybrid gene codes for a fusion protein with deregulated tyrosine kinase activity that can apparently cause malignant transformation. CGP57148B, a 2-phenylaminopyrimidine derivative, has been shown to selectively inhibit the tyrosine kinase of ABL and BCR-ABL. We report here that this compound selectively suppresses the growth of colony-forming unit-granulocyte/macrophage (CFU-GM) and burst-forming unit-erythroid derived from CML over a 2-logarithmic dose range with a maximal differential effect at 1.0 µmol/L. However, almost all CML colonies that grow in the presence of 1.0 µmol/L CGP57148B are BCR-ABL-positive, which may reflect the fact that residual normal clonogenic myeloid precursors are infrequent in most patients with CML. We also studied the effects of CGP57148B on hematopoietic cell lines. Proliferation was suppressed in most of the BCR-ABL-positive lines; all five BCR-ABL-negative lines were unaffected. We conclude that this new agent may have significant therapeutic applications. Blood, Vol. 90 No. 9 (November 1), 1997: pp. 3691-3698 © 1997 by The American Society of Hematology. CiteULike    Connotea    Del.icio.us    Digg    Reddit    Technorati    What's this? This article has been cited by other articles: H. Yuan, Z. Wang, C. Gao, W. Chen, Q. Huang, J.-K. Yee, R. Bhatia, and W. Chen BCR-ABL Gene Expression Is Required for Its Mutations in a Novel KCL-22 Cell Culture Model for Acquired Resistance of Chronic Myelogenous Leukemia J. Biol. 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Ramadevi, E. Winton, S. Wittmann, and K. N. Bhalla CGP57148B (STI-571) induces differentiation and apoptosis and sensitizes Bcr-Abl-positive human leukemia cells to apoptosis due to antileukemic drugs Blood, September 15, 2000; 96(6): 2246 - 2253. [Abstract] [Full Text] [PDF] N. J. Donato and M. Talpaz Clinical Use of Tyrosine Kinase Inhibitors: Therapy for Chronic Myelogenous Leukemia and Other Cancers Clin. Cancer Res., August 1, 2000; 6(8): 2965 - 2966. [Full Text] G. W. Krystal, S. Honsawek, J. Litz, and E. Buchdunger The Selective Tyrosine Kinase Inhibitor STI571 Inhibits Small Cell Lung Cancer Growth Clin. Cancer Res., August 1, 2000; 6(8): 3319 - 3326. [Abstract] [Full Text] F. X. Mahon, M. W. N. Deininger, B. Schultheis, J. Chabrol, J. Reiffers, J. M. Goldman, and J. V. 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