Generating improved single-chain Fv molecules for tumor targeting

Journal of Immunological Methods

Volumn 231, Issue 1-2, 1999, Pages 249-260

  Adams, Gregory P ^a   Schier, Robert ^b  

^a FOX CHASE CANCER CENTER   (United States)

^b Xenon Pharmaceuticals   (Germany)

Author keywords

Affinity; Mutagenesis; Phage display; Single chain Fv (scFv); Valence

Indexed keywords

MONOCLONAL ANTIBODY;

ANTIGEN BINDING; ANTIGEN RECOGNITION; ARTICLE; CANCER; IMAGING; MUTAGENESIS; PHAGE DISPLAY; PRIORITY JOURNAL; TUMOR;

ANIMALS; ANTIBODIES, NEOPLASM; ANTIBODY AFFINITY; DRUG DELIVERY SYSTEMS; GENETIC ENGINEERING; HUMANS; HYBRIDOMAS; IMMUNOGLOBULIN FRAGMENTS; IMMUNOGLOBULIN VARIABLE REGION; MUTAGENESIS, SITE-DIRECTED; NEOPLASMS; PEPTIDE LIBRARY; TUMOR CELLS, CULTURED;

EID: 0033506131     PISSN: 00221759     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0022-1759(99)00161-1     Document Type: Article

References (63)

