A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient

Gastroenterology

Volumn 127, Issue 1, 2004, Pages 294-299

  Tamborini, Elena ^a   Bonadiman, Lorena ^a   Greco, Angela ^b   Albertini, Veronica ^a   Negri, Tiziana ^a   Gronchi, Alessandro ^b   Bertulli, Rossella ^b   Colecchia, Maurizio ^a   Casali, Paolo G ^b   Pierotti, Marco A ^b,c   Pilotti, Silvana ^a,d  

^a U of Exp Molecular Pathology   (Italy)

^b Institute of Molecular Oncology ^*  (Italy)

^c FIRC INSTITUTE OF MOLECULAR ONCOLOGY   (Italy)

^d NATIONAL CANCER INSTITUTE   (Italy)

Author keywords

chronic myelogenous leukemia; CML; gastrointestinal stromal tumors; GIST; PDGFR; platelet derived growth factor receptor

Indexed keywords

ADENOSINE TRIPHOSPHATE; AMINO ACID; COMPLEMENTARY DNA; EPIRUBICIN; GENOMIC DNA; IFOSFAMIDE; IMATINIB; PROTEIN TYROSINE KINASE INHIBITOR; RECEPTOR PROTEIN; STEM CELL FACTOR;

AGED; ARTICLE; CANCER SURGERY; CASE REPORT; CLINICAL TRIAL; DISEASE COURSE; DNA DETERMINATION; DNA SEQUENCE; DRUG SENSITIVITY; EXON; FATIGUE; GASTROINTESTINAL TOXICITY; GASTROINTESTINAL TUMOR; GENE MUTATION; GENETIC TRANSFECTION; HUMAN; IMMUNOPRECIPITATION; MALE; MUTAGENESIS; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; WESTERN BLOTTING;

EID: 20844448396     PISSN: 00165085     EISSN: None     Source Type: Journal    
DOI: 10.1053/j.gastro.2004.02.021     Document Type: Article

References (23)

