Potent inhibition of angiogenesis by D,L-peptides derived from vascular endothelial growth factor receptor 2

Thrombosis and Haemostasis

Volumn 90, Issue 3, 2003, Pages 501-510

  Piossek, Christine ^f   Thierauch, Karl Heinz ^b   Schneider Mergener, Jens ^c,d   Volkmer Engert, Rudolf ^c   Bachmann, Martin F ^f   Korff, Thomas ^e   Augustin, Hellmut G ^e   Germeroth, Lothar ^a  

^a IBA GmbH   (Germany)

^b BAYER PHARMA AG   (Germany)

^c CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

^d Jerini AG   (Germany)

^e TUMOR BIOLOGY CENTER   (Germany)

^f CYTOS BIOTECHNOLOGY AG   (Switzerland)

Author keywords

Angiogenesis; D,L peptides; Endothelial cells; Spheroid sprouting assay; VEGFR 2

Indexed keywords

ANGIOGENESIS INHIBITOR; PEPSPOTS; PEPTIDE DERIVATIVE; VASCULOTROPIN; VASCULOTROPIN RECEPTOR 2;

AMINO ACID SUBSTITUTION; ANGIOGENESIS; ARTICLE; ASSAY; AUTOPHOSPHORYLATION; BINDING SITE; CANCER; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG DESIGN; DRUG EFFECT; DRUG POTENCY; DRUG STABILITY; DRUG SYNTHESIS; ENDOTHELIUM CELL; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; NEWBORN; PRIORITY JOURNAL; PROTEIN BINDING; SPHEROID CELL;

EID: 0141540653     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1160/th03-02-0106     Document Type: Article

References (45)