1. Adams, G.P., 1998. Improving the tumor specificity and retention of antibody-based molecules. In Vivo 12, 11-22.
2. Adams, D.P., McCartney, J.E., Tai, M.-S., Oppermann, H., Huston, J.S., Stafford, W.F., Bookman, M.A., Fand, I., Houston, L.L., Weiner, L.M., 1993. Highly specific in vivo tumor targeting by monovalent and divalent forms of 741F8 anti-c-erbB-2 single-chain Fv. Cancer Res. 53, 4026-4034.
3. Adams, G.P., Schier, R., Marshall, K., Wolf, E.J., McCall, A.M., Marks, J.D., Weiner, L.M., 1998a. Increased affinity leads to improved selective tumor delivery of single-chain Fv antibodies. Cancer Res. 58, 485-490.
4. Adams, G.P., Schier, R., McCall, A.M., Simmons, H., Horak, E., Marks, J.D., Weiner, L.M., 1998b. What are the determinants of antibody-based targeting?. Proc. Am. Assoc. Cancer Res. 39, 436.
5. Adams, G.P., Schier, R., McCall, A.M., Crawford, R.S., Wolf, E.J., Weiner, L.M., Marks, J.D., 1998c. Prolonged in vivo tumor retention of a human diabody targeting the extracellular domain of human HER2/neu. Brit. J. Cancer 77, 1405-1412.
6. Balint, R.F., Larrick, J.W., 1993. Antibody engineering by parsimonious mutagenesis. Gene 137, 109-118.
7. Behr, T.M., Goldenberg, D.M., Becker, W., 1998. Reducing renal accretion of radiolabelled antibody fragments and peptides: improvement of therapeutic efficacy by overcoming nephrotoxic potential? A review. Tumor Targeting 3, 2-12.
8. Bird, R.E., Hardman, K.D., Jacobson, J.W., Johnson, S., Kaufman, B.M., Lee, S.M., Lee, T., Pope, S.H., Riordan, G.S., Whitlow, M., 1988. Single-chain antigen-binding proteins. Science 242, 423-426.
9. Chang, R.S., Ueki, I.F., Troy, J.L., Deen, W.M., Robertson, C.R., Brenner, B.M., 1975. Permselectivity of the glomerular capillary wall to macromolecules: II. Experimental studies in rat using neutral dextran. Biophys. J. 15, 887-906.
10. Clackson, T., Hoogenboom, H.R., Griffiths, A.D., Winter, G., 1991. Making antibody fragments using phage display libraries. Nature 352, 624-628.
11. Colcher, D., Bird, R., Roselli, M., Hardman, K.D., Johnson, S., Pope, S., Dodd, S.W., Pantoliano, M.W., Milenic, D.E., Schlom, J., 1990. In vivo tumor targeting of a recombinant single-chain antigen-binding protein. J. Natl. Cancer Inst. 82, 1191-1197.
12. Crameri, A., Cwirla, S., Stemmer, W.P., 1996. Construction and evolution of antibody-phage libraries by DNA shuffling. Nat. Med. 2, 100-102.
13. de Kruif, J., Boel, E., Logtenberg, T., 1995a. Selection and application of human single-chain Fv antibody fragments from a semi-synthetic phage antibody display library with designed CDR3 regions. J. Mol. Biol. 21 (248), 97-105.
14. de Kruif, J., Terstappen, L., Boel, E., Logtenberg, T., 1995b. Rapid selection of cell subpopulation-specific human monoclonal antibodies from a synthetic phage antibody library. Proc. Natl. Acad. Sci. U.S.A. 92, 3938-3942.
15. Deo, Y.M., Graziano, R.F., Repp, R., van de Winkel, J.G.J., 1997. Clinical significance of IgG Fc receptors and Fc-γR-directed immunotherapies. Immunol. Today 18, 127-134.
16. Figini, M., Obici, L., Mezzanzanica, D., Griffiths, A., Colnaghi, M.I., Winter, G., Canevari, S., 1998. Panning phage antibody libraries on cells: isolation of human Fab fragments against ovarian carcinoma using guided selection. Cancer Res. 58, 991-996.
17. 2 and Fab in tumors. Cancer Res. 49, 5656-5663.
18. Ghetie, V., Ward, E.S., 1997. FcRn: the MHC class I-related receptor that is more than an IgG transporter. Immunol. Today 18, 592-598.
19. Griffiths, A.D., Williams, S.C., Hartley, O., Tomlinson, I.M., Waterhouse, P., Crosby, W.L., Kontermann, R.E., Jones, P.T., Low, N.M., Allison, T.J., Prospero, T.D., Hoogenboom, H.R., Nissim, A., Cox, J.P.L., Harrison, J.L., Zaccolo, M., Gherardi, E., Winter, G., 1994. Isolation of high affinity human antibodies directly from large synthetic repertoires. EMBO J. 13, 3245-3260.
20. Hanes, J., Pluckthun, A., 1997. In vitro selection and evolution of functional proteins by using ribosome display. Proc. Natl. Acad. Sci. U.S.A. 94, 4937-4942.
21. Hanes, J., Jermutus, L., Weber-Bornhauser, S., Bosshard, H.R., Pluckthun, A., 1998. Ribosome display efficiently selects and evolves high-affinity antibodies in vitro from immune libraries. Proc. Natl. Acad. Sci. U.S.A. 95, 14130-14135.
22. Hawkins, R.E., Russell, S.J., Winter, G., 1992. Selection of phage antibodies by binding affinity. Mimicking affinity maturation. J. Mol. Biol. 226, 889-896.
