Cellular targets of gefitinib

Cancer Research

Volumn 65, Issue 2, 2005, Pages 379-382

  Brehmer, Dirk ^a   Greff, Zoltán ^a   Godl, Klaus ^a   Blencke, Stephanie ^a   Kurtenbach, Alexander ^a   Weber, Martina ^a   Müller, Stefan ^a   Klebl, Bert ^a   Cotten, Matt ^a   Kéri, György ^a   Wissing, Josef ^a   Daub, Henrik ^a,b  

^a SEMMELWEIS UNIVERSITY   (Hungary)

^b Axxima Pharmaceuticals AG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

CELL PROTEIN; CYCLIN DEPENDENT KINASE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; GEFITINIB; MITOGEN ACTIVATED PROTEIN KINASE P38; PROTEIN KINASE (CALCIUM,CALMODULIN) II; PROTEIN SERINE THREONINE KINASE; PROTEIN TYROSINE KINASE; STRESS ACTIVATED PROTEIN KINASE;

AFFINITY CHROMATOGRAPHY; ANIMAL CELL; ARTICLE; CANCER; CANCER CHEMOTHERAPY; DRUG SELECTIVITY; DRUG TARGETING; ENZYME INHIBITION; HELA CELL; HUMAN; HUMAN CELL; IN VITRO STUDY; MASS SPECTROMETRY; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEOMICS; TARGET CELL; UTERINE CERVIX CARCINOMA;

ANIMALS; ANTINEOPLASTIC AGENTS; CERCOPITHECUS AETHIOPS; COS CELLS; HELA CELLS; HUMANS; PROTEIN KINASE INHIBITORS; PROTEOMICS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 19944432043     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (20)

1. Dancey J, Sausville EA. Issues and progress with protein kinase inhibitors for cancer treatment. Nat Rev Drug Discov 2003;1:296-313.
2. Cohen MH, Williams GA, Sridhara R, et al. United States Food and Drug Administration Drug approval summary: gefitinib (ZD1839; Iressa) tablets. Clin Cancer Res 2004;10:1212-8.
3. Lynch TJ, Bell DW, Sordella R, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004;350:2129-39.
4. Paez JG, Janne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304:1497-500.
5. Godl K, Wissing J, Kurtenbach A, et al. An efficient proteomics method to identify the cellular targets of protein kinase inhibitors. Proc Natl Acad Sci U S A 2003;100:15434-9.
6. Daub H, Godl K, Brehmer D, Klebl B, Müller G. Evaluation of kinase inhibitor selectivity by chemical proteomics. Assay Drug Dev Technol 2004;2:215-24.
7. Barker AJ, Gibson KH, Grundy W, et al. Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer. Bioorg Med Chem Lett 2001;11:1911-4.
8. Wissing J, Godl K, Brehmer D, et al. Chemical proteomic analysis reveals alternative modes of action for pyrido[2,3-d]pyrimidine kinase inhibitors. Mol Cell Proteomics 2004. Epub ahead of print.
9. Blencke S, Ullrich A, Daub, H. Mutation of threonine 766 in the epidermal growth factor receptor reveals a hotspot for resistance formation against selective tyrosine kinase inhibitors. J Biol Chem 2003;278:15435-40.
10. Mitchell PJ, Barker KT, Martindale JE, et al. Cloning and characterisation of cDNAs encoding a novel non-receptor tyrosine kinase, brk, expressed in human breast tumours. Oncogene 1994;9:2383-90.
11. Daub H, Blencke S, Habenberger P, et al. Identification of SRPK1 and SRPK2 as the major cellular protein kinases phosphorylating hepatitis B virus core protein. J Virol 2002;76:8124-37.
12. Blencke S, Zech B, Engkvist O, et al. Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors. Chem Biol 2004;11:691-701.
13. Peters RT, Liao, SM, Maniatis T. IKKε is part of a novel PMA-inducible IκB kinase complex. Mol Cell 2000;5:513-22.
14. Stamos J, Sliwkowski MX, Eigenbrot C. Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J Biol Chem 2002;277:46265-72.
15. Wood ER, Truesdale AT, McDonald OB, et al. A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res 2004;64:6652-9.
16. Kobayashi K, Inohara N, Hernandez LD, et al. RICK/Rip2/CARDIAK mediates signalling for receptors of the innate and adaptive immune systems. Nature 2002;416:194-9.
17. Kamalati T, Jolin HE, Mitchell PJ, et al. Brk, a breast tumor-derived non-receptor protein-tyrosine kinase, sensitizes mammary epithelial cells to epidermal growth factor. J Biol Chem 1996;271:30956-63.
18. Llor X, Serfas MS, Bie W, et al. BRK/Sik expression in the gastrointestinal tract and in colon tumors. Clin Cancer Res 1999;5:1767-77.
19. Zhang L, Gjoerup O, Roberts TM. The serine/threonine kinase cyclin G-associated kinase regulates epidermal growth factor receptor signaling. Proc Natl Acad Sci U S A 2004;101:10296-301.
20. Li B, Chang CM, Yuan M, McKenna WG, Shu HK. Resistance to small molecule inhibitors of epidermal growth factor receptor in malignant gliomas. Cancer Res 2003;63:7443-50.