1. Tuveson D.A., Willis N.A., Jacks T., Griffin J.D., Singer S., Fletcher C.D., Fletcher J.A., Demetri G.D. STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein biological and clinical implications. Oncogene. 20:2001;5054-5058
2. Mauro M.J., O'Dwyer M., Heinrich M.C., Druker B.J. STI571 a paradigm of new agents for cancer therapeutics. J Clin Pathol. 20:2002;325-334
3. Heinrich M.C., Corless C.L., Duensing A., McGreevey L., Chen C.J., Joseph N., Singer S., Griffith D.J., Haley A., Town A., Demetri G.D., Fletcher C.D., Fletcher J.A. PDGFRA activating mutation in gastrointestinal stromal tumors. Science. 299:2003;708-710
4. Demetri G.D., von Mehren M., Blanke C.D., Van den Abbeele A.D., Eisenberg B., Roberts P.J., Heinrich M.C., Tuveson D.A., Singer S., Janicek M., Fletcher J.A., Silverman S.G., Silberman S.L., Capdeville R., Kiese B., Peng B., Dimitrijevic S., Druker B.J., Corless C., Fletcher C.D., Joensuu H. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med. 347:2002;472-480
5. Rubin B.P., Schuetze S.M., Eary J.F., Norwood T.H., Mirza S., Conrad E.U., Bruckner J.D. Molecular targeting of platelet-derived growth factor B by imatinib mesylate in a patient with metastatic dermatofibrosarcoma protuberans. J Clin Oncol. 20:2002;3586-3591
6. Maki R.G., Awan R.A., Dixon R.H., Jhanwar S., Antonescu C.R. Differential sensitivity to Imatinib of 2 patients with metastatic sarcoma arising from dermatofibrosarcoma protuberans. Int J Cancer. 100:2002;623-626
7. La Rosee P., O'Dwyer M.E., Druker B.J. Insights from pre-clinical studies for new combination treatment regimens with Bcr-Abl kinase inhibitor imatinib mesylate (Gleevec/Glivec) in chronic myelogenous leukaemia a translational perspective. Leukemia. 16:2002;1213-1219
8. Azam M., Latek R.R., Daley G.Q. Mechanisms of autoinhibition and STI571/Imatinib resistance revealed by mutagenesis of BCR-ABL. Cell. 112:2003;831-843
9. Joensuu H., Fletcher C., Dimitrijevic S., Silberman S., Roberts P., Demetri G. Management of malignant gastrointestinal stromal tumours. Lancet Oncol. 3:2002;655-664
10. Heinrich M.C., Blanke C.D., Druker B.J., Corless C.L. Inhibition of KIT tyrosine kinase activity a novel molecular approach to the treatment of KIT-positive malignancies. J Clin Oncol. 20:2002;1692-1703
11. Heinrich M.C., Corless C.L., Blanke C.D., Demetri G.D., Joensuu H., von Mehren M., McGreevey C.L., Wait C.L., Griffith D., Chen C.J., Haley A., Kiese B., Druker B., Roberts P., Eisenberg B., Singer S., Silberman S., Dimitrijevic S., Fletcher C.D.M, Fletcher J.A. KIT mutational status predicts clinical response to STI571 in patients with metastatic gastrointestinal stromal tumors (GISTs) (abstr). Proc Am Soc Clin Oncol. 21:2002;2a. Abstract 6
12. Fletcher J.A., Corless C.L., Dimitrijevic S., von Mehren M., Eisenberg B., Joensuu H., Fletcher C.D.M, Blanke C., Demetri G.D., Heinrich M.C. Mechanisms of resistance to imatinib-mesilate (IM) in advanced gastrointestinal stromal tumor (GIST) (abstr). Proc Am Soc Clin Oncol. 22:2003;. Abstract 3275
13. Verweij J., Casali P.G., Zalcberg J., Le Cesne A., Reichard P., Blay J.-.Y, Issels R.D., Van Glabbeke M., Donato Di Paola E., Judson I.R. Early efficacy comparison of two doses of imatinib for the treatment of advanced gastro-intestinal stromal tumors (GIST) interim results of a randomized phase III trial from the EORTC-STBSG, ISG and AGITG (abstr). Proc Am Soc Clin Oncol. 22:2003;. Abstract 3272
14. Casali P.G., Verweij J., Zalcberg J., LeCesne A., Reichardt P., RayCoquard I., Wendtner C., Judson I., Donato Di Paola E., Van Glabbeke M., Bertulli R., Dhillon H., Nielsen O.S. Imatinib (Glivec) 400 vs. 800 mg daily in patients with gastrointestinal stromal tumors (GIST): a randomized phase III trial from the EORTC Soft Tissue and Bone Sarcoma Group, the Italian Sarcoma Group (ISG), and the Australasian Gastro-Intestinal Trial Group (AGITG). A toxicity report. Am Soc Clin Oncol Proc. 21:2002;413a. (abstr)
15. Miettinen M., Lasota J. Gastrointestinal stromal tumors-definition, clinical, histological, immunohistochemical, and molecular genetic features and differential diagnosis. Virchows Arch. 438:2001;1-12
16. Hornick J.L., Fletcher C.D.M. Immunohistochemical staining for KIT (CD117) in soft tissues sarcomas is very limited in distribution. Am J Clin Pathol. 117:2002;188-193
17. Rubin B.P., Singer S., Tsao C., Duensing A., Lux M.L., Ruiz R., Hibbard M.K., Chen C.J., Xiao S., Tuveson D.A., Demetri G.D., Fletcher C.D., Fletcher J.A. KIT activation is a ubiquitous feature of gastrointestinal stromal tumors. Cancer Res. 61:2001;8118-8121
18. Tamborini E., Papini D., Mezzelani A., Riva C., Azzarelli A., Sozzi G., Pierotti M.A., Pilotti S. c-KIT and c-KIT ligand (SCF) in synovial sarcoma (SS) an mRNA expression analysis in 23 cases. Br J Cancer. 85:2001;405-411
19. Greco A., Villa R., Fusetti L., Orlandi R., Pierotti M.A. The Gly571Arg mutation, associated with the autonomic and sensory disorder congenital insensitivity to pain with anhidrosis, causes the inactivation of the NTRK1/nerve growth factor receptor. J Cell Physiol. 182:2000;127-133
20. Hanks S.K., Quinn A.M., Hunter T. The protein kinase family conserved features and deduced phylogeny of the catalytic domains. Science. 241:1988;42-52
21. Bohmer F.D., Karagyozov L., Uecker A., Serve H., Botzki A., Mahboobi S., Dove S. A single amino acid exchange inverts susceptibility of related receptor tyrosine kinases for the ATP site inhibitor STI-571. J Biol Chem. 278:2003;5148-5155
22. Corbin A.S., Buchdunger E., Pascal F., Druker B.J. Analysis of the structural basis of specificity of inhibition of the ABL kinase by STI571. J Biol Chem. 277:2002;32214-32219
23. Cools J., DeAngelo D.J., Gotlib J., Stover E.H., Legare R.D., Cortes J., Kutok J., Clark J., Galinsky I., Griffin J.D., Cross N.C., Tefferi A., Malone J., Alam R., Schrier S.L., Schmid J., Rose M., Vandenberghe P., Verhoef G., Boogaerts M., Wlodarska I., Kantarjian H., Marynen P., Coutre S.E., Stone R., Gilliland D.G. A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as therapeutic target of imatinib in idiopathic hypereosinophilic syndrome. N Engl J Med. 348:2003;1201-1214