23. Holliger, P., Prospero, T., Winter, G., 1993. "Diabodies": small bivalent and bispecific antibody fragments. Proc. Natl. Acad. Sci. U.S.A. 90, 444-6448.
24. H gene segments rearranged in vitro. J. Mol. Biol. 227, 381-388.
25. Hudson, P.J., Kortt, A.A., 1999. J. Immunol. Methods (this issue).
26. Hu Shi-zhen, S.L., Andrew, R., Mark, S., Williams Lawrence, E., Wong Jeffrey, Y.C., Shively John, E., Wu Anna, M., 1996. Minibody: a novel engineered anti-carcinoembryonic antigen antibody fragment (single-chain Fv-CH3) which exhibits rapid, high-level targeting of xenografts. Cancer Res. 56, 3055-3061.
27. Huston, J.S., Levinson, D., Mudgett, H.M., Tai, M.S., Novotny, J., Margolies, M.N., Ridge, R.J., Bruccoleri, R.E., Haber, E., Crea, R., Oppermann, H., 1988. Protein engineering of antibody binding sites: recovery of specific activity in an anti-digoxin single-chain Fv analogue produced in Escherichia coli. Proc. Natl. Acad. Sci. U.S.A. 85, 5879-5883.
28. Iliades, P., Kortt, A.A., Hudson, P.J., 1998. Triabodies: single-chain Fv fragments without a linker form trivalent trimers. FEBS Letters 409, 437-441.
29. Irving, R.A., Kortt, A.A., Hudson, P.J., 1996. Affinity maturation of recombinant antibodies using E. coli mutator cells. Immunotechnology 2, 127-143.
30. Jackson, H., Bacon, L., Pedley, R.B., Derbyshire, E., Field, A., Osbourn, J., Allen, D., 1998. Antigen specificity and tumor targeting efficiency of a human carcinoembryonic antigen-specific scFv and affinity-matured derivatives. Br. J. Cancer 78, 181-188.
31. Jain, R.K., 1998. The next frontier of molecular medicine: delivery of therapeutics. Nat. Med. 4, 655-657.
32. Jain, R.K., Baxter, L.T., 1988. Mechanisms of heterogeneous distribution of monoclonal antibodies and other macromolecules in tumors: significance of elevated interstitial pressure. Cancer Res. 48, 7022-7032.
33. Juweid, M., Neumann, R., Paik, C., Perez-Bacete, M.J., Sato, J., van Osdol, W., Weinstein, J.N., 1992. Micropharmacology of monclonal antibodies in solid tumors: direct experimental evidence for a binding site barrier. Cancer Res. 52, 5144-5153.
34. Kobayashi, H., Le, N., Kim, M.-K., Pie, J.-E., Drumm, D., Paik, D.S., Waldmann, T.A., Paik, C.H., Carrasquillo, J.A., 1999. The pharmacokinetic characteristics of glycolated humanized anti-Tac Fabs are determined by their isoelectric points. Cancer Res. 59, 422-430.
35. Lawrence, L.J., Kortt, A.A., Iliades, P., Tulloch, P.A., Hudson, P.J., 1998. Orientation of antigen binding sites in dimeric and trimeric single-chain Fv antibody fragments. FEBS Letters 425, 479-484.
36. Low, N.M., Holliger, P.H., Winter, G., 1996. Mimicking somatic hypermutation: affinity maturation of antibodies displayed on bacteriophage using a bacterial mutator strain. J. Mol. Biol. 260, 359-368.
37. Maack, T., Johnson, V., Kan, S.T., Figueiredo, J., Sigulem, D., 1979. Renal filtration, transport and metabolism of low molecular weight proteins: a review. Kidney Int. 16, 251-270.
38. Marks, J.D., Hoogenboom, H.R., Bonnert, T.P., McCafferty, J., Griffiths, A.D., Winter, G., 1991. By-passing immunization. Human antibodies from V-gene libraries displayed on phage. J. Mol. Biol. 222, 581-597.
39. Marks, J.D., Griffiths, A.D., Malmqvist, M., Clackson, T.P., Bye, J.M., Winter, G., 1992. By-passing immunization: building high affinity human antibodies by chain shuffling. Bio/Technology 10, 779-783.
40. Milenic, D.E., Yokota, T., Filpula, D.R., Finkelman, M.A.J., Dodd, S.W., Wood, J.F., Whitlow, M., Snow, P., Schlom, J., 1991. Construction, binding properties, metabolism, and targeting of a single-chain Fv derived from the pancarcinoma monoclonal antibody CC49. Cancer Res. 51, 6363-6371.
41. Muller, K.M., Arndt, K.M., Pluckthun, A., 1998. A dimeric bispecific miniantibody combines two specificities with avidity. FEBS Letters 432, 45-49.
42. Nissim, A., Hoogenboom, H.R., Tomlinson, I.M., Flynn, G., Midgley, C., Lane, D., Winter, G., 1994. Antibody fragments from a 'single pot' phage display library as immunochemical reagents. EMBO J. 13, 692-869.
43. Osbourn, J.K., Field, A., Wilton, J., Derbyshire, E., Earnshaw, J.C., Jones, P.T., Allen, D., McCafferty, J., 1996. Generation of a panel of related human scFv antibodies with high affinity for human CEA. Immunotechnology 2, 181-196.
