Characterization and development of a peptide substrate-based phosphate transfer assay for the human vascular endothelial growth factor receptor-2 tyrosine kinase

Analytical Biochemistry

Volumn 360, Issue 2, 2007, Pages 196-206

  Zhao, Genshi ^a   Peery, Robert B ^a   Yingling, Jonathan M ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Angiogenesis; Autophosphorylation; Kdr; Kinase domain; Phosphorylation assay; Receptor tyrosine kinase; VEGF

Indexed keywords

AMINO ACIDS; CELL ENGINEERING; CELL PROLIFERATION; CELL SIGNALING; ENDOTHELIAL CELLS; METAL IONS; METALS; PEPTIDES; PURIFICATION; SUBSTRATES; TUMORS;

ANGIOGENESIS; AUTOPHOSPHORYLATION; KINASE DOMAINS; RECEPTOR TYROSINE KINASE; VEGF;

ENZYME ACTIVITY;

ADENOSINE TRIPHOSPHATE; MAGNESIUM ION; MANGANESE; METAL ION; PEPTIDE; PHOSPHATE; PHOSPHOTRANSFERASE; PROTEIN TYROSINE KINASE; VASCULOTROPIN RECEPTOR 2;

AMINO ACID SEQUENCE; ANGIOGENESIS; ARTICLE; ASSAY; AUTOPHOSPHORYLATION; CELL SURFACE; ENDOTHELIUM CELL; ENZYME ACTIVITY; ENZYME SUBSTRATE; HIGH THROUGHPUT SCREENING; PEPTIDE SYNTHESIS; PHOSPHATE TRANSPORT; PRIORITY JOURNAL; RECEPTOR BINDING; SIGNAL TRANSDUCTION; SOLID TUMOR; VALIDATION PROCESS;

EID: 33845631253     PISSN: 00032697     EISSN: 10960309     Source Type: Journal    
DOI: 10.1016/j.ab.2006.10.038     Document Type: Article

References (34)

