Semirational design of a potent, artificial agonist of fibroblast growth factor receptors

Nature Biotechnology

Volumn 17, Issue 12, 1999, Pages 1199-1204

  Ballinger, Marcus D ^a   Shyamala, Venkatakrishna ^a   Forrest, Louise D ^a   Deuter Reinhard, Maja ^a   Doyle, Laura V ^a   Wang, Jian Xin ^a   Panganiban Lustan, Lootsee ^a   Stratton, Jennifer R ^a   Apell, Gerald ^a   Winter, Jill A ^a   Doyle, Michael V ^a   Rosenberg, Steven ^a   Kavanaugh, W Michael ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Angiogenesis; Cytokines; Fibroblast growth factor; Ligands; Mimetics; Protein design; Receptors

Indexed keywords

FIBROBLAST GROWTH FACTOR; FIBROBLAST GROWTH FACTOR RECEPTOR; HEPARIN; HYBRID PROTEIN; MITOGENIC AGENT;

ANIMAL CELL; ARTICLE; DRUG DESIGN; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; MITOGENESIS; NONHUMAN; PHAGE DISPLAY; PRIORITY JOURNAL; TREATMENT INDICATION;

ANGINA; ANIMALIA;

EID: 17444406988     PISSN: 10870156     EISSN: None     Source Type: Journal    
DOI: 10.1038/70746     Document Type: Article

References (38)