44. v fragments with high affinity in Escherichia coli. Biochemistry 31, 1579-1584.
45. Pereira, S., Maruyama, H., Siegel, D., Van Belle, P., Elder, D., Curtis, P., Herlyn, D., 1997. A model system for detection and isolation of a tumor cell surface antigen using antibody phage display. J. Immunol. Methods 203, 11-24.
46. Pini, A., Spreafico, A., Botti, R., Neri, D., Neri, P., 1997. Hierarchical affinity maturation of a phage library derived antibody for the selective removal of cytomegalovirus from plasma. J. Immunol. Methods 206, 171-182.
47. Purtell, J.N., Pesce, A.J., Clyne, D.H., Miller, N.C., Pollak, V.F., 1979. Isoelectric point of albumin: effect on renal handling of albumin. Kidney Int. 16, 366-376.
48. Rader, C., Cheresh, D.A., Barbas, C.F. 3rd, 1998. A phage display approach for rapid antibody humanization: designed combinatorial V gene libraries. Proc. Natl. Acad. Sci. U.S.A. 95, 8910-8915.
49. Schier, R., Marks, J.D., Wolf, E.J., Appell, G., Huston, J.S., Weiner, L.M., Adams, G.P., 1995. In vitro and in vivo characterization of a human anti-c-erbB-2 single-chain Fv isolated from a filamentous phage antibody library. Immunotechnology 1, 63-71.
50. Schier, R., Bye, J., Apell, G., McCall, A., Adams, G.P., Malmqvist, M., Weiner, L.M., Marks, J.D., 1996a. Isolation of high-affinity monomeric human anti-c-erbB-2 single-chain Fv using affinity-driven selection. J. Mol. Biol. 255, 28-43.
51. Schier, R., McCall, A., Adams, G.P., Marshall, K.W., Merritt, H., Yim, M., Crawford, R.S., Weiner, L.M., Marks, J.D., 1996b. Isolation of picomolar affinity anti-c-erbB-2 single-chain Fv by molecular evolution of the complementarity determining regions in the center of the antibody binding site. J. Mol. Biol. 263, 551-567.
52. Schier, R., Balint, R.F., McCall, A., Apell, G., Larrick, J.W., Marks, J.D., 1996c. Identification of functional and structural amino acid residues by parsimonious mutagenesis. Gene 169, 147-155.
53. Sheets, M.D., Amersdorfer, P., Finnern, R., Sargent, P., Lindqvist, E., Schier, R., Hemingsen, G., Wong, C., Gerhart, J.C., Marks, J.D., 1998. Efficient construction of a large nonimmune phage antibody library: the production of high-affinity human single-chain antibodies to protein antigens. Proc. Natl. Acad. Sci. U.S.A. 95, 6157-6162.
54. Stemmer, W.P., 1994. Rapid evolution of a protein in vitro by DNA shuffling. Nature 370, 389-391.
55. Thompson, J., Pope, T., Tung, J.S., Chan, C., Hollis, G., Mark, G., Johnson, K.S., 1996. Affinity maturation of a high-affinity human monoclonal antibody against the third hypervariable loop of human immunodeficiency virus: use of phage display to improve affinity and broaden strain reactivity. J. Mol. Biol. 256, 77-88.
56. Tordsson, J., Abrahmsen, L., Kalland, T., Ljung, C., Ingvar, C., Brodin, T., 1997. Efficient selection of scFv antibody phage by adsorption to in situ expressed antigens in tissue sections. J. Immunol. Methods 210, 11-23.
57. Vaughan, T.J., Williams, A.J., Pritchard, K., Osbourn, J.K., Pope, A.R., Earnshaw, J.C., MaCafferty, J., Hodits, R.A., Wilton, J., Johnson, K.S., 1996. Human antibodies with sub-nanomolar affinities isolated from a large non-immunized phage display library. Nature Biotechnology 14, 309-314.
58. H shuffling can be used to convert an Fv fragment of anti-hen egg lysozyme specificity to one that recognizes a T cell receptor Va. Mol. Immunol. 32, 147-156.
59. Weinstein, J.N., Eger, R.R., Covell, D.G., Black, C.D.V., Mulshine, J., Carrasquillo, J.A., Larson, S.M., Keenan, A.M., 1987. The pharmacology of monoclonal antibodies. Ann. N. Y. Acad. Sci. 507, 199-210.
60. Winter, G., Griffiths, A.D., Hawkins, R.E., Hoogenboom, H.R., 1994. Making antibodies by phage display technology. Annu. Rev. Immunol. 12, 433-455.
61. Yang, W.P., Green, K., Pinz-Sweeney, S., Briones, A.T., Burton, D.R., Barbas, C.F. 3rd, 1995. CDR walking mutagenesis for the affinity maturation of a potent human anti-HIV-1 antibody into the picomolar range. J. Mol. Biol. 254, 392-403.
62. Yokota, T., Milenic, D., Whitlow, M., Schlom, J., 1992. Rapid tumor penetration of a single-chain Fv and comparison with other immunoglobulin forms. Cancer Res. 52, 3402-3408.
63. Yuan, F., Dellian, M., Fukumura, D., Leunig, M., Berk, D.A., Torchilin, V.P., Jain, R.K., 1995. Vascular permeability in a human tumor xenograft: molecular size dependence and cutoff size. Cancer Res. 55, 3752-3756.