1. Jakeman L.B., Winer J., Bennett G.L., Altar C.A., and Ferrara N. Binding sites for vascular endothelial growth factor are localized on endothelial cells in adult rat tissues. J. Clin. Invest. 89 (1992) 244-253
2. Taichman N.S., Young S., Cruchley A.T., Taylor P., and Paleolog E. Human neutrophils secrete vascular endothelial growth factor. J. Leukoc. Biol. 62 (1997) 397-400
3. Horiuchi T., and Weller P.F. Expression of vascular endothelial growth factor by human eosinophils: up-regulation by granulocyte macrophage colony-stimulating factor and interleukin-5. Am. J. Respir. Cell Mol. Biol. 17 (1997) 70-77
4. Amano S., Rohan R., Kuroki M., Tolentino M., and Adamis A.P. Requirement for vascular endothelial growth factor in wound- and inflammation-related corneal neovascularization. Invest. Ophthalmol. Vis. Sci. 39 (1998) 18-22
5. Griga T., Tromm A., Spranger J., and May B. Increased serum levels of vascular endothelial growth factor in patients with inflammatory bowel disease. Scand. J. Gastroenterol. 33 (1998) 504-508
6. Fava R.A., Olsen N.J., Spencer G.G., Yeo K.T., Yeo T.K., Berse B., Jackman R.W., Senger D.R., Dvorak H.F., and Brown L.F. Vascular permeability factor/endothelial growth factor (VPF/VEGF): accumulation and expression in human synovial fluids and rheumatoid synovial tissue. J. Exp. Med. 180 (1994) 341-346
7. Nagashima M., Yoshino S., Ishiwata T., and Asano G. Role of vascular endothelial growth factor in angiogenesis of rheumatoid arthritis. J. Rheumatol. 22 (1995) 1624-1630
8. Paleolog E. Target effector role of vascular endothelium in the inflammatory response: insights from the clinical trial of anti-TNFα antibody in rheumatoid arthritis. Mol. Pathol. 50 (1997) 225-233
9. Koch A.E. Angiogenesis: implications for rheumatoid arthritis. Arthritis Rheum. 41 (1998) 951-962
10. Plate K.H., Breier G., Millauer B., Ullrich A., and Risau W. Up-regulation of vascular endothelial growth factor and its cognate receptors in a rat glioma model of tumor angiogenesis. Cancer Res. 53 (1993) 5822-5827
11. Folkman J. Angiogenesis in cancer, vascular, rheumatoid, and other disease. Nat. Med. 1 (1995) 27-31
12. Brown L.F., Berse B., Jackman R.W., Tognazzi K., Manseau E.J., Senger D.R., and Dvorak H.F. Expression of vascular permeability factor (vascular endothelial growth factor) and its receptors in adenocarcinomas of the gastrointestinal tract. Cancer Res. 53 (1993) 4727-4735
13. Brown L.F., Berse B., Jackman R.W., Tognazzi K., Manseau E.J., Dvorak H.F., and Senger D.R. Increased expression of vascular permeability factor (vascular endothelial growth factor) and its receptors in kidney and bladder carcinomas. Am. J. Pathol. 143 (1993) 1255-1262
14. Thomas K.A. Vascular endothelial growth factor, a potent and selective angiogenic agent. J. Biol. Chem. 271 (1996) 603-606
15. Ferrara N., Gerber H.P., and LeCouter J. The biology of VEGF and its receptors. Nat. Med. 9 (2003) 669-676
16. Yancopoulos G.D., Davis S., Gale N.W., Rudge J.S., Wiegand S.J., and Holash J. Vascular-specific growth factors and blood vessel formation. Nature 407 (2000) 242-248
17. Zachary I. VEGF signaling: integration and multi-tasking in endothelial cell biology. Biochem. Soc. Trans. 31 (2003) 1171-1177
18. Sakurai Y., Ohgimoto K., Kataoka Y., Yoshida N., and Shibuya M. Essential role of Flk-1 (VEGF receptor 2) tyrosine residue 1173 in vasculogenesis in mice. Proc. Natl. Acad. Sci. USA 102 (2005) 1076-1081
19. Gerber H.P. Anti-angiogenesis: biology is the foundation for therapy. Drug Discov. Today 8 (2003) 344-346
20. Wood J.M., Bold G., Buchdunger E., Cozens R., Ferrari S., Frei J., Hofmann F., Mestan J., Mett H., O'Reilly T., Persohn E., Rösel J., Schnell C., Stover D., Theuer A., Towbin H., Wenger F., Woods-Cook K., Menrad A., Siemeister G., Schirner M., Thierauch K.-H., Schneider M.R., Drevs J., Martiny-Baron G., Totzke F., and Marmé D. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 60 (2000) 2178-2189
21. Mendel D.B., Laird A.D., Xin X., Louie S.G., Christensen J.G., Li G., Schreck R.E., Abrams T.J., Ngai T.J., Lee L.B., Murray L.J., Carver J., Chan E., Moss K.G., Haznedar J.O., Sukbuntherng J., Blake R.A., Sun L., Tang C., Miller T., Shirazian S., McMahon G., and Cherrington J.M. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin. Cancer Res. 9 (2003) 327-337
22. Wedge S.R., Ogilvie D.J., Dukes M., Kendrew J., Chester R., Jackson J.A., Boffey S.J., Valentine P.J., Curwen J.O., Musgrove H.L., Graham G.A., Hughes G.D., Thomas A.P., Stokes E.S.E., Curry B., Richmond G.H.P., Wadsworth P.F., Bigley A.L., and Hennequin L.F. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res. 62 (2002) 4645-4655
23. Sepp-Lorenzino L., Rands E., Ma X., Connolly B., Shipman J., Antanavage J., Hill S., Davis L., Beck S., Rickert K., Coll K., Ciecko P., Fraley M., Hoffman W., Hartman G., Heimbrook D., Gibbs J., Kohl N., and Thomas K. A novel orally bioavailable inhibitor of kinase insert domain-containing receptor induces antiangiogenic effects and prevents tumor growth in vivo. Cancer Res. 64 (2004) 751-756
24. Clark J.W., Eder J.P., Ryan D., Lathia C., and Lenz H.-J. Safety and pharmacokinetics of the dual action Raf kinase and vascular endothelial growth factor receptor inhibitor, Bay43-9006, in patients with advanced, refractory solid tumors. Clin. Cancer Res. 11 (2005) 5472-5480
25. Traxler P., Bold G., Buchdunger E., Caravatti G., Furet P., Manley P., O'Reilly T., Wood J., and Zimmermann J. Tyrosine kinase inhibitors: from rational design to clinical trials. Med. Res. Rev. 21 (2001) 499-512
26. Laird A.D., and Cherrington J.M. Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. Expert Opin. Invest. Drugs 12 (2003) 51-64
27. Arora A., and Scholar E.M. Role of tyrosine kinase inhibitors in cancer therapy. J. Pharmacol. Exp. Ther. 315 (2005) 971-979
28. Herbst R.S., Onn A., and Sandler A. Angiogenesis and lung cancer: prognostic and therapeutic implications. J. Clin. Oncol. 23 (2005) 3243-3256
29. Ferrara N., Hillan K.J., Gerber H.P., and Novotny W. Discovery and development of bevacizumab, an anti-VEGF antibody for treating cancer. Nat. Drug Discov. 3 (2004) 391-400
30. Ferrara N., Hillan K.J., and Novotny W. Bevacizumab (Avastin), a humanized anti-VEGF monoclonal antibody for cancer therapy. Biochem. Biophys. Res. Commun. 333 (2005) 328-335
31. Parast C.V., Mroczkowski B., Pinko C., Misialek S., Khambatta G., and Appelt K. Characterization and kinetic mechanism of catalytic domain of human vascular endothelial growth factor receptor-2 tyrosine kinase (VEGFR2 TK), a key enzyme in angiogenesis. Biochemistry 37 (1998) 16788-16801
32. Kendall R.L., Rutledge R.Z., Mao X., Tebben A.J., Hungate R.W., and Thomas K.A. Vascular endothelial growth factor receptor Kdr tyrosine kinase activity is increased by autophosphorylation of two activation loop tyrosine residues. J. Biol. Chem. 274 (1999) 6453-6460
33. Zhao G., Meier T.I., Peery R.B., Matsushima P., and Skatrud P.L. Biochemical and molecular analyses of the C-terminal domain of Era GTPase from Streptococcus pneumoniae. Microbiology 145 (1999) 791-800
34. Fry D.W. Mechanism of action of erbB tyrosine kinase inhibitors. Exp. Cell Res. 284 (2003) 131-139