Rational drug redesign to overcome drug resistance in cancer therapy: Imatinib moving target

Cancer Research

Volumn 67, Issue 9, 2007, Pages 4028-4033

  Fernández, Ariel ^a,b,c   Sanguino, Angela ^c   Peng, Zhenghong ^c   Crespo, Alejandro ^a   Ozturk, Eylem ^c,d   Zhang, Xi ^b   Wang, Shimei ^c   Bornmann, William ^c   Lopez Berestein, Gabriel ^c  

^a Rice University   (United States)

^b RICE UNIVERSITY   (United States)

^c UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

^d HACETTEPE UNIVERSITY   (Turkey)

Author keywords

[No Author keywords available]

Indexed keywords

IMATINIB; PHOSPHOTRANSFERASE; STEM CELL FACTOR;

ARTICLE; CANCER; CANCER CHEMOTHERAPY; CANCER RESISTANCE; CELL PROLIFERATION; DRUG DESIGN; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; HUMAN; HUMAN CELL; MOLECULAR DYNAMICS; MUTATION; PRIORITY JOURNAL;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG DESIGN; DRUG RESISTANCE, NEOPLASM; GASTROINTESTINAL STROMAL TUMORS; HUMANS; KINETICS; MODELS, MOLECULAR; MUTATION; PHOSPHORYLATION; PIPERAZINES; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-KIT; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 34249290776     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-07-0345     Document Type: Article

References (20)

1. Druker BJ. Circumventing resistance to kinase-inhibitor therapy. N Engl J Med 2006;354:2594-6.
2. Schittenhelm MM, Shiraga S, Schroeder A, et al. Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res 2006;66:473-81.
3. D816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood 2006;108:286-91.
4. Attoub S, Rivat C, Rodrigues S, et al. The c-kit tyrosine kinase inhibitor STI571 for colorectal cancer therapy. Cancer Res 2002;62:4879-83.
5. Mol CD, Dougan DR, Schneider TR, et al. Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase. J Biol Chem 2004;279:31655-63.
6. Furitsu T, Tsujimura T, Tono T, et al. Identification of mutations in the coding sequence of the proto-oncogene c-kit in a human mast cell leukemia cell line causing ligand-independent activation of c-kit product. J Clin Invest 1993;92:1736-44.
7. Nagata H, Worobec AS, Oh CH, et al. Identification of a point mutation in the catalytic domain of the proto-oncogene c-kit in peripheral blood mononuclear cells of patients who have mastocytosis with an associated hematologic disorder. Proc Natl Acad Sci U S A 1995;92:10560-4.
8. Cheng Y, Rossky PJ. Surface topography dependence of biomolecular hydrophobic hydration. Nature 1998;392:696-9.
9. Fabian MA, Biggs WH, Treiber DK, et al. A small molecule kinase interaction map for clinical kinase inhibitors. Nat Biotechnol 2005;23:329-36.
10. Fernández A. Keeping dry and crossing membranes. Nat Biotechnol 2004;22:1081-4.
11. Wang J, Morin P, Wang W, Kollman PA. Use of MM-PBSA in reproducing the binding free energies to HIV-1 RT of TIBO derivatives and predicting the binding mode to HIV-1 RT of Efavirenz by docking and MM-PBSA. J Am Chem Soc 2001;123:5221-30.
12. Andricioaei I, Karplus MJ. On the calculation of entropy from covariance matrices of the atomic fluctuations. Chem Phys 2001;115:6289-92.
13. Li JJ, Johnson DS, Sliskovic DR, Roth BD. Contemporary drug synthesis. New Jersey: Wiley-Interscience; 2004. p. 32-3.
14. Schindler T, Bornmann W, Pellicena P, et al. Structural mechanism for STI-571 inhibition of Abelson tyrosine kinase. Science 2000;289:1938-42.
15. DeMatteo RP. The GIST of targeted cancer therapy: a tumor (gastrointestinal stromal tumor), a mutated gene (c-kit), and a molecular inhibitor (STI571). Ann Surg Oncol 2002;9:831-9.
16. Corbin AS, Griswold IJ, La Rosee P, et al. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood 2004;104:3754-7.
17. La Rosee P, Corbin AS, Stoffregen EP, Deininger MW, Druker BJ. Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). Cancer Res 2002;62:7149-53.
18. Butterfield JH, Weiler D, Dewald G, Gleich GJ. Establishment of an immature mast cell line from a patient with mast cell leukemia. Leuk Res 1988;12:345-55.
19. Ongusaha PP, Kim JI, Fang L, et al. p53 induction and activation of DDR1 kinase counteract p53-mediated apoptosis and influence p53 regulation through a positive feedback. EMBO J 2003;22:1289-301.
20. Timokhina I, Kissel H, Stella G, Besmer P. Kit signaling through PI 3-kinase and Src kinase pathways: an essential role for Rac1 and JNK activation in mast cell proliferation. EMBO J 1998;17:6250-62.