1. Risau W. Mechanisms of angiogenesis. Nature 1997; 386(6626): 671-4.
2. Aiello LP, Pierce EA, Foley ED, Takagi H, Chen H, Riddle L, et al. Suppression of retinal neovascularization in vivo by inhibition of vascular endothelial growth factor (VEGF) using soluble VEGF-receptor chimeric proteins. Proc Natl Acad Sci U S A 1995; 92(23): 10457-61.
3. Folkman J. Angiogenesis in cancer, vascular, rheumatoid and other disease. Nat Med 1995; 1(1): 27-31.
4. Ferrara N, Alitalo K. Clinical applications of angiogenic growth factors and their inhibitors. Nat Med 1999; 5(12): 1359-64.
5. Ferrara N, Houck K, Jakeman L, Leung DW. Molecular and biological properties of the vascular endothelial growth factor family of proteins. Endocr Rev 1992; 13(1): 18-32.
6. Gospodarowicz D, Abraham JA, Schilling J. Isolation and characterization of a vascular endothelial cell mitogen produced by pituitary-derived folliculo stellate cells. Proc Natl Acad Sci U S A 1989; 86(19): 7311-5.
7. Neufeld G, Tessler S, Gitay-Goren H, Cohen T, Levi BZ. Vascular endothelial growth factor and its receptors. Prog Growth Factor Res 1994; 5(1): 89-97.
8. Dvorak HF, Nagy JA, Feng D, Brown LF, Dvorak AM. Vascular permeability factor/vascular endothelial growth factor and the significance of microvascular hyperpermeability in angiogenesis. Curr Top Microbiol Immunol 1999; 237: 97-132.
9. Plouet J, Schilling J, Gospodarowicz D. Isolation and characterization of a newly identified endothelial cell mitogen produced by AtT-20 cells. Embo J 1989; 8(12): 3801-6.
10. Leung DW, Cachianes G, Kuang WJ, Goeddel DV, Ferrara N. Vascular endothelial growth factor is a secreted angiogenic mitogen. Science 1989; 246(4935): 1306-9.
11. Ferrara N, Carver-Moore K, Chen H, Dowd M, Lu L, O'Shea KS, et al. Heterozygous embryonic lethality induced by targeted inactivation of the VEGF gene. Nature 1996; 380(6573): 439-42.
12. Carmeliet P, Ferreira V, Breier G, Pollefeyt S, Kieckens L, Gertsenstein M, et al. Abnormal blood vessel development and lethality in embryos lacking a single VEGF allele. Nature 1996; 380(6573): 435-9.
13. Schuh AC, Faloon P, Hu QL, Bhimani M, Choi K. In vitro hematopoietic and endothelial potential of flk-1(-/-) embryonic stem cells and embryos. Proc Natl Acad Sci USA 1999; 96(5): 2159-64.
14. Dumont DJ, Jussila L, Taipale J, Lymboussaki A, Mustonen Pajusola K, et al. Cardiovascular failure in mouse embryos deficient in VEGF receptor-3. Science 1998; 282(5390): 946-9.
15. Fong GH, Rossant J, Gertsenstein M, Breitman ML. Role of the Flt-1 receptor tyrosine kinase in regulating the assembly of vascular endothelium. Nature 1995; 376(6535): 66-70.
16. Shalaby F, Rossant J, Yamaguchi TP, Gertsenstein M, Wu XF, Breitman ML, et al. Failure of blood-island formation and vasculogenesis in Flk-1-deficient mice. Nature 1995; 376(6535): 62-6.
17. Jakeman LB, Winer J, Benneth GL, Altar CA, Ferrara N. Binding sites for vascular endothelial growth factor are localized on endothelial cells in adult rat tissues. J Clin Invest 1992; 89(1): 244-53.
18. Makinen T, Jussila L, Veikkola T, Karpanen T, Kettunen MI, Pulkkanen KJ, et al. Inhibition of lymphangiogenesis with resulting lymphedema in transgenic mice expressing soluble VEGF receptor-3. Nat Med 2001; 7(7): 199-205.
19. Brekken RA, Overholser JP, Stastny VA, Waltenberger J, Minna JD, Thorpe PE. Selective inhibition of vascular endothelial growth factor (VEGF) receptor 2 (KDR/Flk-1) activity by a monoclonal anti-VEGF antibody blocks tumor growth in mice. Cancer Res 2000; 60(18): 5117-24.
20. Borgstrom P, Hillan KJ, Sriramarao P, Ferrara N. Complete inhibition of angiogenesis and growth of microtumors by anti-vascular endothelial growth factor neutralizing antibody: Novel concepts of angiostatic therapy from intravital videomicroscopy. Cancer Res 1996; 56(17): 4032-9.
21. Kim KJ, Li B, Winer J, Armanini M, Gillett N, Phillips HS, et al. Inhibition of vascular endothelial growth factor-induced angiogenesis suppresses tumour growth in vivo. Nature 1993; 362(6423): 841-4.
