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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 Carroll, M. Articles by Druker, B. J. Search for Related Content PubMed PubMed Citation Articles by Carroll, M. Articles by Druker, B. J. Related Collections Neoplasia Social Bookmarking                   What's this?  Previous Article  |  Table of Contents  |  Next Article  CGP 57148, a Tyrosine Kinase Inhibitor, Inhibits the Growth of Cells Expressing BCR-ABL, TEL-ABL, and TEL-PDGFR Fusion Proteins Martin Carroll, Sayuri Ohno-Jones, Shu Tamura, Elisabeth Buchdunger, Jürg Zimmermann, Nicholas B. Lydon, D. Gary Gilliland, and Brian J. Druker From the Division of Hematology and Medical Oncology, Oregon Health Sciences University, Portland, Oregon; Oncology Research Department, Novartis, CH-4002, Basel, Switzerland; and Brigham and Women's Hospital, Harvard Medical School, Boston, MA. CGP 57148 is a compound of the 2-phenylaminopyrimidine class that selectively inhibits the tyrosine kinase activity of the ABL and the platelet-derived growth factor receptor (PDGFR) protein tyrosine kinases. We previously showed that CGP 57148 selectively kills p210BCR-ABL-expressing cells. To extend these observations, we evaluated the ability of CGP 57148 to inhibit other activated ABL tyrosine kinases, including p185BCR-ABL and TEL-ABL. In cell-based assays of ABL tyrosine phosphorylation, inhibition of ABL kinase activity was observed at concentrations similar to that reported for p210BCR-ABL. Consistent with the in vitro profile of this compound, the growth of cells expressing activated ABL protein tyrosine kinases was inhibited in the absence of exogenous growth factor. Growth inhibition was also observed with a p185BCR-ABL-positive acute lymphocytic leukemia (ALL) cell line generated from a Philadelphia chromosome-positive ALL patient. As CGP 57148 inhibits the PDGFR kinase, we also showed that cells expressing an activated PDGFR tyrosine kinase, TEL-PDGFR, are sensitive to this compound. Thus, this compound may be useful for the treatment of a variety of BCR-ABL-positive leukemias and for treatment of the subset of chronic myelomonocytic leukemia patients with a TEL-PDGFR fusion protein. Blood, Vol. 90 No. 12 (December 15), 1997: pp. 4947-4952 © 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: P. M. Hassoun, L. Mouthon, J. A. Barbera, S. 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Fidler Treatment for Malignant Pleural Effusion of Human Lung Adenocarcinoma by Inhibition of Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Phosphorylation Clin. Cancer Res., March 1, 2000; 6(3): 957 - 965. [Abstract] [Full Text] H. Kantarjian, J. V. Melo, S. Tura, S. Giralt, and M. Talpaz Chronic Myelogenous Leukemia: Disease Biology and Current and Future Therapeutic Strategies Hematology, January 1, 2000; 2000(1): 90 - 109. [Abstract] [Full Text] [PDF] R. G. Wickremasinghe and A. V. Hoffbrand Biochemical and Genetic Control of Apoptosis: Relevance to Normal Hematopoiesis and Hematological Malignancies Blood, June 1, 1999; 93(11): 3587 - 3600. [Full Text] [PDF] M. Wetzler, R. K. Dodge, K. Mrozek, A. J. Carroll, R. Tantravahi, A. W. Block, M. J. Pettenati, M. M. L. Beau, S. R. Frankel, C. C. Stewart, et al. Prospective Karyotype Analysis in Adult Acute Lymphoblastic Leukemia: The Cancer and Leukemia Group B Experience Blood, June 1, 1999; 93(11): 3983 - 3993. 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Tonks Protein tyrosine phosphatase PTP1B suppresses p210 bcr-abl-induced transformation of Rat-1 fibroblasts and promotes differentiation of K562 cells PNAS, November 24, 1998; 95(24): 14094 - 14099. [Abstract] [Full Text] [PDF] S. Shangary, K. D. Brown, A. W. Adamson, S. Edmonson, B. Ng, T. K. Pandita, J. Yalowich, G. E. Taccioli, and R. Baskaran Regulation of DNA-dependent Protein Kinase Activity by Ionizing Radiation-activated Abl Kinase Is an ATM-dependent Process J. Biol. Chem., September 22, 2000; 275(39): 30163 - 30168. [Abstract] [Full Text] [PDF] J. Sun, J. Zhao, M. A. Schwartz, J. Y. J. Wang, T. Wiedmer, and P. J. Sims c-Abl Tyrosine Kinase Binds and Phosphorylates Phospholipid Scramblase 1 J. Biol. Chem., July 27, 2001; 276(31): 28984 - 28990. [Abstract] [Full Text] [PDF]

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