Primary and Secondary Kinase Genotypes Correlate With the Biological and Clinical Activity of Sunitinib in Imatinib-Resistant Gastrointestinal Stromal Tumor
作者： Michael C. Heinrich , Robert G. Maki , Christopher L. Corless , Cristina R. Antonescu , Amy Harlow
关键词: Stromal tumor 、 Imatinib 、 PDGFRA 、 Sunitinib 、 Cancer 、 Tyrosine-kinase inhibitor 、 Cancer research 、 Imatinib mesylate 、 GiST 、 Medicine
摘要: Purpose Most gastrointestinal stromal tumors (GISTs) harbor mutant KIT or platelet-derived growth factor receptor α (PDGFRA) kinases, which are imatinib targets. Sunitinib, targets KIT, PDGFRs, and several other has demonstrated efficacy in patients with GIST after they experience failure. We evaluated the impact of primary secondary kinase genotype on sunitinib activity. Patients Methods Tumor responses were assessed radiologically a phase I/II trial 97 metastatic, imatinib-resistant/intolerant GIST. KIT/PDGFRA mutational status was determined for 78 by using tumor specimens obtained before prior therapy. Kinase mutants biochemically profiled sensitivity. Results Clinical benefit (partial response stable disease ≥ 6 months) observed three most common genotypes: exon 9 (58%), 11 (34%), wild-type (56%). Progre...
elsevier.com
cshl.edu
sci-hub.se 参考文章(40)
Nick J. Dibb, Stephen M. Dilworth, Clifford D. Mol, Switching on kinases: oncogenic activation of BRAF and the PDGFR family. Nature Reviews Cancer. ,vol. 4, pp. 718- 727 ,(2004) , 10.1038/NRC1434
Elena Tamborini, M. Stefania Lagonigro, Tiziana Negri, Elisa Gabanti, Silvana Pilotti, Sabrina Pricl, Marco A. Pierotti, KIT/Val654Ala Receptor Detected in One Imatinib-Resistant GIST Patient Cancer Research. ,vol. 65, pp. 1115- 1115 ,(2005)
Elena Tamborini, Lorena Bonadiman, Angela Greco, Veronica Albertini, Tiziana Negri, Alessandro Gronchi, Rossella Bertulli, Maurizio Colecchia, Paolo G. Casali, Marco A. Pierotti, Silvana Pilotti, A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient. Gastroenterology. ,vol. 127, pp. 294- 299 ,(2004) , 10.1053/J.GASTRO.2004.02.021
Maria Debiec-Rychter, Jan Cools, Herlinde Dumez, Raf Sciot, Michel Stul, Nicole Mentens, Hilde Vranckx, Bartosz Wasag, Hans Prenen, Johannes Roesel, Anne Hagemeijer, Allan Van Oosterom, Peter Marynen, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants Gastroenterology. ,vol. 128, pp. 270- 279 ,(2005) , 10.1053/J.GASTRO.2004.11.020
Lesley J. Murray, Tinya J. Abrams, Kelly R. Long, Theresa J. Ngai, Lisa M. Olson, Weiru Hong, Paul K. Keast, Jacqueline A. Brassard, Anne Marie O'Farrell, Julie M. Cherrington, Nancy K. Pryer, SU11248 inhibits tumor growth and CSF-1R-dependent osteolysis in an experimental breast cancer bone metastasis model. Clinical & Experimental Metastasis. ,vol. 20, pp. 757- 766 ,(2003) , 10.1023/B:CLIN.0000006873.65590.68
David J. Kwiatkowski, Rhebbing up mTOR: new insights on TSC1 and TSC2, and the pathogenesis of tuberous sclerosis. Cancer Biology & Therapy. ,vol. 2, pp. 471- 476 ,(2003) , 10.4161/CBT.2.5.446
Hans Prenen, Jan Cools, Nicole Mentens, Cedric Folens, Raf Sciot, Patrick Schöffski, Allan Van Oosterom, Peter Marynen, Maria Debiec-Rychter, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate. Clinical Cancer Research. ,vol. 12, pp. 2622- 2627 ,(2006) , 10.1158/1078-0432.CCR-05-2275
Satoru Yuzawa, Yarden Opatowsky, Zhongtao Zhang, Valsan Mandiyan, Irit Lax, Joseph Schlessinger, Structural Basis for Activation of the Receptor Tyrosine Kinase KIT by Stem Cell Factor Cell. ,vol. 130, pp. 323- 334 ,(2007) , 10.1016/J.CELL.2007.05.055
Christopher D.M. Fletcher, Heikki Joensuu, George D. Demetri, Margaret von Mehren, Charles D. Blanke, Annick D. Van den Abbeele, Burton Eisenberg, Peter J. Roberts, Michael C. Heinrich, David A. Tuveson, Samuel Singer, Milos Janicek, Jonathan A. Fletcher, Stuart G. Silverman, Sandra L. Silberman, Renaud Capdeville, Beate Kiese, Bin Peng, Sasa Dimitrijevic, Brian J. Druker, Christopher Corless, Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. The New England Journal of Medicine. ,vol. 347, pp. 472- 480 ,(2002) , 10.1056/NEJMOA020461
Dong Wook Kim, Young Suk Jo, Hye Sook Jung, Hyo Kyun Chung, Jung Hun Song, Ki Cheol Park, Su Hyeon Park, Jung Hwan Hwang, So Young Rha, Gi Ryang Kweon, Su-Jae Lee, Ki-Won Jo, Minho Shong, An orally administered multitarget tyrosine kinase inhibitor, SU11248, is a novel potent inhibitor of thyroid oncogenic RET/papillary thyroid cancer kinases. The Journal of Clinical Endocrinology and Metabolism. ,vol. 91, pp. 4070- 4076 ,(2006) , 10.1210/JC.2005-2845