22. Prewett M, Huber J, Li Y, Santiago A, O'Connor W, King K, et al. Antivascular endothelial growth factor receptor (fetal liver kinase 1) monoclonal antibody inhibits tumor angiogenesis and growth of several mouse and human tumors. Cancer Res 1999; 59 (20): 5209-18.
23. Skobe M, Rockwell P, Goldstein N, Vosseler S, Fusenig NE. Halting angiogenesis suppresses carcinoma cell invasion. Nat Med 1997; 3(11): 1222-7.
24. Witte L, Hicklin DJ, Zhu Z, Pytowski B, Kotanides H, Rockwell P, et al. Monoclonal antibodies targeting the VEGF receptor-2 (Flk1/KDR) as an anti-angiogenic therapeutic strategy. Cancer Metastasis Rev 1998; 17(2): 155-61.
25. Lin P, Sankar S, Shan S, Dewhirst MW, Polverini PJ, Quinn TQ, et al. Inhibition of tumor growth by targeting tumor endothelium using a soluble vascular endothelial growth factor receptor. Cell Growth Differ 1998; 9(1): 49-58.
26. Goldman CK, Kendall RL, Cabrera G, Soroceanu L, Heike Y, Gillespie GY, et al. Paracrine expression of a native soluble vascular endothelial growth factor receptor inhibits tumor growth, metastasis, and mortality rate. Proc Natl Acad Sci USA 1998; 95(15): 8795-800.
27. Pan B, Li B, Russell SJ, Tom JY, Cochran AG, Fairbrother WJ. Solution structure of a phage-derived peptide antagonist in complex with vascular endothelial growth factor. J Mol Biol 2002; 316(3): 769-87.
28. Binetruy-Tournaire R, Demangel C, Malavaud B, Vassy R, Rouyre S, Kraemer M, et al. Identification of a peptide blocking vascular endothelial growth factor (VEGF)-mediated angiogenesis. Embo J 2000; 19(7): 1525-33.
29. Fong TA, Shawver LK, Sun L, Tang C, App H, Powell TJ, et al. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res 1999; 59(1): 99-106.
30. Wood J. Pharmacological profile of a potent and orally active inhibitor of VEGF receptor tyrosine kinases. Proc. Am. Assoc. Cancer Res. 1998; 39: 96.
31. Hamby JM, Showalter HD. Small molecule inhibitors of tumor-promoted angiogenesis, including protein tyrosine kinase inhibitors. Pharmacol Ther 1999; 82(2-3): 169-93.
32. Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Lohmann JJ, et al. Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors. J Med Chem 1999; 42(26): 5369-89.
33. Piossek C, Schneider-Mergener J, Schirner M, Vakalopoulou E, Germeroth L, Thierauch KH. Vascular endothelial growth factor (VEGF) receptor II-derived peptides inhibit VEGF. J Biol Chem 1999; 274(9): 5612-9.
34. Frank RW. Tetrahedron 1992; 48: 9217-9232.
35. Kramer A. Comp. Methods Enzymol 1994; 6: 388-395.
36. Gausepohl H, Boulin C, Kraft M, Frank RW. Automated multiple peptide synthesis. Pept Res 1992; 5(6): 315-20.
37. Korff T, Augustin HG. Tensional forces in fibrillar extracellular matrices control directional capillary sprouting. J Cell Sci 1999; 112(Pt 19): 3249-58.
38. Korff T, Kimmina S, Martiny-Baron G, Augustin HG. Blood vessel maturation in a 3-dimensional spheroidal coculture model: Direct contact with smooth muscle cells regulates endothelial cell quiescence and abrogates VEGF responsiveness. Faseb J 2001; 15 (2): 447-57.
39. Goodman M, Chorev M. On the concept of linear modified retro-peptide structures. Accounts Chem Res 1979; 12: 1-7.
40. Chorev M, Goodman M. Recent developments in retro peptides and proteins - An ongoing topochemical exploration. Trends Biotechnol 1995 1995; 13: 438-445.
41. Schumacher TN, Mayr LM, Minor DL, Jr., Milhollen MA, Burgess MW, Kim PS. Identification of D-peptide ligands through mirror-image phage display. Science 1996; 271(5257): 1854-7.
42. Eckert DM, Malashkevich VN, Hong LH, Carr PA, Kim PS. Inhibiting HIV-1 entry: Discovery of D-peptide inhibitors that target the gp41 coiled-coil pocket. Cell 1999; 99(1): 103-15.
43. Kramer A, Stigler RD, Knaute T, Hoffmann B, Schneider-Mergener J. Stepwise transformation of a cholera toxin and a p24 (HIV-1) epitope into D-peptide analogs. Protein Eng 1998; 11(10): 941-8.
44. Kramer A, Reineke U, Dong L, Hoffmann B, Hoffmuller U, Winkler D, et al. Spot synthesis: Observations and optimizations. J Pept Res 1999; 54(4): 317-27.
45. Hagedorn M, Bikfalvi A. Target molecules for anti-angiogenic therapy: From basic research to clinical trials. Crit Rev Oncol Hematol 2000; 34(2): 89-110.