1. Mason, I.J. The ins and cuts of fibroblast growth factors. Cell 78, 547-552 (1994).
2. Wilkie, A.O., Morriss-Kay, G.M., Jones, E.Y. & Heath, J.K. Functions of fibroblast growth factors and their receptors. Curr. Biol. 5, 500-507 (1995).
3. Asahara, T. et al. Synergistic effect of vascular endothelial growth factor and basic fibroblast growth factor on angiogenesis in vivo. Circulation 1, II365-II371 (1995).
4. Baffour, R. et al. Enhanced angiogenesis and growth of collaterals by in vivo administration of recombinant basic fibroblast growth factor in a rabbit model of acute lower limb ischemia: dose-response effect of basic fibroblast growth factor. J. Vasc. Surg. 16, 181-191 (1992).
5. Harada, K. et al. Basic fibroblast growth factor improves myocardial function in chronically ischemic porcine hearts. J. Clin. Invest. 94, 623-630 (1994).
6. Landau, C., Jacobs, A.K. & Haudenschild, C.C. Intrapericardial basic fibroblast growth factor induces myocardial angiogenesis in a rabbit model of chronic ischemia. An. Heart J. 129, 924-931 (1995).
7. Lazarous, D.F. et al. Effects of chronic systemic administration of basic fibroblast growth factor on collateral development in the canine heart. Circulation 91, 145-153 (1995).
8. Yanagisawa-Miwa, A. et al. Salvage of infarcted myocardium by angiogenic action of basic fibroblast growth factor. Science 257, 1401-1403 (1992).
9. Koketsu, N. et al. Pretreatment with intraventricular basic fibroblast growth factor decreases infarct size following focal cerebral ischemia in rats. Ann. Neurol. 35, 451-457 (1994).
10. Tian, S.S. et al. A small, nonpeptidyl mimic of granulocyte-colony-stimulating factor. Science 281, 257-259 (1998).
11. Cwirla, S.E. et al. Peptide agonist of the thrombopoietin receptor as potent as the natural cytokine. Science 276, 1696-1699 (1997).
12. Wrighton, N.C. et al. Small peptides as potent mimetics of the protein hormone erythropoietin. Science 273, 458-464 (1996).
13. Zhang, B. et al. Discovery of a small molecule insulin mimetic with antidiabetic activity in mice. Science 284, 974-977 (1999).
14. Waksman, G. & Herr, A.B. New insights into heparin-induced FGF oligomerization. Nat. Struct. Biol. 5, 527-530 (1998).
15. Bellot, F. et al. Ligand-induced transphosphorylation between different FGF receptors. EMBO J. 10, 2849-2854 (1991).
16. Baird, A., Schubert, D., Ling, N. & Guillemin, R. Receptor- and heparin-binding domains of basic fibroblast growth factor. Proc. Natl. Acad. Sci. USA 85, 2324-2328 (1988).
17. Gallagher, J.T. & Turnbull, J.E. Heparan sulphate in the binding and activation of basic fibroblast growth factor. Glycobiology 2, 523-528 (1992).
18. Moy, F.J. et al. Properly oriented heparin-decasaccharide-induced dimers are the biologically active form of basic fibroblast growth factor. Biochemistry 36, 4782-4791 (1997).
19. DiGabriele, A.D. et al Structure of a heparin-linked biologically active dimer of fibroblast growth factor. Nature 393, 812-817 (1998).
20. Spivak-Kroizman, T. et al. Heparin-induced oligomerization of FGF molecules is responsible for FGF receptor dimerization, activation, and cell proliferation. Cell 79, 1015-1024 (1994).
21. Riley, L.G. et al. Cloning, expression, and spectroscopic studies of the Jun leucine zipper domain. Eur. J. Biochem. 219, 877-886 (1994).
22. Patel, L.R., Curran, T. & Kerppola, T.K. Energy transfer analysis of Fos-Jun dimerization and DNA binding. Proc. Natl. Acad. Sci. USA 91, 7360-7364 (1994).
23. Crameri, R. & Suter, M. Display of biologically active proteins on the surface of filamentous phages: a cDNA cloning system for the selection of functional gene products linked to the genetic information responsible for their production. Gene 160, 139 (1995).
24. de Kruif, J. & Logtenberg, T. Leucine zipper dimerized bivalent and bispecific scFv antibodies from a semi-synthetic antibody phage display library. J. Biol. Chem. 271, 7630-7634 (1996).
25. Claude, P., Parada, I.M., Gordon, K.A., D'Amore, P.A. & Wagner, J.A. Acidic fibroblast growth factor stimulates adrenal chromaffin cells to proliferate and to extend neurites, but is not a long-term survival factor. Neuron 1, 783-790 (1988).
26. Marshall, C.J. Specificity of receptor tyrosine kinase signaling: transient versus sustained extracellular signal-regulated kinase activation. Cell 80, 179-185 (1995).
27. Werner, S. et al. Differential splicing in the extracellular region of fibroblast growth factor receptor 1 generates receptor variants with different ligand-binding specificities. Mot. Cell. Biol. 12, 82-88 (1992).
28. Wang, F., Kan, M., Xu, J., Yan, G. & McKeehan, W.L. Ligand-specific structural domains in the fibroblast growth factor receptor. J. Biol. Chem. 270, 10222-10230 (1995).
29. Hulme, E.G. & Birdsall, N.J.M. in Receptor-ligand interactions: a practical approach (ed. Hulme, E.G.) 101-104 (Oxford University Press, New York; 1993).
30. Ray, J., Baird, A. & Gage, F.H. A 10-amino acid sequence of fibroblast growth factor 2 is sufficient for its mitogenic activity on neural progenitor cells. Proc. Natl. Acad. Sci. USA 94, 7047-7052 (1997).
31. Yayon, A. et al. Isolation of peptides that inhibit binding of basic fibroblast growth factor to its receptor from a random phage-epitope library. Proc. Natl. Acad. Sci. USA 90, 10643-10647 (1993).
32. Pantoliano, M.W. et al. Multivalent ligand-receptor binding interactions in the fibroblast growth factor system produce a cooperative growth factor and heparin mechanism for receptor dimerization. Biochemistry 33, 10229-10248 (1994).
33. Plotnikov, A.N., Schlessinger, J., Hubbard, S.R. & Mohammadi, M. Structural basis for FGF receptor dimerization and activation. Cell 98, 641-650 (1999).
34. Doyle, M.V. et al. in Combinatorial libraries: synthesis, screening and application potential (ed. Cortese, R.) 171 (Walter de Gruyter, New York; 1996).
35. Kiefer, M.C. et al. Molecular cloning of a human basic fibroblast growth factor receptor cDNA and expression of a biologically active extracellular domain in a baculovirus system. Growth Factors 5, 115-127 (1991).
36. Grussenmeyer, T., Scheidtmann, K.H., Hutchinson, M.A., Eckhart, W. & Walter, G. Complexes of polyoma virus medium T antigen and cellular proteins. Proc. Natl. Acad. Sci. USA 82, 7952-7954 (1985).
37. Laminet, A.A., Apell, G., Conroy, L. & Kavanaugh, W.M. Affinity, specificity, and kinetics of the interaction of the SHC phosphotyrosine binding domain with asparagine-X-X-phosphotyrosine motifs of growth factor receptors. J. Biol. Chem. 271, 264-269 (1996).
38. Shyamala, V. et al. High-throughput screening for ligand-induced c-fos mRNA expression by branched DNA assay in Chinese hamster ovary cells. Anal. Biochem. 266, 140-147 (1999).